Relugolix

한글명:Relugolix

카스 번호737789-87-6

상품명:Relugolix

CBNumberCB42658205

분자식C29H27F2N7O5S

포뮬러 무게623.63

MOL 파일737789-87-6.mol

화학적 성질

녹는점	228 °C (decomp)(Solv: ethyl acetate (141-78-6); tetrahydrofuran (109-99-9))
밀도	1.442±0.06 g/cm3(Predicted)
저장 조건	Store at -20°C
용해도	DMSO:20.0(Max Conc. mg/mL);32.1(Max Conc. mM) Ethanol:1.0(Max Conc. mg/mL);1.6(Max Conc. mM)
물리적 상태	결정성 고체
산도 계수 (pKa)	13.17±0.70(Predicted)
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

그림문자(GHS)

Relugolix 화학적 특성, 용도, 생산

개요
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.
용도
Relugolix is a highly selective, oral, nonpeptide GnRH antagonist being investigated as a possible prostate cancer treatment
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.
부작용
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 공급 업체

Send Inquriy