Catalog No.
Product Name
Application
Product Information
Citations
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CRFR1 antagonist
NBI-27914 is a potent and selective antagonist of corticotropin-releasing factor receptor 1 (CRFR1), a member of the G protein-coupled receptor (GPCR) superfamily. By selectively blocking CRFR1, NBI-27914 is useful for studying stress-related pathways and disorders mediated by CRF signaling, such as anxiety and depression. -
CRF2 receptor agonist
Urocortin, human, is a 40-amino acid neuropeptide that functions as a selective agonist of the endogenous corticotropin-releasing factor receptor 2 (CRF₂). It exhibits high binding affinity with Kᵢ values of 0.4 nM for human CRF₁, 0.3 nM for rat CRF₂α, and 0.5 nM for mouse CRF₂β. Urocortin plays a role in modulating stress responses, cardiovascular function, and feeding behavior. -
CRF1 antagonist
JNJ19567470 (R317573) is a selective, non-peptidergic corticotropin-releasing factor type 1 (CRF₁) receptor antagonist. It effectively blocks sodium lactate (NaLac)-induced panic-like behavior and associated cardiovascular responses. JNJ19567470 also reduces regional glucose utilization in the amygdala and attenuates anxiety-related responses -
CRHR1 antagonist
Antalarmin is a selective, nonpeptide antagonist of corticotropin-releasing factor receptor 1 (CRHR1), with a Ki of 2.7 nM. It is capable of crossing the blood–brain barrier, making it a valuable compound for investigating CRHR1-mediated central nervous system functions and stress-related disorders. -
CRF2 receptor antagonist
α-Helical CRF(9-41) is a competitive antagonist of the corticotropin-releasing factor receptor 2 (CRF₂) with a K\_B of approximately 100 nM. It also acts as a partial agonist at the CRF₁ receptor, with an EC₅₀ of 140 nM. This dual activity makes it a useful tool for studying CRF receptor signaling and stress-related physiological responses. -
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. -
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. -
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. -
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). -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. - 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.
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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. -
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. -
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. -
LPA Receptor Activator
1-Oleoyl lysophosphatidic acid sodium is a potent LPA receptor activator, functioning primarily as a bioactive phospholipid. This compound promotes mitosis by inducing DNA synthesis, making it critical for studies in cell proliferation. Additionally, 1-Oleoyl lysophosphatidic acid sodium plays a role in mediating both normal and pathological emotional responses, including anxiety and depression, contributing to research in neurobiology and mental health disorders. -
Orexin Receptor Agonist
RTIOXA-43 is an orexin receptor agonist that exhibits potent activity with EC50 values of 24 nM for both OX1 and OX2 receptors. This compound is valuable for research applications related to sleep regulation, appetite control, and energy metabolism. By activating orexin receptors, RTIOXA-43 facilitates investigations into neurodegenerative diseases and sleep disorders. -
GPR18 Agonist
N-Arachidonylglycine (NA-Gly) selectively acts as an agonist for the GPR18 receptor, exhibiting an EC50 value of 44.5 nM. Unlike its structural analog anandamide, NA-Gly does not engage with CB1 or CB2 receptors. This compound also demonstrates inhibitory activity on GLYT2 with an IC50 of 5.1 μM. Additionally, N-Arachidonylglycine has been shown to effectively promote the migration of endometrial cells, making it a valuable tool for research in cellular migration and cannabinoid receptor activity. -
Adrenergic Receptor Antagonist
Propranolol hydrochloride is a nonselective β-adrenergic receptor antagonist that effectively crosses the blood-brain barrier. It exhibits high affinity for both β1AR and β2AR receptors, with Ki values of 1.8 nM and 0.8 nM, respectively, and inhibits [3H]-DHA binding in rat brain membranes with an IC50 of 12 nM. This reagent is widely used in research related to hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy. -
Antihypertensive Agent
Indoramin is an orally active antihypertensive agent targeting the α1A-adrenoceptor. This compound works by selectively blocking α1-adrenoceptors, leading to vasodilation and a reduction in blood pressure. Indoramin is utilized in cardiovascular research to study blood pressure regulation and the mechanisms of hypertension. -
