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GPCR

GPCR

Cat. No. Product Name CAS No. Information
CSN23156 TC-O 9311 444932-31-4 TC-O 9311 is a potent orphan G protein-coupled receptor 139 (GPR139) agonist with an EC50 of 39 nM[1].
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.
CSN23214 ZQ 16 376616-73-8 Selective GPR84 agonist
CSN25229 SBI-115 882366-16-7 SBI-115 is a GPBAR1 (TGR5) antagonist.
CSN21268 SB-568849 395679-53-5 SB-568849 is a melanin-concentrating hormone receptor 1 MCH R1 antagonist with a pKi of 77
CSN24134 PMX 53 219639-75-5 PMX 53 is a potent C5a receptor antagonist.
CSN22483 PBI-4050 1254472-97-3 PBI-4050 acts as an agonist for GPR40 and as an antagonist or inverse agonist for GPR84.
CSN17281 NIBR189 1599432-08-2 NIBR189 is a potent and selective EBI2 (GPR183) receptor antagonist with IC50 value of 11nM.
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.
CSN22253 Monosodium Taurocholate   145-42-6 Monosodium taurocholate is an agonist of GPBAR1 and is potential of the treatment of type 2 diabetes and obesity in rats
CSN24295 ML401 1597489-14-9 ML401 is a selective inhibitor of GPR183.
CSN18472 MK-0354 851776-28-8 MK-0354 is a partial agonist of GPR109a receptor for hGPR109a mGPR109a with EC50 of 165108 M showed no activation of GPR109b
CSN21727 Melanin Concentrating Hormone, salmon 87218-84-6 Melanin concentrating hormone, a cyclic peptide originally isolated from chum salmon pituitaries, is a ligand for an orphan G protein-coupled receptor (SLC-1/GPR24) and MCHR2.
CSN21282 MCHr1 Antagonist 2 863115-70-2 MCHr1 antagonist 2 is an antagonist of melanin concentrating hormone receptor 1 with an IC50 of 65 nM also inhibits hERG with an IC50 of 40 nM in IMR-32 cells
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.
CSN21217 MCH-1 Antagonist 1 1039825-68-7 MCH-1 antagonist 1 is a potent melanin concentrating hormone MCH-1 antagonist with a Ki of 26 nM MCH-1 antagonist 1 also inhibits CYP3A4 with an IC50 of 10 M
CSN16084 MBX-2982 1037792-44-1 MBX-2982 is a selective orally-available GPR119 agonist for the treatment of type 2 tiabetes
CSN21714 Lodoxamide 53882-12-5 Lodoxamide is an agonist of GPR35.
CSN23709 GW-803430 515141-51-2 GW 803430 is a selective melanin-concentrating hormone receptor 1 (MCH1) antagonist with IC50 of 9.3 nM.
CSN25330 GSK1292263 HCl 1032824-54-6 GSK 1292263 HCl is a novel GPR119 receptor agonist that is currently under development for the treatment of type 2 diabetes.
CSN14893 Grifolic Acid 80557-12-6 Grifolic acid, a natural product isolated and purified from the Cylindrocarpon ianthothele var. majus, with anti-tumour and anti-haemolytic activities. Grifolic acid is a glucose-6-phosphatase inhibitor and a selective partial GPR120 agonist, can induce ERK and Ca2i responses in cells expressing GPR120.
CSN22421 GPR84 Antagonist 8 1445846-30-9 GPR84 antagonist 8 is a selective GPR84 antagonist.
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.
CSN16256 GPR40 Activator 2 1312787-30-6 GPR40 activator 2 is a potent GPR40 activator
CSN20435 GPR4 Antagonist C39c 1197879-16-5 GPR4 antagonist C39c shows potent cellular activity and is efficacious in animal models of angiogenesis, inflammation and pain.
CSN21935 GPR120-IN-1 1599477-75-4 GPR120-IN-1 is a selective Gpr120 agonist with a logEC50 of −7.62.
CSN17433 GPR120 Modulator 2 1050506-87-0 GPR120 modulator 2 is useful for modulating G protein-coupled receptor 120 GPR120
CSN17432 GPR120 Modulator 1 1050506-75-6 GPR120 modulator 1 is useful for modulating G protein-coupled receptor 120 GPR120
CSN22236 GPR120 Agonist 2 1234844-11-1 GPR120 Agonist 2 is a GPR120 agonist extracted from patent US 20110313003 A1 example 209
CSN12484 Ginsenoside Rb2 11021-13-9 Ginsenoside Rb2 is a 20 (S)-protopanaxadiol glycoside extracted from ginseng, shows potent antioxidant and anticancer biological activities.
CSN18981 Etrasimod 1206123-37-6 Etrasimod is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.
CSN22390 E6130 1427058-33-0 E6130 is an orally available and highly selective CX3CR1 modulator, that may be effective for treatment of inflammatory bowel disease.
CSN22386 Dihydromunduletone 674786-20-0 Dihydromunduletone is a selective adhesion G protein–coupled receptor antagonist (aGPR) with an IC50 of ~21 μM.
CSN25392 Deoxycholic acid sodium salt 302-95-4 Deoxycholic acid sodium salt is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.
CSN10769 Deoxycholic Acid   83-44-3 Deoxycholic Acid is a proinflammatory agent and used in a study to investigate dose-dependent anti-inflammatory effect of ursodeoxycholic acid in experimental colitis.
CSN20443 CYM 5541 945128-26-7 CYM-5541 is an allosteric agonist of S1P3 with EC50 of 72 nM - 132 nM.
CSN18454 CID-16020046 834903-43-4 CID-16020046 is a selective GPR55 LPI receptor antagonist with IC50 of 015 M
CSN22239 BMS-819881 1197420-05-5 BMS-819881 is a melaninconcentrating hormone receptor 1 MCHR1 antagonist which binds rat MCHR1 with a Ki of 7 nM BMS-819881 also is selective and potent for CYP3A4 activity with an EC50 of 13 M
CSN16029 APD668 832714-46-2 APD668 is a potent GPR119 agonist with EC50 of 27 nM and 33 nM for hGPR119 and ratGPR119 respectively
CSN18497 AMG-837 Sodium 865231-45-4 AMG-837 sodium is a potent GPR40 agonist EC5013 nM with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents
CSN20400 AEZS-108 139570-93-7 AEZS-108 is a peptide agonist of the gonadotropin releasing hormone-1 receptor (GnRH-1R).
CSN16337 6-OAU 83797-69-7 6-OAU is a surrogate agonist of GPR84 activating human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.
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.
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