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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Guanylate Cyclase-BI 685509
BI 685509

Chemical Structure : BI 685509

CAS No.: 1579514-06-9

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BI 685509 (Avenciguat, BI-685509)

货号: PC-49581Not For Human Use, Lab Use Only.

BI 685509 (Avenciguat) is a potent, selective and orally bioavailable soluble guanylate cyclase (sGC) activator, increases cGMP in human and rat platelet-rich plasma treated with ODQ with EC50 of 467 nM and 304 nM, respectively.

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

    生物&药学活性

    BI 685509 (Avenciguat) is a potent, selective and orally bioavailable soluble guanylate cyclase (sGC) activator, increases cGMP in human and rat platelet-rich plasma treated with ODQ with EC50 of 467 nM and 304 nM, respectively.
    BI 685509 increased cGMP production with an EC50 of 9.29, 3.52, 4.69, 8.65, and 5.54 nM against the mouse, rat, dog, cynomolgus monkey, and human α2/β1 enzyme, respectively, compared with an EC50 of 6.81 nM against the human α1/β1 enzyme.
    In conscious telemetry-instrumented rats, BI 685509 did not effect mean arterial pressure (MAP) or heart rate (HR) at 3 and 10 mg/kg (p.o.), whereas 30 mg/kg decreased MAP and increased HR.
    BI 685509 at supratherapeutic doses (60 or 100 mg/kg po, qd, 10 days) attenuated MAP and HR responses to a single 100 mg/kg challenge.
    BI 685509 (1, 3, 10, 30 mg/kg/day qd) co-administered with enalapril (3 mg/kg/day) dose-dependently reduced proteinuria and incidence of glomerular sclerosis in the ZSF1 rat model.
    BI 685509 dose-dependently reduced tubulointerstitial fibrosis in the 7-day rat UUO model.

    物理化学性质&存储条件

    分子量 582.70
    分子式 C34H38N4O5
    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-ethoxy-1-(6-(3-methyl-2-((5-methyl-2-(tetrahydro-2H-pyran-4-yl)-1,2,3,4-tetrahydroisoquinolin-6-yl)methoxy)phenyl)pyridin-2-yl)-1H-pyrazole-4-carboxylic acid

    参考文献

    1. Reinhart GA, et al. J Pharmacol Exp Ther. 2022 Dec 6:JPET-AR-2022-001423.

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