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首页-小分子抑制剂&激动剂-Apoptosis-RIP kinase-RIPK1 inhibitor 22
RIPK1 inhibitor 22

Chemical Structure : RIPK1 inhibitor 22

CAS No.: 2095515-38-9

RIPK1 inhibitor 22 (RIP1-IN-22)

货号: PC-62633Not For Human Use, Lab Use Only.

RIPK1 inhibitor 22 is a highly potent, orally available, and brain-penetrating RIP1 kinase (RIPK1) inhibitor with pKi of 9.04.

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

    生物&药学活性

    RIPK1 inhibitor 22 is a highly potent, orally available, and brain-penetrating RIP1 kinase (RIPK1) inhibitor with pKi of 9.04.
    RIPK1 inhibitor 22 displays excellent specificity for RIP1 kinase over 406 kinases including RIP3 kinase.
    RIPK1 inhibitor 22 strongly suppressed necroptotic cell death and phosphorylation of MLKL (pMLKL) in HT-29 cells (nectoptosis; IC50=2.0 nM, pMLKL; IC50 = 1.3 nM) as well as L929 cells (nectoptosis; IC50=15 nM, pMLKL; IC50=2.7 nM).
    RIPK1 inhibitor 22 attenuates disease progression in the mouse experimental autoimmune encephalomyelitis (EAE) model of multiple sclerosis (MS) after oral administration (10 mg/kg, bid).

    物理化学性质&存储条件

    分子量 461.906
    分子式 C24H20ClN5O3
    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

    (3S)-3-(2-benzyl-3-chloro-7-oxo-2,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl)-5-methyl-4-oxo-2,3,4,5-tetrahydro-1,5-benzoxazepine-8-carbonitrile

    参考文献

    1. Yoshikawa M, et al. J Med Chem. 2018 Feb 27. doi: 10.1021/acs.jmedchem.7b01647.

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