Bioactivity | Edonentan (BMS 207940) hydrate is a potent and selective antagonist of the endothelin A (ETA) receptor, with a Ki of 10 pM. In rats, Edonentan has superior (100%) oral bioavailbility[1]. |
In Vivo | Edonentan (3-10 µmol/kg,口服)可阻断大的 ET-1 升压反应[1]。与 BMS-193884 (HY-19263) 相比,Edonentan (BMS 207940) 显示出改善的全身清除率 (Cl) 和稳态分布容积 (Vss)[1]。 |
Name | Edonentan hydrate |
CAS | 264609-13-4 |
Formula | C28H34N4O6S |
Molar Mass | 554.66 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Murugesan N, et al. Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective antagonist. J Med Chem. 2003 Jan 2;46(1):125-37. |