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首页-小分子抑制剂&激动剂-Others-Other Targets-Org 214444-0
Org 214444-0

Chemical Structure : Org 214444-0

CAS No.: 914093-78-0

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Org 214444-0 (Org214444-0)

货号: PC-20748Not For Human Use, Lab Use Only.

Org 214444-0 is a highly potent, selective, allosteric agonist of follicle stimulating hormone receptor (FSHR) with EC50 of 2.0/1.2 nM (human/rat FSHR) in cell-based assays.

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

    生物&药学活性

    Org 214444-0 is a highly potent, selective, allosteric agonist of follicle stimulating hormone receptor (FSHR) with EC50 of 2.0/1.2 nM (human/rat FSHR) in cell-based assays.
    Org 214444-0 stimulates cAMP synthesis in cell line expressing human FSHR with EC50 of 5 nM in cAMP assays, Emax of 102%.
    Org 214444-0 displays >200-fold selective over the human and rat LHR, and does not activate the human TSHR.
    Org 214444-0 has also negligible antagonistic activity at the human and rat LHR and human TSHR at 1 uM.
    Org 214444-0 is an allosteric agonist interacting with the transmembrane region of the FSHR.
    When co-incubated with FSH, Org 214444-0 augments FSH's potency in binding (6.5-fold) and adenylyl cyclase/cAMP activation (3.5-fold) in a concentration-dependent manner.
    Org 214444-0 induces FSHR internalization and is only marginally effective in stimulating phospholipase C.
    Org 214444-0 stimulates cAMP and estradiol production in human granulosa cells in culture and supports the follicular phase in mature female rats.

    物理化学性质&存储条件

    分子量 664.56
    分子式 C30H32BrF2N3O5S
    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

    N-(2-((2-bromo-4-((4R,7S)-3-cyano-2-methyl-5-oxo-7-propyl-1,4,5,6,7,8-hexahydroquinolin-4-yl)-6-ethoxyphenoxy)methyl)-4,5-difluorophenyl)methanesulfonamide

    参考文献

    1. Chris J van Koppen, et al. Biochem Pharmacol. 2013 Apr 15;85(8):1162-70.

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