TD-0212 TFA
目录号: PL07708 纯度: ≥98%
CAS No. :1073549-11-7
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中文名称
TD-0212 TFA
英文名称
TD-0212 TFA
英文别名
(S)-4'-((2-Ethoxy-4-ethyl-5-((2-mercapto-4-methylpentanamido)methyl)-1H-imidazol-1-yl)methyl)-3'-fluoro-[1,1'-biphenyl]-2-carboxylic acid compound with 2,2,2-trifluoroacetic acid (1:1);TD-0212 (Tfa);TD-0212 TFA
Cas No.
1073549-11-7
分子式
C30H35F4N3O6S
分子量
641.67
包装储存
-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
TD-0212 TFA 是一种具有口服活性的、血管紧张素 II 型 1 受体 AT 1 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。
生物活性
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
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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