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首页-小分子抑制剂&激动剂-GPCR-GNRH Receptor-BAY1214784
BAY1214784

Chemical Structure : BAY1214784

CAS No.: 1631164-24-3

BAY1214784 (BAY-784 )

货号: PC-38730Not For Human Use, Lab Use Only.

BAY 1214784 (BAY-784) is an orally available, potent, and selective antagonist of gonadotropin-releasing hormone receptor (GnRH-R) with IC50 of 21/ 24/ 35 nM for human/rat/cynomolgus GnRH-R, respectively.

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

    生物&药学活性

    BAY 1214784 (BAY-784) is an orally available, potent, and selective antagonist of gonadotropin-releasing hormone receptor (GnRH-R) with IC50 of 21/ 24/ 35 nM for human/rat/cynomolgus GnRH-R, respectively.
    BAY 1214784 showed no agonistic activity in the human GnRH-R up to 20 uM, and was inactive in a cell-based panel of 25 GPCRs.
    BAY 1214784 (10 and 30 mg/kg, p.o.) demonstrated suppression of plasma luteinizing hormone levels in OVX rats and ORX cynomolgus monkeys.

    物理化学性质&存储条件

    分子量 672.11
    分子式 C29H26ClF4N3O5S2
    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

    Spiro[3H-indole-3,4′-[4H]thiopyran]-5-carboxamide, N-[[3-chloro-5-(trifluoromethyl)-2-pyridinyl]methyl]-2-cyclopropyl-1-[(4-fluorophenyl)sulfonyl]-1,2,2′,3′,5′,6′-hexahydro-, 1′,1′-dioxide, (2S)-

    参考文献

    1. Panknin O, et al. J Med Chem. 2020 Oct 22;63(20):11854-11881.

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