A GnRH receptor antagonist (IC50 = 0.1 nM); inhibits GnRH-induced arachidonic acid release in CHO cells expressing human recombinant or monkey recombinant GnRH (IC50s = 0.1 and 10 nM

Sufugolix – 10 mg

Brand:
Cayman
CAS:
308831-61-0
Storage:
-20
UN-No:
Non-Hazardous - /

Sufugolix is a gonadotropin-releasing hormone (GnRH) receptor antagonist (IC50 = 0.1 nM).{45410} Sufugolix inhibits GnRH-induced arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607) release in CHO cells expressing human recombinant or monkey recombinant GnRH (IC50s = 0.1 and 10 nM, respectively), but not the rat GnRH receptor. It inhibits luteinizing hormone (LH) release stimulated by GnRH in monkey pituitary cells ex vivo (IC50 = 36 nM).{45411} Sufugolix (10 and 30 mg/kg) reduces increases in plasma LH following castration in male cynomolgus monkeys and lowers serum LH, estradiol, and progesterone levels in female cynomolgus monkeys when administered at a dose of 90 mg/kg.{45410,45411}  

 

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SKU: 27996 - 10 mg Category:

Description

A GnRH receptor antagonist (IC50 = 0.1 nM); inhibits GnRH-induced arachidonic acid release in CHO cells expressing human recombinant or monkey recombinant GnRH (IC50s = 0.1 and 10 nM, respectively), but not the rat GnRH receptor; inhibits LH release in monkey pituitary cells stimulated ex vivo with GnRH (IC50 = 36 nM); sufugolix reduces increases in plasma LH following castration in male cynomolgus monkeys at 10 and 30 mg/kg; lowers serum LH, estradiol, and progesterone levels in female cynomolgus monkeys at 90 mg/kg

Formal name: N-[4-[1-[(2,6-difluorophenyl)methyl]-1,2,3,4-tetrahydro-5-[[methyl(phenylmethyl)amino]methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]-N’-methoxy-urea

Synonyms:  TAK-013

Molecular weight: 667.7

CAS: 308831-61-0

Purity: ≥95%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Endocrinology & Metabolism|Hormones & Receptors||Research Area|Endocrinology & Metabolism|Reproductive Biology

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