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WAY 207024 dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
WAY 207024 dihydrochloride图片
CAS NO:872002-73-8
包装:10mg
市场价:3896元

产品介绍
GnRH-R antagonist, potent
Cas No.872002-73-8
化学名6-((4-(2-(4-(tert-butyl)phenyl)-1H-benzo[d]imidazol-4-yl)piperazin-1-yl)methyl)quinoxaline dihydrochloride
Canonical SMILESCC(C)(C1=CC=C(C2=NC3=C(N2)C=CC=C3N4CCN(CC5=CC6=C(N=CC=N6)C=C5)CC4)C=C1)C.Cl.Cl
分子式C30H32N6.2HCl
分子量549.54
溶解度<46.71mg/ml in DMSO
储存条件Desiccate at RT
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

WAY 207024 dihydrochloride is a potent gonadotropin releasing hormone receptor (GnRH-R) antagonist with IC50 values of 12 and 71 nM for human and rat GnRH receptors, respectively [1].
GnRH-R is a member of the G-protein coupled receptor (GPCR) family. Activation of the receptor by binding of gonadotropin-releasing hormone causes the release of leuteinizing hormone (LH) and follicle stimulating hormone (FSH) from the anterior pituitary gland and they in turn stimulate sex hormone synthesis and release into the general circulation [1].
WAY 207024 dihydrochloride displayed moderate membrane permeability properties and rat liver microsome stability [1].
In castrated rats, WAY 207024 dihydrochloride was absorbed well following oral administration with a bioavailability of 74%. Also, WAY 207024 dihydrochloride (30 mg/kg, oral gavage) reduced serum LH levels starting at 1 h post dosing and LH levels had returned to the vehicle treated group levels after 24h [1].
References:
[1]. Pelletier JC, Chengalvala MV, Cottom JE, et al. Discovery of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): an orally active antagonist of the gonadotropin releasing hormone receptor (GnRH-R). J Med Chem, 2009, 52(7): 2148-2152.