For research use only, not for therapeutic use.
A-192621（Cat No.:I000182）is a selective antagonist of the cannabinoid receptor 2 (CB2), which is primarily involved in immune system regulation and inflammation. By specifically blocking CB2 receptors, A-192621 inhibits the activation of immune cells like macrophages and microglia, making it a useful tool in studying the role of CB2 in immune responses and inflammatory diseases. Its selective targeting of CB2, without affecting CB1 receptors in the central nervous system, reduces psychoactive effects, making it valuable for research on therapies for conditions such as chronic pain, inflammation, and neurodegenerative disorders.
| Catalog Number | I000182 |
| CAS Number | 195529-54-5 |
| Synonyms | A-192621; A 192621; A192621; A-192621-1; A-192621.1.;(2R,3R,4S)-4-(benzo[d][1,3]dioxol-5-yl)-1-(2-((2,6-diethylphenyl)amino)-2-oxoethyl)-2-(4-propoxyphenyl)pyrrolidine-3-carboxylic acid |
| Molecular Formula | C33H38N2O6 |
| Purity | ≥95% |
| Target | endothelin-B antagonist |
| Solubility | Soluble in DMSO, not in water |
| Storage | Store at -20°C |
| IUPAC Name | (2R,3R,4S)-4-(1,3-benzodioxol-5-yl)-1-[2-(2,6-diethylanilino)-2-oxoethyl]-2-(4-propoxyphenyl)pyrrolidine-3-carboxylic acid |
| InChI | InChI=1S/C33H38N2O6/c1-4-16-39-25-13-10-23(11-14-25)32-30(33(37)38)26(24-12-15-27-28(17-24)41-20-40-27)18-35(32)19-29(36)34-31-21(5-2)8-7-9-22(31)6-3/h7-15,17,26,30,32H,4-6,16,18-20H2,1-3H3,(H,34,36)(H,37,38)/t26-,30-,32+/m1/s1 |
| InChIKey | LQEHCKYYIXQEBM-FUKIBTTHSA-N |
| SMILES | CCCOC1=CC=C(C=C1)[C@H]2[C@@H]([C@H](CN2CC(=O)NC3=C(C=CC=C3CC)CC)C4=CC5=C(C=C4)OCO5)C(=O)O |
| Reference | </br>1:Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: ex vivo and in vivo studies. Wessale JL, Adler AL, Novosad EI, Calzadilla SV, Dayton BD, Marsh KC, Winn M, Jae HS, von Geldern TW, Opgenorth TJ, Wu-Wong JR.Clin Sci (Lond). 2002 Aug;103 Suppl 48:112S-117S. PMID: 12193067 </br>2:Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: in vitro studies. Wu-Wong JR, Dixon DB, Chiou WJ, Sorensen BK, Liu G, Jae HS, Tasker A, von Geldern TW, Winn M, Opgenorth TJ.Clin Sci (Lond). 2002 Aug;103 Suppl 48:107S-111S. PMID: 12193066 </br>3:Use of A-192621 and IRL-2500 to unmask the mesenteric and renal vasodilator role of endothelin ET(B) receptors. Leung SW, Lim SL, Pang CC, Man RY.J Cardiovasc Pharmacol. 2002 Apr;39(4):533-43. PMID: 11904527 </br>4:Use of A-192621 to provide evidence for involvement of endothelin ET(B)-receptors in endothelin-1-mediated cardiomyocyte hypertrophy. Cullen JP, Bell D, Kelso EJ, McDermott BJ.Eur J Pharmacol. 2001 Apr 13;417(3):157-68. PMID: 11334846 </br>5:Effects of A-192621.1, a specific endothelin-B antagonist, on intrarenal hemodynamic responses to endothelin-1. Brodsky S, Abassi Z, Wessale J, Ramadan R, Winaver J, Hoffman A.J Cardiovasc Pharmacol. 2000 Nov;36(5 Suppl 1):S311-3. PMID: 11078406 |
