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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Matrix Metalloproteinase (MMP)-GLPG1972
GLPG1972

Chemical Structure : GLPG1972

CAS No.: 1957278-93-1

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GLPG1972 (Aldumastat, S201086)

货号: PC-73394Not For Human Use, Lab Use Only.

GLPG1972 (Aldumastat, S201086) is a potent and selective small-molecule inhibitor of ADAMTS5 with IC50 of 19 and <23 nM against human and rat ADAMTS5, respectively.

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

    生物&药学活性

    GLPG1972 (Aldumastat, S201086) is a potent and selective small-molecule inhibitor of ADAMTS5 with IC50 of 19 and <23 nM against human and rat ADAMTS5, respectively.
    GLPG1972 displayed 8-fold selectivity over ADAMTS4, and 60->5,000-fold selectivity over other related proteases (MMPS and ADAM17/TACE).
    GLPG1972 dose-dependently inhibited the IL-α stimulated GAG release with IC50 of <1.5 uM in mouse cartilage explants.
    GLPG1972 dose-dependently inhibited AGNx1 release induced by IL-1β with IC50 of <1 uM in human articular cartilage explants, with no effect on the release of the MMP-driven generation of the AGNx2 neoepitope.
    GLPG1972/S201086 (30-120 mg/kg b.i.d) reduced femorotibial cartilage proteoglycan loss (23-37%), cartilage structural damage (23-39%) and subchondral bone sclerosis (21-36%) in DMM mice.
    GLPG1972/S201086 (10-50 mg/kg b.i.d) reduced cartilage damage (OARSI score reduction, 6-23%), and decreased proteoglycan loss (∼27%) and subchondral bone sclerosis (77-110%) in MNX rats.

    物理化学性质&存储条件

    分子量 406.434
    分子式 C20H24F2N4O3
    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)-5-cyclopropyl-5-(3-((S)-4-(3,5-difluorophenyl)-3-methylpiperazin-1-yl)-3-oxopropyl)imidazolidine-2,4-dione

    参考文献

    1. Clement-Lacroix P, et al. Osteoarthritis Cartilage. 2022 Feb;30(2):291-301.

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