GPCR/G Protein

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  1. CRF1 receptor antagonist

    Tildacerfont is a potent and orally active corticotropin-releasing factor type 1 (CRF1) receptor antagonist. It effectively reduces levels of adrenocorticotropic hormone (ACTH) and adrenal androgens, demonstrating a favorable safety profile. Tildacerfont is being investigated for the treatment of congenital adrenal hyperplasia (CAH) and holds promise for research into disorders of the hypothalamic-pituitary-adrenal (HPA) axis.
  2. PAF activator

    C16-PAF (PAF (C16)) is a phospholipid mediator and a potent platelet-activating factor that functions as a ligand for the PAF G-protein-coupled receptor (PAFR). It exhibits anti-apoptotic effects by inhibiting caspase-dependent cell death through PAFR activation. C16-PAF is a strong activator of the MAPK and MEK/ERK signaling pathways and is known to induce increased vascular permeability.
  3. 5-HT1A receptor agonist

    Buspirone is an orally active anxiolytic agent that acts as a partial agonist at 5-HT1A receptors and an antagonist at dopamine D2 autoreceptors. It is commonly used in the research and treatment of generalized anxiety disorder (GAD), offering anxiolytic effects without the sedative or dependence-forming properties of benzodiazepines.
  4. Prostaglandin Receptor Antagonist

    AL-8810 is a potent and selective antagonist of the prostaglandin F2α (PGF2α) receptor (FP receptor), with Ki values of 0.2 ± 0.06 μM in mouse 3T3 cells and 0.4 ± 0.1 μM in rat A7r5 cells. In addition to its antagonistic activity, AL-8810 also activates MAPK and ERK1/2 signaling pathways. It is commonly used in research related to elevated intraocular pressure (OHT) and primary open-angle glaucoma (POAG).
  5. mGluR5 allosteric modulator

    CDPPB is a selective, orally active allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5). It enhances AKT and ERK1/2 signaling and upregulates BDNF mRNA expression. CDPPB also inhibits caspase-3 activation and mitigates mitochondrial dysfunction, demonstrating therapeutic potential in improving cognitive impairment, depression, and Huntington’s disease.
  6. PAR2 inhibitor

    I-287 is an orally active and selective protease-activated receptor 2 (PAR2) inhibitor that functions as a negative allosteric modulator, specifically targeting Gαq and Gα12/13 signaling pathways and their downstream effectors. By disrupting PAR2-mediated signaling, I-287 effectively reduces inflammation in preclinical models, including Complete Freund's Adjuvant (CFA)-induced inflammation in mice.
  7. NSAID/COX inhibitor

    Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory drug (NSAID) that functions primarily by inhibiting cyclooxygenase (COX) enzymes, thereby reducing the synthesis of pro-inflammatory prostaglandins. In addition to its classical NSAID activity, Fenoprofen has been identified as a positive allosteric modulator (PAM) of melanocortin receptors (MCRs), enhancing MCR-mediated signaling. Fenoprofen also promotes ERK1/2 activation in HEK293T cells, suggesting additional modulation of intracellular signaling pathways involved in inflammation and cellular proliferation.
  8. OX2R agonist

    Firazorexton (TAK-994 free base) is an orally active, brain-penetrant, and highly selective agonist of the orexin type 2 receptor (OX2R). By activating OX2R, Firazorexton enhances wakefulness and has demonstrated efficacy in preclinical models, notably improving narcolepsy-like symptoms in mice. Its targeted action on the orexin system positions it as a promising therapeutic candidate for sleep disorders such as narcolepsy and excessive daytime sleepiness.
  9. PKA/ERK/CREB activator

    4′-Demethylnobiletin is a bioactive metabolite derived from citrus polymethoxyflavones, known for its neuroprotective and cognition-enhancing properties. It activates the PKA/ERK/CREB signaling pathway and enhances CRE (cAMP response element)-mediated transcription in hippocampal neurons, processes essential for synaptic plasticity and memory formation. Additionally, 4′-Demethylnobiletin reverses memory impairment caused by NMDA receptor antagonism by stimulating ERK signaling, highlighting its therapeutic potential for neurodegenerative diseases and cognitive dysfunction.
  10. OX2R agonist

