TD-0212 TFA |
Catalog No.GC38856 |
TD-0212 TFA는 경구 활성 이중 약리학 안지오텐신 II 1형 수용체(AT1) 길항제 및 네프릴리신(NEP) 억제제로, AT1의 경우 pKi가 8.9이고 NEP의 경우 pIC50이 9.2입니다.
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Cas No.: 1073549-11-7
Sample solution is provided at 25 µL, 10mM.
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.
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