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Catalog No.
Product Name
Application
Product Information
Citations
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G protein-coupled receptor kinase Inhibitor
CCG 224061 is a selective inhibitor of G protein-coupled receptor kinase 2 (GRK2) with an IC50 of 0.066 μM. It effectively inhibits GRK activity in cardiomyocytes, making it a valuable tool for studying cardiac signaling pathways. This compound is particularly relevant for research focused on heart disease, heart failure, myocardial hypertrophy, and hypertension. -
GRK5 Inhibitor
CCG273441 is a selective covalent inhibitor of G protein-coupled receptor kinase 5 (GRK5), exhibiting an IC50 value of 3.8 nM. This compound demonstrates a high degree of selectivity over GRK2, with an IC50 of 4.8 μM, by targeting and covalently binding to the Cys474 residue, which is unique to the GRK5 subfamily. CCG273441 serves as a valuable tool for research into GRK5-related signaling pathways and potential therapeutic applications in various disease models. -
GRK2 Inhibitor
CCG258747 is a potent and selective inhibitor of GRK2, demonstrating an IC50 value of 18 nM and high selectivity against GRK1, GRK5, PKA, and ROCK1. This compound effectively prevents the internalization of the µ-opioid receptor (MOR) and inhibits the IgE-mediated anaphylaxis via the GRK2 and FcεRI signaling pathway, while also activating mast cells through MRGPRX2 and MRGPRB2. CCG258747 serves as a valuable tool for investigating disease mechanisms associated with GRK2 overexpression, including heart failure and opioid tolerance. -
GRK Inhibitor
GRK-IN-1 is a selective inhibitor of G protein-coupled receptor kinases (GRKs), which play a crucial role in the regulation of receptor desensitization and downregulation. This compound exhibits potential biological activity in modulating signaling pathways mediated by GPCRs, making it valuable for research focused on cardiovascular diseases, neurological disorders, and cancer. GRK-IN-1 can be utilized to investigate the impact of GRK inhibition on cellular signaling and to explore therapeutic strategies targeting GRK-related pathways. -
GRK6 Inhibitor
GRK6-IN-3 is a selective inhibitor of G protein-coupled receptor kinase 6 (GRK6), exhibiting an IC50 value of 1.03 μM. This compound modulates GRK6 activity, which is crucial for various cellular signaling pathways. GRK6-IN-3 is suitable for research applications aimed at exploring GRK6's role in receptor desensitization and its implications in various physiological and pathological processes. -
GRK5 Inhibitor
CCG-271423 is a selective inhibitor of G protein-coupled receptor kinase 5 (GRK5), demonstrating an IC50 of 2.1 nM for GRK5 and 44 μM for GRK2. This compound effectively reduces cardiomyocyte contractility and lowers calcium transient levels, making it valuable for cardiac research. Additionally, CCG-271423 features an alkyne group, enabling its use in copper-catalyzed azide-alkyne cycloaddition (CuAAc) for bioconjugation applications. -
GRK5 Inhibitor
GRK5-IN-4 is a selective covalent inhibitor of G protein-coupled receptor kinase 5 (GRK5), exhibiting an IC50 of 1.1 μM and demonstrating 90-fold selectivity over GRK2. This compound serves as a valuable tool for heart failure research by modulating GRK5 activity. Additionally, GRK5-IN-4 features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, making it useful for various chemical biology applications. -
GRK6 Inhibitor
GRK6-IN-4 is a selective inhibitor of G protein-coupled receptor kinase 6 (GRK6), exhibiting an IC50 of 1.56 μM. This compound plays a crucial role in the modulation of G protein-coupled receptor signaling pathways and is relevant for research investigating hematological malignancies, inflammatory diseases, and autoimmune disorders. By inhibiting GRK6, GRK6-IN-4 provides valuable insights into the underlying mechanisms of these conditions and potential therapeutic strategies. -
GRK Inhibitor
CCG 258001 is a selective inhibitor of G protein-coupled receptor kinases (GRK), demonstrating IC50 values of 0.29 µM for GRK2, 51.8 µM for GRK1, and 33 µM for GRK5. It effectively inhibits GRK activity in cardiomyocytes and other muscle cell types, making it a valuable tool for investigating the role of GRKs in cardiac function. This compound is relevant for research into various cardiovascular conditions, including heart failure, myocardial hypertrophy, and hypertension. -
GRK Inhibitor
GRL093-22 is a potent and selective inhibitor of G protein-coupled receptor kinases (GRKs), displaying IC50 values of 60 nM for GRK5 and 40 nM for GRK6. This compound is valuable for research on mechanisms underlying heart failure and multiple myeloma, facilitating investigations into the modulation of GRK activity in these conditions. -
