A gonadotropin-releasing hormone receptor antagonist
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Sufugolix

Item No. 27996

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
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-urea
CAS Number
308831-61-0
Synonyms
  • TAK-013
Molecular Formula
C36H31F2N5O4S
Formula Weight
667.7
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 5mg/mLDMF:PBS (pH 7.2) (1:2): 0.3mg/mLDMSO: 3mg/mL
λmax
299 nm
SMILES
O=C1N(C2=CC=CC=C2)C(C(C(CN(C)CC3=CC=CC=C3)=C(C4=CC=C(NC(NOC)=O)C=C4)S5)=C5N1CC6=C(F)C=CC=C6F)=O
InChi Code
InChI=1S/C36H31F2N5O4S/c1-41(20-23-10-5-3-6-11-23)21-28-31-33(44)43(26-12-7-4-8-13-26)36(46)42(22-27-29(37)14-9-15-30(27)38)34(31)48-32(28)24-16-18-25(19-17-24)39-35(45)40-47-2/h3-19H,20-22H2,1-2H3,(H2,39,40,45)
InChi Key
UCQSBGOFELXYIN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $40

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    5 mg

    $160

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    10 mg

    $246

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    Product Description

    Sufugolix is a gonadotropin-releasing hormone (GnRH) receptor antagonist (IC50 = 0.1 nM).1 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).2 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.1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sasaki, S., Cho, N., Nara, Y., 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. 46(1), 113-124 (2003).

    2. Hara, T., Araki, H., Kusaka, M., et al. Suppression of a pituitary-ovarian axis by chronic oral administration of a novel nonpeptide gonadotropin-releasing hormone antagonist, TAK-013, in cynomolgus monkeys. J. Clin. Endocrinol. Metab. 88(4), 1697-1704 (2003).