| Identification | Back Directory | [Name]
SUFUGOLIX | [CAS]
308831-61-0 | [Synonyms]
TAK013
SUFUGOLIX
tak-013, >98%
TAK013;TAK 013
SUFUGOLIX, >98%
Sufugolix(TAK-013)
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
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- | [Molecular Formula]
C36H31F2N5O4S | [MDL Number]
MFCD09837896 | [MOL File]
308831-61-0.mol | [Molecular Weight]
667.72 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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. | [storage]
Store at -20°C,unstable in solution, ready to use. |
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