GRK5 Inhibitor
CCG-273463 is a selective covalent inhibitor of G protein-coupled receptor kinase 5 (GRK5), demonstrating an IC50 of 8.6 nM. This compound is instrumental in research related to heart failure, hypertrophic cardiomyopathy, and various cancer pathways. Its specificity for GRK5 makes it a valuable tool for elucidating the role of this kinase in disease mechanisms and therapeutic development. -
GRK2 Inhibitor
CCG-224406 is a selective inhibitor of G protein-coupled receptor kinase 2 (GRK2), exhibiting an IC50 of 13 nM and demonstrating over 700-fold selectivity against other GRK subfamilies, with no inhibition of ROCK1. This small molecule is suitable for research into GRK2's role in heart failure and offers a valuable tool for exploring GRK-related signaling pathways in cardiovascular biology. -
GRK5 Inhibitor
GRK5-IN-3 is a covalent inhibitor targeting G Protein-Coupled Receptor Kinase 5 (GRK5). This compound demonstrates potent inhibitory activity against GRK5 and GRK6, with IC50 values of 0.22 μM and 0.41 μM, respectively. GRK5-IN-3 is suitable for research applications focused on understanding the role of GRK5 in cellular signaling and its implications in various pathological conditions. -
GRK6 Inhibitor
GRK6-IN-5 is a selective inhibitor of G protein-coupled receptor kinase 6 (GRK6), exhibiting an IC50 of 4.48 μM. This compound is instrumental for investigating its role in hematological malignancies, inflammation-related conditions, and autoimmune disorders. Researchers can utilize GRK6-IN-5 to elucidate the biochemical pathways influenced by GRK6, potentially leading to therapeutic advancements in these diseases. -
GRK5 Inhibitor
GRK5-IN-5 is a selective inhibitor of G protein-coupled receptor kinase 5 (GRK5), demonstrating an IC50 of 0.03 μM. This compound also exhibits activity against GRK2 and GRK6, with IC50 values of 2.2 μM and 0.036 μM, respectively. GRK5-IN-5 is known for its potent activity in inhibiting myocardial hypertrophy and reducing non-myocardial cell proliferation. It effectively suppresses the upregulation of hypertrophy markers Nppa and Nppb, thereby preventing pathological remodeling of cardiac tissue. This reagent is valuable for investigating mechanisms underlying cardiac hypertrophy. -
ASM Inhibitor
KARI 201 hydrochloride is a selective inhibitor of acid sphingomyelinase (ASM) with a competitive mechanism of action, exhibiting an IC50 of 338.3 nM. This compound is capable of penetrating the blood-brain barrier and has demonstrated potential in improving neuropathological features associated with Alzheimer's disease. KARI 201 hydrochloride serves as a valuable tool for research applications focused on neurodegenerative disorders and the modulation of sphingolipid metabolism. -
ASM Inhibitor
KARI 201 is a selective, brain-penetrant competitive inhibitor of acid sphingomyelinase (ASM), exhibiting an IC50 of 338.3 nM. This compound acts as a ghrelin receptor agonist and demonstrates significant potential in ameliorating neuropathological features associated with Alzheimer's disease. KARI 201 is valuable for research investigating the modulation of ASM activity and its implications in neurodegenerative disorders. -
GLP-1R Inhibitor
GLP-1 receptor agonist 13 is a selective agonist targeting the glucagon-like peptide-1 receptor (GLP-1R), exhibiting an EC50 of 76 nM. This compound plays a significant role in enhancing glucose-dependent insulin secretion, thereby influencing metabolic processes. It is particularly useful in research applications focused on diabetes, obesity, and related metabolic disorders. -
GLP Inhibitor
MS012 is a selective glucagon-like peptide (GLP) inhibitor with an IC50 value of 7 nM. This compound serves as a valuable tool in the investigation of GLP dysregulation associated with various conditions, including cancer, inflammatory diseases, and neuroregenerative disorders. Its application in research may facilitate the understanding of GLP's role in these pathophysiological processes. -
Adenosine A2A Receptor Inhibitor
4-Desmethyl Istradefylline is a selective adenosine A2A receptor antagonist, serving as a significant metabolite of Istradefylline. With a Ki of 2.2 nM, it demonstrates potent inhibition of the A2A receptor, making it relevant for exploring therapeutic strategies in Parkinson's disease and related neurological disorders. Its oral bioactivity allows for convenience in in vivo research applications targeting adenosine signaling pathways. -
Platelet Aggregation Inhibitor
