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首页-小分子抑制剂&激动剂-GPCR-mAChR-ML381 fumarate
ML381 fumarate

Chemical Structure : ML381 fumarate

CAS No.:

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ML381 fumarate (VU0488130 fumarate)

货号: PC-62144Not For Human Use, Lab Use Only.

ML381 (VU0488130) is a highly mAChR subtype selective M5 orthosteric antagonist with IC50/Ki of 450/340 nM for hM5, has no inhibitory activity on hM1-4 (IC50>30 uM).

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

    生物&药学活性

    ML381 (VU0488130) fumarate is a highly mAChR subtype selective M5 orthosteric antagonist with IC50/Ki of 450/340 nM for hM5, has no inhibitory activity on hM1-4 (IC50>30 uM).
    ML381 exhibits good DMPK properties and CNS penetration (B:P ratio of 0.58) to support both in vitro and in vivo studies.

    物理化学性质&存储条件

    分子量 495.488
    分子式 C25H25N3O8
    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-Acetylphenoxy)methyl]-N-methyl-N-[(1S)-1-pyridin-2-ylethyl]-1,2-oxazole-3-carboxamide fumarate

    参考文献

    1. Gentry PR, et al. ChemMedChem. 2014 Aug;9(8):1677-82.

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