Serotonergic Receptor Antagonist
Hymenidin is a natural antagonist of serotonergic receptors, exhibiting significant inhibitory effects on voltage-gated potassium channels. This compound demonstrates the ability to induce apoptosis in cancer cells, making it a valuable tool for research in cancer biology and therapeutics targeting serotonergic signaling pathways. Its dual action on ion channels and receptor antagonism positions Hymenidin as a noteworthy reagent for exploring complex cellular mechanisms in neurobiology and oncology. -
Prostaglandin E2 Inhibitor
Thielavin B is an inhibitor of prostaglandin biosynthesis, specifically targeting the synthesis of prostaglandin E2 from endoperoxide precursors. This compound demonstrates significant anti-inflammatory activity, as evidenced by its efficacy in reducing carrageenan-induced edema in rat models following intravenous administration. Thielavin B is valuable for research focused on inflammation and pain pathways. -
Endogenous Glucocorticoids
Corticosterone (17-Deoxycortisol) is an orally active and adrenal cortex-produced glucocorticoid, which plays an important role in regulating neuronal functions of the limbic system (including hippocampus, prefrontal cortex, and amygdala). Corticosterone increases the Rab-mediated AMPAR membrane traffic via SGK-induced phosphorylation of GDI. Corticosterone also interferes with the maturation of dendritic cells and shows a good immunosuppressive effect. -
PDE Inhibitor
Theophylline, a potent phosphodiesterase (PDE) inhibitor, primarily targets PDE3, leading to relaxation of airway smooth muscle and enhanced bronchodilation. This compound also functions as an adenosine receptor antagonist and exhibits anti-inflammatory properties by elevating IL-10 levels and inhibiting NF-κB translocation into the nucleus. Additionally, Theophylline has been shown to induce apoptosis in certain cell types. Its applications are particularly relevant in the research of asthma and chronic obstructive pulmonary disease (COPD). -
β2-Adrenergic Receptor Agonist
Levalbuterol hydrochloride is a potent β2-adrenergic receptor agonist and the active (R)-enantiomer of Salbutamol. It exhibits enhanced bronchodilator activity, making it a valuable reagent in respiratory research. Primarily, it is utilized in studies focusing on the treatment of chronic obstructive pulmonary disease (COPD) and other airway obstruction disorders. -
L-glutamate Uptake Inhibitor
Evans Blue is a potent inhibitor of L-glutamate uptake through the membrane-bound excitatory amino acid transporter (EAAT). This compound effectively inhibits L-glutamate and kainate receptor-mediated currents, making it valuable for research into neurophysiological processes. Additionally, due to its strong affinity for serum albumin, Evans Blue serves as a high molecular weight protein tracer and is widely used to investigate blood-brain barrier (BBB) permeability. -
Endothelin Receptor Inhibitor
Carperitide is a synthetic analogue of Atrial Natriuretic Peptide (ANP) that acts as an endothelin receptor inhibitor. This 28-amino acid peptide significantly reduces endothelin-1 secretion in a dose-dependent manner, thereby promoting vasodilation and natriuresis. It is primarily used in research applications related to cardiovascular physiology, providing insights into heart failure mechanisms and the regulation of blood pressure. -
Histamine H1 Receptor Antagonist
Epinastine is a selective histamine H1 receptor antagonist, known for its effectiveness as a mast cell stabilizer. It exhibits high affinity for neuronal octopamine receptors in various insects, demonstrating potential roles in modulating immune responses. Epinastine also inhibits pro-inflammatory cytokines such as TARC, IL-8, and IL-4, making it valuable for research into allergic diseases and anti-cancer immunity mechanisms. Its ability to reduce scratching behavior and vascular permeability further underscores its relevance in studying allergic and inflammatory conditions. -
Histamine H1 Receptor Antagonist
Mebhydrolin is a selective antagonist of the histamine H1 receptor, primarily known for its role in mediating allergic responses. This compound exhibits significant antihistaminic activity, making it valuable for research in allergy and immunology. Its effectiveness in blocking histamine-induced physiological effects allows for the exploration of H1 receptor pathways and the development of related therapeutic strategies. -
