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GPCR

GPCR

Cat. No. Product Name CAS No. Information
CSN25826 Zaprinast 37762-06-4 Zaprinast is selective inhibitor of cGMP-specific phosphodiesterases V and VI (PDE5/6) and an agonist at the G protein-coupled receptor 35 (GPR35).
CSN24454 GPR39-C3   1621175-65-2 TC-G 1008 is a selective GPR39 agonist with EC50 value of 0.8 nM.
CSN25253 TC-G 1005 1415407-60-1 TC-G 1005 is a TGR5 agonist with EC50 values of 0.72nM and 6.2nM for hTGR5 and mTGR5, respectively. It exhibited a significant dose-dependent glucagon-like peptide-1 (GLP-1) secretion effect.
CSN25830 TC-G 1001 494191-73-0 TC-G 1001 is an agonist of GPR35.
CSN26374 SNAP 94847 487051-12-7 SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor 1 (MCHR1) antagonist with with Ki of 2.2 nM, Kd of 530 pM. It displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters[1][2].
CSN26659 2-(3-Pentylphenyl)acetic acid 1002101-19-0 Setogepram, also known as PBI-4050, is a CTGF expression inhibitor potentially for treatment of idiopathic pulmonary fibrosis.
CSN23214 ZQ 16 376616-73-8 Selective GPR84 agonist
CSN25229 SBI-115 882366-16-7 SBI-115 is a GPBAR1 (TGR5) antagonist.
CSN26356 Sb-756050 447410-57-3 SB756050 is an agonist of selective TGR5 and has the potential treatment of type 2 diabetes.
CSN26345 SB-657510 474960-44-6 SB-657510 is a selective urotensin II (UII) receptor antagonist with Ki value of 61 nM.
CSN51366 PW0787 2624131-45-7 PW0787 is an orally bioavailable, brain-penetrant, potent, and selective GPR52 agonist.
CSN34909 ONC212 1807861-48-8 ONC212 is a fluorinated ONC201 analog. It was identified as activator of an orphan GPCR GPR132 and Gαq signaling, which functions as a tumor suppressor.
CSN25832 Ogerin 1309198-71-7 Ogerin is a selective allosteric modulator of GPR68 with pEC50 of 6.83.
CSN27549 NE 52-QQ57 1401728-56-0 NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM. NE 52-QQ57 has anti-inflammatory activity.
CSN25819 MS 21570 65373-29-7 MS 21570 is an antagonist of GPR171 with IC50 of 220 nM.
CSN25822 5-Methacrylamidoisophthalic acid 73912-52-4 MS 15203 is a selective GPR171 partial agonist with EC50 of 90 nM.
CSN25825 ML 194 264233-05-8 ML 194 is a competitive and reversible antagonist of the orphan receptor GPR35 with Ki of 12.8 nM.
CSN25824 ML 145 1164500-72-4 ML 145 is a selective antagonist of the GPR35 orphan receptor with IC50 of 20.1 nM.
CSN23711 MCHr1 Antagonist 1 391610-37-0 MCHr1 antagonist 1 is a selective antagonist of MCH1 receptor with Kb of 1 nM and Ki of 4 nM at human MCHR1, may be used to reduce the body mass.
CSN21714 Lodoxamide 53882-12-5 Lodoxamide is an agonist of GPR35.
CSN25817 IBC 293 306935-41-1 IBC 293 is a selective agonist of GPR109B (HM74).
CSN24786 GPR40 agonist 4 2102196-57-4 GPR40 agonist 4 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54.
CSN33106 GPR35 antagonist 1 354126-20-8 GPR35 antagonist 1 is a GPR35 antagonist with IC50 value of 0.55μM.
CSN21935 GPR120-IN-1 1599477-75-4 GPR120-IN-1 is a selective Gpr120 agonist with a logEC50 of −7.62.
CSN26204 FTBMT 1358575-02-6 FTBMT is a selective GPR52 agonist with an EC50 of 75 nM. It demonstrates antipsychotic-like and procognitive effects in rodents and has revealed a potential therapeutic agent for schizophrenia.
CSN20629 Diphenyleneiodonium Chloride 4673-26-1 Diphenyleneiodonium chloride is a GPR3 agonist (EC50 = 1 μM) which activates adenylate cyclase through GPR3 but not GPR6 or GPR12. It also induces Ca2+ mobilization and β-arrestin receptor internalization.
CSN44136 DA-1241 1914136-10-9 DA-1241 is a first-in-class GPR119 agonist which improved glucose control in patients with type 2 diabetes in US Phase 1b study.
CSN32889 CVN424 2254706-21-1 CVN424 is an orally active and selective GPR6 inverse agonist with a EC50 of 9.4 nM and an EC50 of 38 nM.
CSN29508 N-acetyl-S-farnesyl-L-Cysteine 135304-07-3 Arazine (N-Acetyl-S-farnesyl-L-cysteine) is a cell-permeable modulator of G protein and G-protein coupled receptor signaling. Arazine can be a a substrate for isoprenylcysteine methyltransferase by competing with prenylated G protein or its receptors site.
CSN25407 4-CMTB 300851-67-6 4-CMTB is a selective free fatty acid receptor 2 (FFA2/GPR43) agonist and a positive allosteric modulator (pEC50=6.38).
CSN25414 3-chloro-5-hydroxybenzoic Acid 53984-36-4 3-chloro-5-hydroxybenzoic Acid is a selective GPR81 agonist that exhibited favorable in vivo effects on lipolysis in a mouse model of obesity.
CSN33107 TAK-041 1929519-13-0
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