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 SMILES | CC(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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation 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. |
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