U-51605 is a platelet aggregation inhibitor that targets thromboxane synthesis. It also functions as a prostaglandin I2 synthase inhibitor and has been shown to block retinal vasodilation responses induced by nitric oxide donors like NOR3. This reagent is valuable for research applications focusing on cardiovascular health and vascular biology. -
TRP Channel Inhibitor
Cannabidiorcol (CBDO) is an inhibitor of transient receptor potential (TRP) channels. This compound, structurally related to cannabidiol with a shortened pentyl side chain, exhibits anti-inflammatory properties while displaying low affinity for cannabinoid receptors. Research applications include investigations into its potential role in modulating inflammation and exploring its effects on tumorigenesis at elevated concentrations. -
ACU Inhibitor/VR1 Agonist
OMDM-5 is a selective anandamide cellular uptake (ACU) inhibitor, exhibiting a Ki of 4.8 μM. In addition, OMDM-5 demonstrates potent activity as a vanilloid receptor type 1 (VR1, TRPV1) agonist, with an EC50 of 75 nM. This compound also shows weak activity as a cannabinoid receptor type 1 (CB1) ligand, with a Ki of 4.9 μM. Its properties make OMDM-5 useful for studies involving pain modulation and endocannabinoid signaling pathways. -
RGS Protein Inhibitor
CCG 203769 is a selective inhibitor of the regulator of G protein signaling (RGS4), effectively disrupting the RGS4-Gαo protein-protein interaction with an IC50 of 17 nM. This compound is instrumental for research applications focused on G protein-coupled signaling pathways and the modulation of G protein activity. CCG 203769 may be utilized in studies exploring the role of RGS proteins in various physiological processes and disease states. -
RGS14 Inhibitor
Z55660043 is a selective inhibitor of Regulator of G protein Signaling-14 (RGS14) with an IC50 of 2.3 μM. This compound acts by non-covalently inhibiting the GTPase-accelerating protein (GAP) activity of RGS14, demonstrating a favorable safety profile without significant cytotoxic effects. Z55660043 is suitable for research focused on central nervous system and metabolic disorders, contributing to the understanding of RGS14's role in these biological processes. -
RGS4 Inhibitor
CCG-2046 is a selective inhibitor of the regulator of G-protein signaling 4 (RGS4), demonstrating an IC50 value of 4.3 μM for inhibiting the RGS4-Gαo interaction. This compound modulates G-protein signaling pathways, making it a valuable tool for studying their role in various physiological processes. CCG-2046 is suitable for research applications focused on neurobiology, cardiac function, and potential therapeutic interventions for related disorders. -
RGS Protein Inhibitor
CCG-4986 is a selective RGS protein inhibitor that covalently modifies the Cys-132 residue of RGS4, thereby inhibiting its activity. This compound is valuable for studying the implications of altered G protein-coupled receptor (GPCR) signaling in various pathological conditions, including Parkinson's disease and opioid addiction. CCG-4986 is a useful tool for researchers investigating the role of RGS proteins in cellular signaling pathways. -
MMP Inhibitor
Sucrose octasulfate is a matrix metalloproteinase (MMP) inhibitor that modulates cellular activities by regulating the extracellular matrix. It promotes the release of somatostatin-like immunoreactivity from gastric D cells, facilitating ulcer healing through increased endogenous somatostatin levels. This compound has demonstrated efficacy in improving wound closure in diabetic foot ulcers and venous leg ulcers, making it pertinent for research in chronic wound healing and gastrointestinal disorders. Additionally, sucrose octasulfate serves as a valuable pharmaceutical excipient in various therapeutic applications. -
MMP Inhibitor
Sucrose octasulfate sodium is a potent matrix metalloproteinase (MMP) inhibitor that enhances the release of somatostatin-like immunoreactivity (SLI) from gastric D cells. This compound promotes ulcer healing by increasing endogenous gastric somatostatin levels. Sucrose octasulfate sodium is utilized in research related to chronic wound healing and has shown significant efficacy in improving wound closure in diabetic foot ulcers and venous leg ulcers. Additionally, it serves as a useful pharmaceutical excipient in various applications. -
Somatostatin Receptor Inhibitor
SRA880 free base is a somatostatin receptor inhibitor, specifically targeting the somatostatin-1 autoreceptor. This compound exhibits antidepressant-modulating effects and has been shown to enhance the efficacy of imipramine, resulting in antidepressant-like outcomes. Additionally, SRA880 influences brain-derived neurotrophic factor (BDNF) mRNA expression and modulates the phosphorylation of associated proteins, making it a valuable tool in neurobiological research focusing on mood disorders and related pathways. -
