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TD-0212 TFA
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TD-0212 TFA图片
CAS NO:1073549-11-7
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
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。
Cas No.1073549-11-7
Canonical SMILESOC(C(F)(F)F)=O.OC(C1=CC=CC=C1C2=CC=C(CN3C(CNC([C@H](CC(C)C)S)=O)=C(CC)N=C3OCC)C(F)=C2)=O
分子式C30H35F4N3O6S
分子量641.67
溶解度DMSO: 125 mg/mL (194.80 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.