    Firazorexton hydrate (TAK-994) is an orally active, brain-penetrant selective agonist of the orexin type 2 receptor (OX2R). It effectively promotes wakefulness by stimulating OX2R signaling, which plays a critical role in regulating the sleep–wake cycle. In preclinical studies, Firazorexton hydrate has demonstrated the ability to alleviate narcolepsy-like symptoms in mouse models, making it a promising therapeutic candidate for sleep disorders such as narcolepsy and excessive daytime sleepiness.
  11. NMDAR/TRPM4 inhibitor

    Brophenexin (compound 8) is a potent inhibitor of the interaction interface between NMDA receptors (NMDAR) and TRPM4 channels, exhibiting significant neuroprotective activity. It prevents NMDA-induced excitotoxicity, including cell death and mitochondrial dysfunction in hippocampal neurons, with an IC₅₀ of 2.1 μM. In vivo, Brophenexin protects against brain damage in mice subjected to middle cerebral artery occlusion (MCAO) and preserves retinal ganglion cells from NMDA-induced degeneration. These findings support its potential as a therapeutic agent for neurodegenerative diseases and ischemic brain injury.
  12. CMKLR1 Agonist

    Chemerin-9 (149–157) TFA is a potent peptide agonist of chemokine-like receptor 1 (CMKLR1), exhibiting significant anti-inflammatory activity. It activates downstream signaling pathways by stimulating the phosphorylation of Akt and ERK and promoting reactive oxygen species (ROS) production. Chemerin-9 (149–157) TFA has demonstrated neuroprotective effects, including the amelioration of Aβ₁₋₄₂-induced memory impairment in Alzheimer's disease models. Additionally, it plays important roles in modulating immune responses, regulating adipocyte differentiation, and improving glucose metabolism, making it a valuable tool for research in inflammation, neurodegeneration, and metabolic disorders.
  13. GRK5 inhibitor

    KR-39038 is a potent and orally bioavailable inhibitor of G protein-coupled receptor kinase 5 (GRK5), with an IC₅₀ of 0.02 μM. It effectively suppresses angiotensin II–induced cellular hypertrophy by inhibiting the HDAC5 signaling pathway in neonatal cardiomyocytes. KR-39038 exhibits strong anti-hypertrophic activity and improves cardiac function in preclinical models, making it a promising candidate for research in heart failure and related cardiovascular diseases.
  14. Oleuropein Aglycone (3,4-DHPEA-EA) is a bioactive polyphenol and the aglycone form of oleuropein, generated through enzymatic, acidic, or acetylated hydrolysis. It exhibits a broad range of pharmacological effects. In a TgCRND8 transgenic mouse model of Alzheimer’s disease, dietary supplementation (50 mg/kg) increases neuronal autophagic vesicles, reverses cognitive deficits, and reduces histone deacetylase 2 (HDAC2) levels in the cortex and hippocampus. In a high-fat diet-induced obesity rat model, Oleuropein Aglycone elevates urinary norepinephrine, interscapular brown adipose tissue epinephrine, and UCP1 protein levels, while reducing plasma leptin levels and total abdominal fat mass. Additionally, in a carrageenan-induced pleurisy mouse model, it mitigates lung neutrophil infiltration, lipid peroxidation, and IL-1β production. These findings highlight its potential in neurodegenerative, metabolic, and inflammatory disease research.
  15. ErbB2 inhibitor