Somatostatin Receptor Inhibitor
Des-threoninol-octreotide is a potent somatostatin receptor inhibitor, primarily targeting the mSSTR2b, rSSTR5, and hSSTR5 receptor subtypes. This compound demonstrates high inhibitory activity with IC50 values of 13.62 nM, 10.63 nM, and 10.95 nM, respectively. It is valuable for research applications exploring neuroendocrine regulation, peptide hormone signaling, and potential therapeutic interventions involving somatostatin pathways. -
Platelet Aggregation Inhibitor
4-Trifluoromethylsalicylic acid, also known as Desacetyl triflusal, functions as a platelet aggregation inhibitor. This compound is instrumental in research related to cardiovascular disorders, particularly in the study of thrombus formation and prevention. Its ability to modulate platelet activity makes it a valuable tool for investigating hematological processes and developing antithrombotic therapies. -
Platelet Aggregation Inhibitor
Cloricromen is a potent platelet aggregation inhibitor that functions by targeting the mechanisms involved in thrombus formation. Demonstrating efficacy in inhibiting platelet aggregation in both human subjects and experimental models, Cloricromen is a valuable reagent for research in cardiovascular disease and thrombotic disorders. Its application in studying platelet function and related pathologies makes it an essential tool for investigations in vascular biology. -
Platelet Aggregation Inhibitor
Ataprost is a potent platelet aggregation inhibitor that functions as an orally active analogue of Carboprostacyclin. This compound demonstrates 2.6 times greater efficacy than Carboprostacyclin in inhibiting ADP-induced platelet aggregation in vitro. Additionally, Ataprost has been shown to alleviate coronary spasm, making it relevant for research in cardiovascular diseases and platelet function studies. -
Blood Platelet Aggregation Inhibitor
Ent-8-Iso-15(S)-prostaglandin F2α is a potent inhibitor of blood platelet aggregation. This compound exhibits superior activity compared to its isomer, 8-Isoprostaglandin F2α, in whole blood assays, making it a valuable tool for studying platelet function and related cardiovascular research. Its mechanism of action can aid in the exploration of therapeutic strategies for conditions associated with abnormal platelet aggregation. -
FAAH Inhibitor
3-Decyl-5,5'-diphenyl-2-thioxo-4-imidazolidinone is a potent inhibitor of fatty acid amide hydrolase (FAAH) with a pI50 of 5.89. This compound exhibits significant activity against endocannabinoids and lipid mediators, making it relevant for studies in pain management, inflammation, and cannabinoid signaling pathways. Its limited affinity for cannabinoid receptors CB(1) and CB(2) allows for targeted research into FAAH-related physiological processes without direct receptor modulation. -
NR4A1 Inhibitor
Glycerol kinase, microorganism functions as an NR4A1 inhibitor by directly binding to and inhibiting the transcription factor NR4A1, which plays a critical role in hepatic gluconeogenesis. This inhibition leads to reduced blood glucose levels and positively influences UCP1 expression through the β-adrenergic receptor-cAMP-CREB signaling pathway, promoting the browning of white adipose tissue and enhancing thermogenesis. Additionally, it modulates intracellular fatty acid composition and energy metabolism. Research using glycerol kinase in diabetic mouse models has demonstrated its ability to counteract NR4A1-induced hyperglycemia, indicating its potential applications in diabetes and obesity studies. -
Platelet Aggregation Inhibitor
Myrianthic acid is a pentacyclic triterpenoid that functions as a platelet aggregation inhibitor. Isolated from the root wood of Myrianthus arboreus and the leaves of Campsis grandiflora, it effectively inhibits adrenaline-induced platelet aggregation, demonstrating an IC50 of 46.2 μM. This compound is valuable for research applications focused on thrombosis and related cardiovascular disorders. -
IBAT Inhibitor
Elobixibat hydrate is an orally active inhibitor of the intestinal bile acid transporter (IBAT), demonstrating potent activity with IC50 values of 0.53 nM for human IBAT, 0.13 nM for mouse IBAT, and 5.8 nM for canine IBAT. This compound has been shown to effectively lower LDL cholesterol levels, enhance serum GLP-1 concentrations, and promote colonic motility. Elobixibat hydrate is valuable for research applications related to chronic idiopathic constipation (CIC), dyslipidemia, non-alcoholic fatty liver disease, and the study of liver tumors, particularly in elderly populations. -
