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Relugolix

Relugolix Structure
Relugolix
  • CAS No.737789-87-6
  • Chemical Name:Relugolix
  • CBNumber:CB42658205
  • Molecular Formula:C29H27F2N7O5S
  • Formula Weight:623.63
  • MOL File:737789-87-6.mol
Relugolix Property
  • Melting point 228 °C (decomp)(Solv: ethyl acetate (141-78-6); tetrahydrofuran (109-99-9))
  • Density 1.442±0.06 g/cm3(Predicted)
  • storage temp. Store at -20°C
  • solubility DMSO:20.0(Max Conc. mg/mL);32.1(Max Conc. mM)
    Ethanol:1.0(Max Conc. mg/mL);1.6(Max Conc. mM)
  • form A crystalline solid
  • pka 13.17±0.70(Predicted)
  • color White to off-white
  • InChIKey AOMXMOCNKJTRQP-UHFFFAOYSA-N
  • SMILES N(C1=CC=C(C2SC3=C(C=2CN(C)C)C(=O)N(C2=NN=C(OC)C=C2)C(=O)N3CC2=C(F)C=CC=C2F)C=C1)C(NOC)=O
  • FDA UNII P76B05O5V6
  • NCI Drug Dictionary relugolix
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H361-H371
  • Precautionary statements P201-P202-P281-P308+P313-P405-P501-P260-P264-P270-P309+P311-P405-P501

Relugolix Chemical Properties,Usage,Production

  • Description Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. It possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209). Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al.
  • Uses Relugolix is a highly selective, oral, nonpeptide GnRH antagonist being investigated as a possible prostate cancer treatment
  • Mechanism of action The mechanism of action of relugolix is as a Gonadotropin Releasing Hormone Receptor Antagonist, and Cytochrome P450 3A Inducer, and Cytochrome P450 2B6 Inducer, and Breast Cancer Resistance Protein Inhibitor, and P-Glycoprotein Inhibitor. The physiologic effect of relugolix is by means of Decreased GnRH Secretion.
  • Pharmacokinetics Relugolix is a selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (IC50 = 0.12 nM).A single oral administration of relugolix at a dose of 3 mg/kg has been found to suppress luteinizing hormone (LH) levels for more than 24 hours in castrated cynomolgus monkeys, indicating a long duration of action. The drug (80–160 mg/day) has been found to reduce testosterone levels to sustained castrate levels in men with once-daily administration.[8] Lower dosages (10–40 mg/day) are being studied in the treatment of endometriosis and uterine fibroids to achieve partial sex hormone suppression.  The reasoning behind partial suppression for these conditions is to reduce the incidence and severity of menopausal symptoms such as hot flushes and to avoid bone mineral density changes caused by estrogen deficiency that can eventually lead to osteoporosis.
  • Clinical Use Relugolix was first approved in Japan in 2019, under the brand name Relumina, for the symptomatic treatment of uterine fibroids, and more recently by the United States' FDA in 2020, under the brand name Orgovyx, for the treatment of advanced prostate cancer. Relugolix has also been studied in the symptomatic treatment of endometriosis. 
  • Side effects Common side effects of Relugolix include: hot flashes; flushing of the skin; sweating; weight gain or loss of ability; pain in the muscles, back, joints or bones; fatigue; diarrhoea; constipation; difficulty sleeping; depression; and breast enlargement. More serious side effects include: dizziness; fainting; rapid heartbeat; or chest pain; swelling of the face, lips, mouth or tongue; difficulty breathing or swallowing; rash; measles; redness of the skin; chest pain or tightness in the chest; or pain in the arms, back, neck or jaw; sudden numbness or weakness of the face, arms, or legs (especially on one side of the body); sudden blurred consciousness; difficulty speaking or understanding; sudden difficulty seeing with one or both eyes; or sudden difficulty walking, walking, or seeing with one or both eyes. or sudden difficulty walking, dizziness, loss of balance or coordination, etc.
  • Synthesis Relugolix is produced by the reaction of 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione and phenyl N-methoxycarbamate.Relugolix
Relugolix Preparation Products And Raw materials
Raw materials
Preparation Products
Relugolix Suppliers
Global(312)Suppliers
  • Supplier：
    RongNa Biotechnology Co.,Ltd
  • Tel：+86-86-13583358881<br/>+8618560316533
  • Email：Brad@rongnabiotech.com
  • Country：China
  • ProdList：3084
  • Advantage：58