    AG-825 is a selective, ATP-competitive inhibitor of ErbB2 (HER2) tyrosine kinase, with an IC₅₀ of 0.35 μM. It exhibits both anticancer and anti-inflammatory activities and has been shown to significantly accelerate apoptosis in human neutrophils. AG-825 also increases β₁-adrenergic receptor (β₁AR) density, suggesting potential cardiomodulatory effects. Due to its multifaceted biological activity, AG-825 is a valuable compound for research in oncology, inflammation, and cardiovascular disease.
  16. FFAR3 agonist

    AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3, also known as GPR41), with an IC₅₀ of 117 nM. It demonstrates anti-inflammatory, antitumor, and antidiabetic activities. AR420626 improves neurogenic diarrhea by modulating neural pathways mediated by nicotinic acetylcholine receptors (nAChRs). In cancer models, it suppresses the growth of HepG2 xenografts and inhibits hepatoma cell proliferation through apoptosis induction. Additionally, AR420626 mitigates allergic asthma and eczema and enhances glucose uptake by activating FFAR3-mediated Ca²⁺ signaling, offering potential therapeutic benefits in metabolic disorders such as diabetes.
  17. GLP-2R agonist

    Glepaglutide (ZP1848) is a long-acting glucagon-like peptide-2 (GLP-2) analogue and a potent agonist of the GLP-2 receptor (GLP-2R). It enhances intestinal absorption, reduces faecal output, and alleviates small intestinal inflammation. Glepaglutide is a valuable agent for research in inflammatory bowel disease (IBD), including Crohn’s disease.
  18. PAF receptor antagonist

    ST-899 is a specific antagonist of the platelet-activating factor (PAF) receptor, demonstrating significant efficacy in reducing mortality in endotoxin (LPS)-induced shock models in mice. This compound effectively inhibits the elevation of serum tumor necrosis factor (TNF) levels triggered by LPS while showing no impact on interleukin-6 (IL-6) levels. By interrupting the positive feedback loop between PAF and TNF, ST-899 mitigates the inflammatory response. This reagent is valuable for research into inflammatory diseases, particularly septic shock.
  19. PDE Inhibitor

    Theophylline sodium acetate functions as a potent phosphodiesterase (PDE) inhibitor, specifically targeting PDE3 to promote the relaxation of airway smooth muscle. It also acts as an adenosine receptor antagonist and histone deacetylase (HDAC) activator, contributing to its anti-inflammatory properties by elevating IL-10 levels and inhibiting NF-κB translocation to the nucleus. Additionally, Theophylline sodium acetate is known to induce apoptosis, making it a valuable reagent for research on asthma and chronic obstructive pulmonary disease (COPD).
  20. CRTH2 Receptor Antagonist

    CT-133 is a selective and potent antagonist of the CRTH2 receptor, exhibiting a Ki value of 2.2 nM, while demonstrating minimal affinity for the DP1 receptor (Ki > 3800 nM). This compound effectively inhibits neutrophil migration induced by PGD2 and has been shown to significantly reduce lung inflammation and improve lung function in a mouse model of acute lung injury (ALI) triggered by cigarette smoke. Additionally, CT-133 suppresses the overexpression of pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6, and promotes the recovery of the anti-inflammatory cytokine IL-10. CT-133 is valuable for research on acute lung injury and inflammatory responses.
  21. Neurotransmitter

    Histamine dihydrochloride acts as an agonist for histamine receptors and functions as a vasodilator. This organic nitrogen compound plays a crucial role in local immune responses and regulates intestinal physiological functions while also serving as a neurotransmitter. Histamine dihydrochloride influences the p38 MAPK/Akt signaling pathway and demonstrates notable antitumor, antioxidant, and anti-inflammatory properties. It is valuable in research applications related to acute myeloid leukemia, malignant melanoma, and renal cell carcinoma.
  22. Neurotransmitter

    Histamine phosphate is an agonist of the histamine receptor and functions as a potent vasodilator. This organic nitrogen compound plays a crucial role in local immune responses, modulates intestinal physiological functions, and serves as a key neurotransmitter. Histamine phosphate influences the p38 MAPK/Akt signaling pathway and demonstrates notable antitumor, antioxidant, and anti-inflammatory activities. It is applicable in research related to acute myeloid leukemia, malignant melanoma, and renal cell carcinoma.
  23. Adrenergic Receptor Agonist