NPRs Agonist
Nesiritide, a recombinant form of human B-type natriuretic peptide, primarily functions as an agonist of natriuretic peptide receptors (NPRs), specifically NPR-A and NPR-C, with affinity constants of 7.3 pM and 13 pM, respectively. It effectively regulates the activation and inactivation of L-type calcium channels, resulting in significant vasodilatory, diuretic, and natriuretic effects. Nesiritide is utilized in research on cardiovascular diseases, particularly in models of heart failure and vascular remodeling following arterial injury. -
MC4R Agonist
Tetracosactide is a potent agonist of the melanocortin-4 receptor (MC4R), activating human MC4R with an EC50 of 0.65 nM. This synthetic analogue of adrenocorticotrophic hormone (ACTH) is known to stimulate the release of corticosteroids, including cortisol, from the adrenal gland. Tetracosactide is utilized in research investigating conditions such as ulcerative colitis, Crohn's disease, and various forms of arthritis, including juvenile and adult rheumatoid arthritis and osteoarthrosis. -
α-adrenergic Receptor Agonist
Naphazoline (Naphthazoline) hydrochloride is a potent α-adrenergic receptor agonist. Naphazoline hydrochloride reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline hydrochloride reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF. Naphazoline hydrochloride can be used for non-bacterial conjunctivitis research. -
β1-Adrenergic Blocker
Esmolol hydrochloride is an ultra-short-acting cardioselective β1-adrenergic blocker, primarily targeting the β1-adrenergic receptors. This compound demonstrates significant antiarrhythmic properties and is effective in mitigating post-resuscitation myocardial dysfunction. Additionally, esmolol hydrochloride inhibits aldose reductase activity, reducing advanced glycation end products and enhancing fibroblast migration, which contributes to improved diabetic wound healing. It serves as a valuable tool for research into cardiac diseases, including arrhythmias and diabetic foot ulcers. -
5-HT2BR Antagonist
PRX-08066 maleate is a selective antagonist of the 5-hydroxytryptamine receptor 2B (5-HT2BR) with a Ki value of 3.4 nM. It effectively inhibits the MAPK signaling pathway, as well as the release of serotonin and the expression of key fibrotic factors such as TGFβ1, CTGF, and FGF2. PRX-08066 maleate demonstrates the ability to inhibit the proliferation of KRJ-I cells and induce apoptosis via caspase-3 activation. This compound shows potential for research in the context of pulmonary arterial hypertension (PAH) and neuroendocrine tumors (NET). -
β2-adrenergic receptor Antagonist
Zenidolol is a selective β2-adrenergic receptor antagonist, exhibiting a Ki value of 0.7 nM for the β2 receptor, alongside higher Ki values for β1 and β3 receptors at 49.5 nM and 611 nM, respectively. This compound demonstrates significant antitumor activity by inducing apoptosis, inhibiting tumor sphere formation, and downregulating the HIF pathway in tumor cells. Additionally, Zenidolol has a unique vasodilatory effect specific to pulmonary vessels in mouse models and can serve as an intraocular pressure-lowering agent in ophthalmic research applications. -
Stable Isotope
Terfenadine-d3 is the deuterated form of Terfenadine, which primarily targets the hERG potassium channel as a potent open-channel blocker with an IC50 of 204 nM. As an H1 histamine receptor antagonist, Terfenadine-d3 demonstrates significant biological activity by inducing apoptosis in melanoma cells through the modulation of calcium homeostasis. Its mechanism includes the generation of reactive oxygen species (ROS) and the subsequent activation of caspases -4, -2, and -9, making it valuable for research in cancer biology and apoptosis pathways. -
CXCR4 Antagonist
Nef-M1 is a CXCR4 antagonist peptide derived from the myristoylated protein encoded by the nef gene in HIV. It induces apoptosis by enhancing caspase-3 levels in cancer cells and inhibits critical processes associated with tumor progression, including angiogenesis and epithelial-mesenchymal transition (EMT). Nef-M1 reduces levels of VEGF-A, phosphorylated GSK-3β, and vimentin while promoting E-cadherin expression. This compound is valuable for research applications focused on colorectal cancer and breast cancer. -
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. -
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). -
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. -
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. -
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.
