SUFUGOLIX
SUFUGOLIX Basic information
- Product Name:
- SUFUGOLIX
- Synonyms:
-
- SUFUGOLIX
- TAK013
- N-(4-(5-((benzyl(methyl)amino)methyl)-1-(2,6-difluorobenzyl)-1,2,3,4-tetrahydro-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl)phenyl)-N'-methoxyurea
- TAK013;TAK 013
- Sufugolix(TAK-013)
- SUFUGOLIX, >98%
- tak-013, >98%
- Urea, 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-
- CAS:
- 308831-61-0
- MF:
- C36H31F2N5O4S
- MW:
- 667.72
- Mol File:
- 308831-61-0.mol
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.
Uses
Sufugolix (TAK-013) is a highly potent and orally available luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC50 of 0.1 nM.
in vivo
Oral administration of sufugolix causes almost complete suppression of the plasma LH levels in castrated male cynomolgus monkeys at a 30 mg/kg dose with sufficient duration of action (more than 24 h). The maximum plasma concentrations of sufugolix are 0.34 μM (reached 6 h after administration) and 0.18 μM (reached 4 h after administration) at 30 and 10 mg/kg doses, respectively[1].
References
[1] Sasaki S, et al. Discovery of a thieno[2,3-d]pyrimidine-2,4-dione bearing a p-methoxyureidophenyl moiety at the 6-position: a highly potent and orally bioavailable non-peptide antagonist for the human luteinizing hormone-releasing hormone receptor. J Med Chem. 2003 Jan 2;46(1):113-24. DOI:10.1021/jm020180i
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