    Tizanidine hydrochloride is a selective α2-adrenoceptor agonist that serves as an effective skeletal muscle relaxant. It primarily promotes muscle relaxation by reducing the presynaptic release of excitatory amino acids, such as glutamate and aspartate, within spinal cord interneurons. In addition to its central effects, Tizanidine hydrochloride demonstrates potential anti-cancer properties by inhibiting lung cancer cell proliferation, migration, and invasion, while promoting apoptosis via the modulation of the AKT and Wnt3a/β-catenin signaling pathways. This compound is clinically relevant for the management of spasticity associated with conditions like multiple sclerosis, stroke, and spinal cord injury.
  24. Neurotransmitter

    Histamine is a biogenic amine that acts as an agonist for histamine receptors, playing a significant role as a neurotransmitter. It is involved in local immune responses and the regulation of various physiological functions, including vasodilation. Histamine influences the p38 MAPK/Akt signaling pathway and demonstrates notable antitumor, antioxidant, and anti-inflammatory properties. It is commonly utilized in research related to acute myeloid leukemia, malignant melanoma, and renal cell carcinoma.
  25. Adrenergic Receptor Agonist

    Tizanidine is a selective α2-adrenoceptor agonist that functions primarily as a skeletal muscle relaxant. It exerts muscle relaxation effects by inhibiting the release of excitatory amino acids, thereby modulating synaptic activity in the spinal cord. Additionally, Tizanidine demonstrates anti-cancer properties by inhibiting proliferation, migration, and invasion of lung cancer cells, as well as inducing apoptosis through the upregulation of Nischarin and suppression of the AKT and Wnt3a/β-catenin pathways. This compound is utilized clinically for the management of spasticity associated with conditions such as multiple sclerosis, stroke, and spinal cord injury.
  26. Stable Isotope

    Histamine-d4 is a deuterium-labeled derivative of histamine, functioning primarily as a stable isotope for metabolic and pharmacokinetic studies. This compound acts as an agonist at histamine receptors and serves as a notable vasodilator, playing a critical role in local immune responses, intestinal physiological regulation, and neurotransmission. Histamine influences several signaling pathways, including p38 MAPK and Akt, and exhibits diverse biological activities such as anti-inflammatory, antioxidant, and potential antitumor effects. Its applications in research extend to the study of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma, facilitating a deeper understanding of these conditions.
  27. 5-HT5A Receptor Antagonist

    SB-699551 free base is a selective antagonist of the 5-HT5A receptor, characterized by a pKi of 8.2 nM, which allows for effective brain penetration. It exhibits significant selectivity over various serotonin receptor subtypes, dopamine receptors, and the α1B adrenoceptor. This compound disrupts Gαi/o-coupled and PI3K/AKT/mTOR signaling pathways, influencing the phosphorylation of key proteins such as CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 in breast tumor cells. SB-699551 free base is valuable for research into anxiety, breast cancer, and Alzheimer's disease.
  28. Stable Isotope

    Histamine-13C5 is a stable isotope-labeled form of histamine, primarily functioning as an agonist for histamine receptors. This organic nitrogen compound plays a critical role in local immune responses, modulates intestinal physiological functions, and acts as a neurotransmitter. Histamine influences the p38 MAPK/Akt signaling pathway and demonstrates antitumor, antioxidant, and anti-inflammatory properties. Research applications of Histamine-13C5 include the investigation of conditions such as acute myeloid leukemia, malignant melanoma, and renal cell carcinoma, facilitating deeper insights into these diseases.
  29. Anti-CXCR4 Antibody

    LY-2624587 is a humanized IgG4 monoclonal antibody that antagonizes CXCR4. By blocking the interaction between SDF-1 and CXCR4, it inhibits SDF-1-induced GTP binding, significantly reducing cell migration and promoting apoptosis in human lymphoma and leukemia cells. Additionally, LY-2624587 impedes CXCR4 and SDF-1-mediated signaling pathways, including the activation of MAPK and AKT. This reagent is valuable for research applications involving human hematological malignancies, particularly acute myeloid leukemia (AML).
  30. CXCR4 Antagonist.

