TD-0212 TFA is an orally active dual pharmacology angiotensin II type 1 receptor (AT 1 ) antagonist and neprilysin (NEP) inhibitor, with a pK i of 8.9 for AT 1 and a pIC 50 of 9.2 for NEP.
性状
Solid
IC50 & Target[1][2]
pKi: 8.9 (AT1)
pIC50: 9.2 (NEP).
体外研究(In Vitro)
TD-0212 provides the enhanced activity of dual AT1/NEP inhibition with a potentially lower risk of angioedema relative to dual ACE/NEP inhibition. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[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.
溶解度数据
In Vitro: DMSO : 125 mg/mL (194.80 mM; Need ultrasonic)配制储备液