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

Chemical Structure : Forasartan

CAS No.: 145216-43-9

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Forasartan (SC-52458, SC52458)

货号: PC-49657Not For Human Use, Lab Use Only.

Forasartan (SC-52458) is a potent, specific, competitive and reversible angiotensin II receptor (AT1 receptor) antagonist with binding Ki value of 2.9 nM.

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

    生物&药学活性

    Forasartan (SC-52458) is a potent, specific, competitive and reversible angiotensin II receptor (AT1 receptor) antagonist with binding Ki value of 2.9 nM.
    Forasartan (SC-52458) is a potent inhibitor of [125I]AII binding to AT1 receptors in rat adrenal cortex and uterine smooth muscle membranes (IC50 values of 2.8 and 6.9 nM, respectively).
    Forasartan (SC-52458) shows no effect on the activity of angiotensin converting enzyme (ACE) or renin in vitro.
    Forasartan administration selectively inhibits L-type calcium channels in the plateau component of the smooth muscle cells, favoring relaxation of the smooth muscle.
    Forasartan also decreases heart rate by inhibiting the positive chronotropic effect of high frequency preganglionic stimuli.
    In dogs, it was found to block the pressor response of Angiotensin II with maximal inhibition, 91%.
    Daily treatment with Forasartan (SC-52458) at 20, 30, and 50 mg/kg by gavage for 4 days decreased blood pressure (BP) in conscious, spontaneously hypertensive rats (SHR).

    物理化学性质&存储条件

    分子量 416.53
    分子式 C23H28N8
    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

    5-[(3,5-dibutyl-1,2,4-triazol-1-yl)methyl]-2-[2-(2H-tetrazol-5-yl)phenyl]pyridine

    参考文献

    1. Csajka C, et al. Clinical Pharmacokinetics. 41 (2): 137–52.

    2. G M Olins, et al. J Cardiovasc Pharmacol. 1993 Oct;22(4):617-25.

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