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GPCR

GPCR

Cat. No. Product Name CAS No. Information
CSN13936 TUG-891   1374516-07-0 TUG-891 is a selective agonist of long chain free fatty acid LCFA receptor 4 GPR120
CSN17794 TUG-770 1402601-82-4 TUG-770 is a highly potent free fatty acid receptor 1 FFA1GPR40 agonist with EC50 of 6 nM for hFFA1
CSN13717 TGR5 Receptor Agonist 1197300-24-5 TGR5 receptor agonist a potent TGR5 GPCR19 agonist showed improved potency in the U2-OS cell assay pEC50 68 and in melanophore cells pEC50 75
CSN15825 TAK-875 Hemihydrate 1374598-80-7 TAK-875 is a selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line 400-fold more potent than oleic acid
CSN13586 TAK-875 1000413-72-8 TAK-875 is a potent selective and orally bioavailable GPR40 agonist with EC50 of 0072 M
CSN21268 SB-568849 395679-53-5 SB-568849 is a melanin-concentrating hormone receptor 1 MCH R1 antagonist with a pKi of 77
CSN16413 PSN632408 857652-30-3 PSN632408 is an optimized agonist of GPR119 receptors that shows similar potency to OEA at both recombinant mouse and human GPR119 receptors exhibiting EC50 values of 56 and 79 M respectively
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 small molecule antagonist of the Epstein-Barr virus-induced gene 2 (EBI2 GPR183) receptor with IC50 of 16 nM (Binding) and 11 nM (Functional).
CSN21271 NGD-4715 476322-70-0 NGD-4715 is a selective and orally active melanin-concentrating hormone receptor 1 MCHR1 antagonist
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
CSN20277 ML-290 1482500-76-4 ML290 is a biased allosteric agonist at the relaxin receptor RXFP1 possessing a signalling profile indicative of vasodilator and anti-fibrotic properties
CSN16921 MK-6892 917910-45-3 MK-6892 is a highly potential GPR109A agonist with Ki value of 40 nM
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
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
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
CSN11273 Latanoprost 130209-82-4 Latanoprost is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect Latanoprost increases uveoscleral outflow and thereby reduces intraocular pressure
CSN18985 INT-777 R-Enantiomer 1198786-98-9 INT-777 R-enantiomer is the R-enantiomer of INT-777 with EC50 of 479 M for TGR5 and less potent than INT-777
CSN17039 INT-777 1199796-29-6 INT-777 is a potent and selective TGR5 agonist with remarkable in vivo activity EC50082 M
CSN12659 GW9508   885101-89-3 GW9508 is selective FFA1 GPR40 agonist with pEC50 of 732 and stimulates insulin secretion in a glucose-sensitive manner
CSN13558 GSK1292263 1032823-75-8 GSK1292263 is an agonist of GPR119 receptor that is used to treat type 2 diabetes
CSN22421 GPR84 Antagonist 8 1445846-30-9 GPR84 antagonist 8 is a selective GPR84 antagonist.
CSN16256 GPR40 Activator 2 1312787-30-6 GPR40 activator 2 is a potent GPR40 activator
CSN17674 GPR40 Activator 1 1309435-60-6 GPR40 activator 1 is a potent GPR40 activator for treatment of type 2 diabetes
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.
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
CSN20374 GPR119 Agonist C26 1353004-92-8 GPR119 agonist C26 shows potent GPR119 agonistic activity EC50 42 nM Emax 117 with improved liver microsome clearance than other GPR119 agonists in the series and exerted 33 reduction in blood glucose AUC at a dose of 10 mgkg in an oral glucose tolerance test in C57BL6 N mice
CSN20362 G-1 881639-98-1 G-1 is a nonsteroidal high-affinity selective agonist of GPR30 that binds with a Ki value of 11 nM
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.
CSN20481 DC260126 346692-04-4 DC260126 is antagoniat of free fatty acid receptor 1 FFA1GPR40 and inhibits FFA-induced the increase of intracellular Ca2 level
CSN20443 CYM 5541 945128-26-7 CYM-5541 is an allosteric agonist of S1P3 with EC50 of 72 nM - 132 nM.
CSN20173 CP-154526 157286-86-7 CP-154526 is a selective non-peptide CRF1 receptor antagonist Ki values are 27 and 10000 nM for CRF1 and CRF2 receptors respectively CP-154526 blocks CRF-induced adenylate cyclase activation Ki 37 nM and attenuates activation of the HPA axis by CRF
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
CSN13564 AR 231453 733750-99-7 AR 231453 is a potent and selective small molecule agonist of GPR119 that enhances glucose-dependent insulin secretion and glucagon-like peptide 1 GLP-1 release used as an antidiabetic agent
CSN16029 APD668 832714-46-2 APD668 is a potent GPR119 agonist with EC50 of 27 nM and 33 nM for hGPR119 and ratGPR119 respectively
CSN18543 APD597   897732-93-3 APD597 is an agonist of GPR119 with EC50 of 46 nM and is used for the treatment of type 2 diabetes
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
CSN13002 AMG-837 865231-46-5 AMG-837 is a potent GPR40 agonist EC5013 nM with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents
CSN22344 AM-1638 1142214-62-7 AM-1638 is a potent and orally bioavailable GPR40FFA1 full agonist with an EC50 of 016 M
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.
CSN24479 BAY-293 2244904-70-7
CSN22671 AH 7614 6326-06-3
CSN22386 Dihydromunduletone 674786-20-0
CSN23709 GW-803430 515141-51-2
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