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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 | TC-G-1008 | 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 | GPR35 agonist 2 | 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 | Fezagepras | 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 | SB756050 | 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. |
| CSN24134 | PMX-53 | 219639-75-5 | PMX 53 is a potent C5a receptor antagonist. |
| 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 | MS21570 | 65373-29-7 | MS 21570 is an antagonist of GPR171 with IC50 of 220 nM. |
| CSN25822 | MS15203 | 73912-52-4 | MS 15203 is a selective GPR171 partial agonist with EC50 of 90 nM. |
| CSN25825 | CID 2745687 | 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 | GPR109 receptor agonist-1 | 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 | CID1231538 | 354126-20-8 | GPR35 antagonist 1 is a GPR35 antagonist with IC50 value of 0.55μM. |
| CSN21935 | GPR120 Agonist 3 | 1599477-75-4 | GPR120-IN-1 is a selective Gpr120 agonist with a logEC50 of −7.62. |
| CSN25587 | G15 | 1161002-05-6 | G15 is a high-affinity and selective GPER receptor antagonist with Ki value of 20nM. |
| CSN26204 | TP-024 | 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 | Arazine | 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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