TD-0212 TFA 是一种具有口服活性的、血管紧张素II型1受体AT1 和脑啡肽酶 (NEP)的双抑制剂，其对AT1的pKi值为 8.9， 对NEP 的pIC50值为9.2。
货号:ajcx15496
CAS:1073549-11-7
分子式:C30H35F4N3O6S
分子量：641.67
溶解度:DMSO: 125 mg/mL (194.80 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

TD-0212 TFA is an orally active dual pharmacology angiotensin II type 1 receptor (AT1) antagonist and neprilysin (NEP) inhibitor, with a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP[1].

TD-0212 provides the enhanced activity of dual AT1/NEP inhibition with a potentially lower risk of angioedema relative to dual ACE/NEP inhibition[1].

TD-0212 produces blood pressure reductions similar to omapatrilat and combinations of AT1 receptor antagonists and NEP inhibitors in models of renin-dependent and -independent hypertension[1].

[1]. McKinnell RM, et al. Discovery of TD-0212, an Orally Active Dual Pharmacology AT1 Antagonist and Neprilysin Inhibitor (ARNI). ACS Med Chem Lett. 2018 Dec 3;10(1):86-91.