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Basic Info

  • Grade: Pharmaceutical Grade

    Factory Location: Zhongcheng Future Industrial Park, Hangcheng Avenue, Baoan District, Shenzhen

    Main Sales Markets: North America,Central/South America,Western Europe,Eastern Europe,Asia,Middle East,Africa

  • Contract Manufacturing: CRO,CMO

  • Sample Provided: yes

    Payment Terms: L/C

    Relugolix Biological Activity

    Description:Relugolix is a novel, non-peptide, orally active gonadotropin-releasing hormone (GnRH) antagonist with IC50 of 0.33 nM in the presence of 40% fetal bovine serum, TAK-385 possesses higher affinity and potent antagonistic activity compared with TAK-013.target: GnRH [1]IC50: 0.33 nM [1]In vivo: In female knock-in mice, twice-daily oral administration of TAK-385 (100mg/kg) induces constant diestrous phases within the first week, decreases the uterus weight to ovariectomized levels and downregulated GnRH receptor mRNA in the pituitary after 4 weeks.

    Molecular Formula:C29H27F2N7O5S

    Molecular Weight:623.63

    PSA:169.36000

    LogP:3.96660

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