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首页-小分子抑制剂&激动剂-GPCR-Angiotensin Receptor-TD-0212
TD-0212

Chemical Structure : TD-0212

CAS No.: 1073549-10-6

TD-0212 (TD0212, TD 0212)

货号: PC-35877Not For Human Use, Lab Use Only.

TD-0212 (TD0212) is a potent, orally efficacious, dual AT1 antagonist/Neprilysin (NEP) inhibitor with pKi of 8.9 (AT1) and pIC50 of 9.2 (NEP).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    TD-0212 (TD0212) is a potent, orally efficacious, dual AT1 antagonist/Neprilysin (NEP) inhibitor with pKi of 8.9 (AT1) and pIC50 of 9.2 (NEP).
    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, does not increase TPE at antihypertensive doses in rat tracheal plasma extravasation (TPE) models.

    物理化学性质&存储条件

    分子量 527.655
    分子式 C28H34FN3O4S
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    (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

    参考文献

    1. R. Murray McKinnell, et al. Discovery of TD-0212, an Orally Active Dual Pharmacology AT1 Antagonist and Neprilysin Inhibitor (ARNI). ACS Med. Chem. Lett. DOI: 10.1021/acsmedchemlett.8b00462

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