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Relugolix Spectrum
737789-87-6, RelugolixRelated Search:
  • 737789-87-6
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  • C29H27F2N7O5S
  • 瑞卢戈利,10 MM DMSO 溶液
  • 瑞卢戈利/精确称量
  • 瑞卢戈利对照品
  • 瑞卢戈利相关杂质
  • 瑞卢戈利及中间体、杂质
  • RVT-601|||瑞卢戈利|||TAK-385
  • 1-(4-(1-(2,6-二氟苄基)-5-((二甲胺基)甲基)-3-(6-甲氧基哒嗪-3-基)-2,4-二氧代-1,2,3,4-四氢噻吩并[2,3-D]嘧啶-6-基)苯基)-3-甲氧基脲
  • 瑞卢戈利 (TAK-385)
  • 瑞卢戈利粗品
  • 1-(4-(1-(2,6-二氟苄基)-5-((二甲基氨基)甲基)-3-(6-甲氧基哒嗪-3-基)-2,4-二氧代-1,2,3,4-四氢噻吩并[2,3-D]嘧啶-6-基)苯基)-3-甲氧基脲
  • 1-(4-(1-(2,6-二氟苄基)-5-((二甲基氨基)甲基)-3-(6-甲氧基哒嗪-3-基)-2,4-二氧-1,2,3,4-四氢噻吩并[2,3-D]嘧啶-6-基)苯基)-3-甲氧基脲
  • RELUGOLIX瑞卢戈利 TAK-385
  • 雷卢戈利克斯
  • N-[4-[1-[(2,6-二氟苯基)甲基]-5-[(二甲基氨基)甲基]-1,2,3,4-四氢-3-(6-甲氧基-3-吡嗪基)-2,4-二氧噻吩并[2,3-D]嘧啶-6-基]苯基]-N'-甲氧基脲
  • RELUGOLIX游离态
  • N- [4- [1 - [(2,6-二氟苯基)甲基]-5 - [(二甲基氨基)甲基] -1,2,3,4-四氢-3-(6-甲氧基-3-哒嗪基) - 2,4-二氧噻吩并[2,3-D]嘧啶-6-基]苯基] -N'-甲氧基脲
  • 1-(4-(1-(2,6-二氟苄基)-5-((二甲基氨基)甲基)-3-(6-甲氧基哒嗪-3-基)-2,4-二氧-1,2,3,4-四氢噻吩并[2,3-D]嘧啶-6-基)苯基)-3-甲氧基脲,瑞卢戈利
  • 瑞卢戈利
  • 737789-87-6
  • Relugolix, 10 mM in DMSO
  • Relugolix(NEC-1)
  • RVT-601|||TAK-385
  • 2H6]-RVT-601
  • ruiugoli
  • Rui Lu Geli
  • ethyl 5-(4-aminophenyl)-2-((2,6-difluorobenzyl)(ethoxycarbonyl)amino)-4-((dimethylamino)methyl)thiophene-3-carboxylate
  • A60%,B 40%
  • N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenylcarbamoyl)-N-methoxybutyramide
  • Relugoli
  • Relugolix TAK-385
  • 1-[4-[1-[(2,6-difluorophenyl)methyl]-5-(dimethylaminomethyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-6-thieno[4,5-e]pyrimidinyl]phenyl]-3-methoxyurea
  • Altropane
  • Relugolix
  • Cefepime hydrochloride anhydrous
  • Rui Lugoli
  • Urea, N-[4-[1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-1,2,3,4-tetrahydro-3-(6-methoxy-3-pyridazinyl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-N'-methoxy-

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