    BPRCX807 is a selective and potent antagonist of the CXC chemokine receptor type 4 (CXCR4). It effectively inhibits CXCL12-mediated phosphorylation of ERK and Akt, leading to significant suppression of primary tumor growth. This compound is applicable for research in hepatocellular carcinoma, providing insights into its therapeutic potential in cancer treatment.
  31. GLP-1R Agonist

    Pegloxenatide is a long-acting glucagon-like peptide-1 receptor (GLP-1R) agonist. It exhibits various biological activities, including the reduction of blood glucose and lipids, weight management, anti-inflammatory effects, and promotion of wound healing, as well as providing protective effects on liver and heart tissues. Pegloxenatide is primarily utilized in research focused on type 2 diabetes and its associated complications.
  32. S1PR Regulator

    Mocravimod is a sphingosine-1-phosphate receptor (S1PR) modulator that inhibits the signaling necessary for T cell egress from lymph nodes and other lymphoid tissues. It preferentially binds to S1PR1, exhibiting beneficial effects such as a reduction in reactive oxygen species (ROS) levels, prevention of mitochondrial permeability transition pore opening, and enhancement of mitochondrial membrane potential (MMP). Additionally, Mocravimod promotes the phosphorylation of key signaling proteins including AKT, ERK, GSK-3β, JAK2, and STAT3, while preserving T cell effector function. This reagent is suitable for research into acute myelogenous leukemia, diabetes, and myocardial ischemia-reperfusion injury.
  33. CXCR4 Inhibitor

    Hit 14 is a selective inhibitor of C-X-C chemokine receptor type 4 (CXCR4), demonstrating an IC50 value of 254 nM. This compound effectively inhibits the migration and invasion of MDA-MB-231 cells, highlighting its potential in cancer research. Furthermore, Hit 14 modulates Akt phosphorylation and exhibits anti-inflammatory properties, demonstrating efficacy in reducing ear swelling and damage in mouse models. Its diverse biological activities make it a valuable tool for studies related to cancer metastasis and inflammation.
  34. α/β-Adrenergic Agonist

    Etilefrine is an α/β-adrenergic agonist primarily targeting α1 and β1 receptors. Its activity induces vasoconstriction by stimulating α1 receptors, leading to increased peripheral resistance, while β1 receptor activation enhances myocardial contractility and elevates heart rate, resulting in improved blood pressure and cardiac output. Additionally, Etilefrine modulates the AMPK/Akt signaling pathway, influencing phosphorylation levels. This compound is applicable in cardiovascular research, notably in studies related to postural hypotension, chylothorax, and conditions characterized by low cardiac output.
  35. Anticancer Agent

    Auriculasin is an anticancer agent that primarily targets VEGFR2, PI3K/AKT/mTOR, and MAPK signaling pathways. It effectively inhibits cell proliferation, induces apoptosis, and suppresses angiogenesis, while also promoting mitochondrial oxidative stress and ferroptosis. Additionally, Auriculasin demonstrates activity at the cannabinoid receptor CB1 with an IC50 of 8.92 μM. This compound is valuable for cancer research, particularly in studying prostate cancer, non-small cell lung cancer, and the development of anti-angiogenic therapies.
  36. Indole Alkaloid

    Tetrahydroalstonine is an indole alkaloid that acts as a selective antagonist of the α₂-adrenergic receptor. This compound demonstrates neuroprotective effects and has been shown to modulate autophagy-lysosomal function through the activation of the Akt/mTOR signaling pathway. Additionally, Tetrahydroalstonine significantly mitigates injury to primary cortical neurons induced by oxygen-glucose deprivation/reperfusion, making it a valuable tool for research into neuroprotection and cellular stress responses.
  37. α/β-Adrenergic Agonist

