Relugolix CAS non: 737789-87-6

CAS NON: 737789-87-6
Molekile Fomil: C29H29F2N7O5S
Molekile pwa: 625,646
EINECS NON: N/A
MDL NON: N/A

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Non pwodwi: Relugolix CAS non: 737789-87-6

Synonyms:

TAK-385;

Relugolix;

1-[4-[1-[(2, 6-difluorophenyl) méthyle]-5-[(dimethylamino) méthyle]-3-(6-methoxypyridazin-3-yl)-2, 4-dioxothieno [2, 3-d] pyrimidin-6-yl] phenyl] -3-methoxyurea;

N-[4-[1-[(2, 6-Difluorophenyl) méthyle]-5-[(dimethylamino) méthyle]-1, 2, 3, 4-tetrahydro-3-(6-methoxy-3-pyridazinyl)-2, 4-dioxothieno [2, 3-d] pyrimidin-6-yl] phenyl]-n'-methoxy ure;

Chimik & pwopriyete fizik

Aparans: blan poud.

Épreuves: ≥ 99,0%

Relugolix (INN) (devlopman non Kod TAK-385) se yon ki pa-peptides, oralman-aktif, Selektif antagonis nan koryal-Divilge monn récepteurs a (GnRHR) (IC50 = 0,12 nM) ki se anba devlopman pou sevi ak klinik pa Takeda. Li se kounye a nan faz II ese klinik pou tretman an nan endometriosis, ranche leiomyoma, ak kanse pwostat.

Yon sel administrasyon oral nan relugolix nan yon doz de 3mg/kg te jwenn siprime nivo omon luteinizant pou plis pase 24 edtan nan castrated cynomolgus makak, ki endike yon dire lontan nan aksyon. Dwog la (80 – 160mg/jou) ki te jwenn diminye nivo testostewon yo soutni nivo bistonnen nan gason ak-chak jou administrasyon kwonik. Lower mouna (10-40mg/jou) yo te etidye nan tretman an nan endometriosis ak ranche leiomyoma reyalize pati seks omon gason soupresyon. Rezonman la deye soupresyon pasyel pou kondisyon sa yo se diminye ensidan a ak gravite nan sentom menopoz tankou flushes cho ak pou fe pou evite dansite mineral ki lakoz ki koze pa defisyans monn fi ki ka evantyelman mennen nan osteyopowoz.

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