SUFUGOLIX Chemical Properties

Density 

1.383±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C,unstable in solution, ready to use.

solubility 

DMF: 5mg/mL; DMF:PBS (pH 7.2) (1:2): 0.3mg/mL; DMSO: 3mg/mL

form 

A solid

pka

13.20±0.70(Predicted)

color 

Light yellow to yellow

SUFUGOLIX Usage And Synthesis

Description

Sufugolix is a gonadotropin-releasing hormone (GnRH) receptor antagonist (IC₅₀ = 0.1 nM). 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). 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.

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