MAGL Inhibitor
OMDM169 is a selective inhibitor of monoacylglycerol lipase (MAGL), effectively increasing the levels of 2-arachidonoylglycerol (2-AG) in biological systems. This compound demonstrates significant analgesic properties through the indirect activation of cannabinoid receptors. OMDM169 exhibits an effective concentration of 0.13 μM, making it a valuable tool for research focused on pain modulation and cannabinoid receptor signaling pathways. -
HIF Inhibitor
Arylsulfonamide 64B is a potent inhibitor of hypoxia-inducible factor (HIF). This compound effectively suppresses hypoxia/HIF-mediated expression of key oncogenes such as c-Met and CXCR4, thereby demonstrating significant anti-tumor activity. Arylsulfonamide 64B is particularly relevant for research focused on uveal melanoma, as it has been shown to reduce primary tumor growth and metastasis in mouse models. -
AVP Release Inhibitor/Kappa Opioid Receptor Agonist
Niravoline is an arginine vasopressin (AVP) release inhibitor and a selective kappa opioid receptor agonist. This compound is notable for inducing a pure water diuresis effect while minimizing electrolyte loss. Additionally, Niravoline has demonstrated efficacy in reducing brain edema following transient forebrain ischemia in rodent models, making it a valuable tool for research in neuroprotection and fluid balance mechanisms. -
Gβγ-subunit Inhibitor
M119 (NSC 119910) is a selective Gβγ-subunit inhibitor that modulates μ-opioid receptor signaling. This compound has been shown to enhance μ-opioid-dependent antinociception by inhibiting μ-receptor-dependent phospholipase (PLC) activation. M119 is useful in pain research, particularly in studies investigating opioid analgesia, as well as in the assessment of acute tolerance and dependence in animal models. -
Opioid Receptor Inhibitor
Neuropeptide AF (human) is an endogenous peptide that acts as an opioid receptor inhibitor. This neuropeptide plays a critical role in modulating pain and stress responses, making it a valuable tool for studies focused on opioid signaling pathways. Research applications include investigations into pain management, addiction, and the physiological effects of endogenous opioid peptides. -
ORL-1 Inhibitor
rel-SB-612111 hydrochloride is a selective antagonist of the human opiate receptor-like orphan receptor (ORL-1), exhibiting a high binding affinity with a Ki value of 0.33 nM. This compound demonstrates notable selectivity against μ-, κ-, and δ-opioid receptors, with Ki values of 57.6 nM, 160.5 nM, and 2109 nM, respectively. rel-SB-612111 hydrochloride has been shown to effectively inhibit the pronociceptive effects of Nociceptin in acute pain models, making it a valuable tool for research into pain mechanisms and opioid receptor interactions. -
μ-Opioid Receptor Agoinst/AChE Inhibitor
Eseroline is a potent μ-opioid receptor agonist and a selective, competitive inhibitor of acetylcholinesterase (AChE), with Ki values of 0.1 μM for AChE and 200 μM for butyrylcholinesterase (BuChE). This compound also acts as a nicotinic acetylcholine receptor allosteric enhancing ligand, enhancing acetylcholine signal transduction without directly activating the receptor. Eseroline's neurotoxic effects include cell membrane damage and energy metabolism disruption, making it a valuable tool for investigating Alzheimer's disease pathology and cholinergic signaling. -
MOR Inhibitor
MOR agonist-1 is a selective μ-opioid receptor (MOR) agonist known for its pronounced analgesic activity. This compound is valuable for research focused on pain modulation and the exploration of pain-related disorders. Its mechanism of action makes it an essential tool for studies investigating opioid pharmacology and therapeutic interventions in pain management. -
OX1R Inhibitor
Tebideutorexant is a selective inhibitor of the orexin receptor 1 (OX1R), demonstrating significant oral bioavailability and the ability to cross the blood-brain barrier. With a human OX1R pKi of 8.17 and a rat OX1R pKi of 8.13, this compound specifically targets OX1R while exerting minimal effects on OX2R. Tebideutorexant is a valuable tool for investigating panic and anxiety disorders in preclinical research settings. -
Melanogenesis Inhibitor
Ethyl linolenate is a fatty acid ethyl ester that functions as a melanogenesis inhibitor. It effectively reduces melanin production in cells, exhibiting an IC50 of 70 μM. This compound is valuable in research applications focused on skin pigmentation and related disorders, as well as in the exploration of potential therapeutic agents for hyperpigmentation conditions.
