308831-61-0

Basic information

• Product Name: SUFUGOLIX
• Synonyms: SUFUGOLIX;TAK013
• CAS NO: 308831-61-0
• Molecular Formula: C₃₆H₃₁F₂N₅O₄S
• Molecular Weight: 667.734
• Mol File: 308831-61-0.mol
• Article Data: 11

Chemical Properties

• Appearance: /
• Density: 1.383±0.06 g/cm3(Predicted)
• PKA: 13.20±0.70(Predicted)
• CAS DataBase Reference: SUFUGOLIX(CAS DataBase Reference)
• NIST Chemistry Reference: SUFUGOLIX(308831-61-0)
• EPA Substance Registry System: SUFUGOLIX(308831-61-0)

Safety Data

• Hazardous Substances Data: 308831-61-0(Hazardous Substances Data)

Usage

Description

Sufugolix is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC50 value of 0.1 nM. It effectively inhibits GnRH-induced arachidonic acid release in CHO cells expressing human or monkey recombinant GnRH receptors, but not the rat GnRH receptor. Sufugolix also suppresses luteinizing hormone (LH) release stimulated by GnRH in monkey pituitary cells ex vivo and has been shown to reduce plasma LH levels following castration in male cynomolgus monkeys. Additionally, it lowers serum LH, estradiol, and progesterone levels in female cynomolgus monkeys when administered at a higher dose.

Uses

Used in Pharmaceutical Industry:
Sufugolix is used as a therapeutic agent for the treatment of conditions related to the overproduction of luteinizing hormone (LH) and other sex hormones. Its application in this context is due to its ability to inhibit GnRH-induced LH release and modulate the levels of sex hormones such as estradiol and progesterone.
Used in Endocrinology Research:
Sufugolix is used as a research tool in endocrinology for studying the role of GnRH receptors and their involvement in the regulation of sex hormone production. Its application in this field is based on its high potency as a GnRH receptor antagonist and its selectivity for human and monkey GnRH receptors over the rat receptor.
Used in Preclinical Studies:
Sufugolix is used in preclinical studies to evaluate its potential as a treatment for conditions related to hormonal imbalances, such as endometriosis and uterine fibroids. Its application in these studies is due to its ability to lower serum LH, estradiol, and progesterone levels, which may help alleviate symptoms and improve patient outcomes.
Used in Drug Development:
Sufugolix is used in the development of new pharmaceuticals targeting GnRH receptors for the treatment of various hormonal disorders. Its application in drug development is based on its potent antagonistic activity and potential to serve as a lead compound for the design of more effective and selective GnRH receptor antagonists.

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Relevant articles and documents

PREMATURE OVULATION PREVENTIVE AGENT

The present invention provides a premature ovulation inhibitor for use in in vitro fertilization or embryo transfer process, which contains a nonpeptidic compound having a gonadotropin releasing hormone antagonistic action. The premature ovulation inhibitor for use in in vitro fertilization or embryo transfer process of the present invention is low toxic, permits oral administration, and has a superior inhibitory effect on premature ovulation in in vitro fertilization or embryo transfer process.

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