    Etilefrine hydrochloride is an α/β-adrenergic agonist that selectively activates α1 and β1 adrenergic receptors. By stimulating α1 receptors, it induces vascular smooth muscle contraction, thereby increasing peripheral resistance and blood pressure. Additionally, activation of β1 receptors enhances myocardial contractility and heart rate, improving cardiac output. Etilefrine hydrochloride is valuable for cardiovascular research, particularly in studies related to postural hypotension, chylothorax, and the management of low cardiac output conditions.
  38. Bombesin Receptor Antagonist

    Kuwanon G is a flavonoid compound that acts as an antagonist of the bombesin receptor. It demonstrates significant biological activities, including bactericidal, anti-tumor, anti-inflammatory, antioxidant, anti-atherosclerotic, and neuroprotective effects. Kuwanon G exhibits potent antibacterial activity against oral pathogens, particularly cariogenic and periodontal bacteria. Additionally, it induces apoptosis while inhibiting the proliferation, migration, and invasion of tumor cells, making it valuable for research in gastric cancer and atherosclerosis.
  39. Amino Acid Polypeptide Hormone Analogue

    Sincalide ammonium is an amino acid polypeptide hormone analogue of cholecystokinin (CCK) that primarily targets gallbladder function. It is utilized in clinical settings for its ability to promote gallbladder contraction, thus facilitating the diagnosis of gallbladder and pancreatic disorders. By increasing bile secretion and causing the contraction of the gallbladder while relaxing the sphincter of Oddi, Sincalide ammonium aids in the efficient drainage of bile into the duodenum, making it a valuable tool in postevacuation cholecystography.
  40. Angiotensin Receptor Inhibitor

    YS-49 monohydrate is a selective angiotensin receptor inhibitor, primarily targeting the angiotensin II pathway. This compound effectively reduces angiotensin II-stimulated proliferation of vascular smooth muscle cells by inducing heme oxygenase-1, offering potential therapeutic insights for cardiovascular research. Additionally, as an isoquinoline alkaloid, YS-49 demonstrates significant positive inotropic effects through the activation of cardiac β-adrenoceptors, making it a valuable reagent for studies involving cardiac function and vascular biology.
  41. CB1/P-gp Inhibitor

    Voacamine is an indole alkaloid that acts as an antagonist of the cannabinoid receptor 1 (CB1) and also functions as a P-glycoprotein (P-gp) inhibitor. This compound enhances the efficacy of Doxorubicin by modulating P-gp activity, promoting apoptosis-independent autophagic cell death in human osteosarcoma cells. Additionally, Voacamine activates mitochondrial-associated apoptosis signaling pathways while inhibiting the PI3K/Akt/mTOR pathway, thus suppressing breast cancer progression. Moreover, it demonstrates oncogenic activity against colorectal cancer by inhibiting epidermal growth factor receptor (EGFR).
  42. S1P1 Agonist

    SEW2871 is a potent and highly selective agonist of the sphingosine-1-phosphate type 1 receptor (S1P1), exhibiting an EC50 of 13.8 nM. This compound activates critical signaling pathways, including ERK, Akt, and Rac, and facilitates S1P1 internalization and recycling. SEW2871 effectively reduces lymphocyte populations in the bloodstream and shows promise for the study of various conditions, such as diabetes, Alzheimer’s disease, liver fibrosis, and inflammatory responses.
  43. 5-HT5A Antagonist

    SB-699551 is a selective 5-HT5A receptor antagonist with a pKi of 8.2 nM, demonstrating significant brain penetrance. This compound exhibits high selectivity over various 5-HT receptor subtypes, dopamine receptors, and α1B adrenoceptors. By disrupting Gαi/o-coupled signaling and the PI3K/AKT/mTOR pathways, SB-699551 influences phosphorylation of key proteins such as CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 in breast tumor cells. It serves as a valuable tool in the study of anxiety, breast cancer, and Alzheimer's disease.
  44. Artificial Insulin

