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SUFUGOLIX

SUFUGOLIX Structure
SUFUGOLIX
  • CAS No.308831-61-0
  • Chemical Name:SUFUGOLIX
  • CBNumber:CB12451333
  • Molecular Formula:C36H31F2N5O4S
  • Formula Weight:667.72
  • MOL File:308831-61-0.mol
SUFUGOLIX Property
  • 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
  • FDA UNII 56S17Z6X9M
Safety
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H315-H319-H335
  • Precautionary statements P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P321-P362+P364-P332+P313-P337+P313-P403+P233-P405-P501

SUFUGOLIX Chemical Properties,Usage,Production

  • 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
SUFUGOLIX Preparation Products And Raw materials
Raw materials
Preparation Products
SUFUGOLIX Suppliers
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SUFUGOLIX Spectrum
308831-61-0, SUFUGOLIXRelated Search:
  • 抑制剂
  • 化合物SUFUGOLIX,10 MM DMSO 溶液
  • 化合物SUFUGOLIX
  • 舒夫戈利
  • 308831-61-0
  • Sufugolix, 10 mM in DMSO
  • TAK 013,Inhibitor,Sufugolix,inhibit,TAK013
  • TAK-013 1-(4-(5-((benzyl(methyl)amino)methyl)-1-(2,6-difluorobenzyl)-2,4-dioxo-3-phenyl-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-3-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-
  • tak-013, >98%
  • SUFUGOLIX, >98%
  • Sufugolix(TAK-013)
  • TAK013;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
  • TAK013
  • SUFUGOLIX

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