    Insulin Detemir is an artificial insulin that regulates blood glucose levels by mimicking the effects of natural insulin. It activates the secretion of GLP-1 through enhanced expression of Gcg, utilizing signaling pathways involving Akt and extracellular signal-regulated kinase (ERK) alongside CREB. This reagent is primarily used in research related to type 2 diabetes, facilitating studies on glucose metabolism and insulin sensitivity.
  45. Dopamine β-hydroxylase Inhibitor

    Fusaric acid is a potent dopamine β-hydroxylase inhibitor that reduces endogenous levels of norepinephrine and epinephrine in various tissues, including the brain, heart, spleen, and adrenal glands. By inducing oxidative stress and apoptosis, fusaric acid disrupts mitochondrial integrity and activates key apoptosis-related proteases such as Caspase-3/7, -8, and -9. Additionally, fusaric acid regulates pivotal apoptotic proteins, inhibits fibrosis-related signaling pathways including NF-κB and TGF-β1/SMADs, and mitigates collagen deposition. Its applications extend to myocardial fibrosis and cardiac hypertrophy research, as well as studies on esophageal and liver cancers.
  46. Stable Isotope

    Theophylline-d3 is a deuterated form of theophylline, primarily used as a stable isotope in research applications. Theophylline functions as a potent phosphodiesterase inhibitor and adenosine receptor antagonist, contributing to its ability to relax airway smooth muscle. Additionally, it demonstrates anti-inflammatory effects by enhancing IL-10 production and inhibiting NF-κB nuclear translocation. This compound is valuable for studying asthma and chronic obstructive pulmonary disease (COPD) mechanisms and therapies.
  47. CB2 Agonists

    MN-25 is an orally active indolpyridone that functions as a selective CB2 agonist, exhibiting a Ki of 245 nM for CB1 and a potent 11 nM for CB2. This compound demonstrates significant anti-inflammatory properties by inhibiting TNF-R release in human peripheral blood mononuclear cells in vitro, with an IC50 of 33 μM. In vivo studies have shown that MN-25 is effective in reducing acute inflammation in a mouse model at oral doses up to 50 mg/kg, making it a valuable reagent for exploring cannabinoid receptor biology and therapeutic applications in inflammation.
  48. Stable Isotope

    Theophylline-13C2,d6 is a stable isotope-labeled form of Theophylline (1,3-Dimethylxanthine), primarily acting as a phosphodiesterase (PDE) inhibitor and adenosine receptor antagonist. This reagent enhances anti-inflammatory responses by increasing IL-10 levels and inhibiting NF-κB nuclear translocation, while also promoting apoptosis. It serves as a valuable tool for research into airway smooth muscle relaxation and the treatment of respiratory conditions such as asthma and chronic obstructive pulmonary disease (COPD).
  49. α-Adrenergic Receptor Agonist

    Naphazoline is a potent α-adrenergic receptor agonist that exerts its biological activity through vasoconstriction and the reduction of vascular hyperpermeability. It effectively diminishes the levels of inflammatory mediators, including TNF-α, IL-1β, IL-6, IFN-γ, IL-4, as well as IgE, GMCSF, and NGF. Naphazoline is widely utilized in research related to non-bacterial conjunctivitis and other conditions involving inflammation and vascular function.
  50. IBAT Inhibitor

    (S)-Elobixibat is a selective inhibitor of the intestinal bile acid transporter (IBAT). It effectively lowers LDL cholesterol levels, enhances serum levels of GLP-1, and promotes colonic motility, making it a valuable tool in metabolic syndrome research. This compound is utilized in studies related to constipation, dyslipidemia, non-alcoholic fatty liver disease, and liver tumors.

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