515141-51-2
中文名稱
GW 803430
英文名稱
GW 803430
CAS
515141-51-2
分子式
C25H24ClN3O3S
分子量
481.99
MOL 文件
515141-51-2.mol
更新日期
2024/11/07 22:37:11
515141-51-2 結(jié)構(gòu)式
基本信息
中文別名
化合物 T15450 英文別名
GW 3430GW 803430
GW-803430A
GW-803430 >=98% (HPLC)
Thieno[3,2-d]pyrimidin-4(3H)-one, 6-(4-chlorophenyl)-3-[3-methoxy-4-[2-(1-pyrrolidinyl)ethoxy]
6-(4-Chlorophenyl)-3-[3-methoxy-4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-thieno[3,2-d]pyrimidin-4(3H)-one
6-(4-chloro-phenyl)-3-[3-methoxy-4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-3H-thieno[3,2-d]pyrimidin-4-one
Thieno[3,2-d]pyrimidin-4(3H)-one, 6-(4-chlorophenyl)-3-[3-methoxy-4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-
物理化學(xué)性質(zhì)
儲(chǔ)存條件2-8°C
溶解度DMSO: ≥4mg/mL at warmed to 60°C
溶解度DMSO：加熱至 60°C 時(shí)≥4mg/mL
形態(tài)粉末
顏色白色至米色
常見問題列表
生物活性
GW-803430 (GW-3430) 是一種有效的選擇性黑色素濃縮激素受體 1 (MCH R1) 拮抗劑，pIC50 為 9.3。GW-803430 在肥胖動(dòng)物模型中具有口服活性。靶點(diǎn)
pIC50: 9.3 (MCH R1)
體外研究
GW-803430 demonstrates a potent antagonist activity towards MCH induced MCHR1 receptor with an IC 50 value of ~13?nM.
體內(nèi)研究
GW-803430 (0.3, 3, and 15 mg/kg; oral administration; once daily) causes a sustained dose-dependent weight loss relative to vehicle controls.
GW-803430 is a suitable compound for its good pharmacokinetic properties (bioavailability=31%, t
1/2
=11 h) and brain penetration (6:1 brain:plasma concentration) in mice.
| Animal Model: | High fat diet-induced obese AKR/J mice |
| Dosage: | 0.3, 3, and 15 mg/kg |
| Administration: | Orally, qd,12 days |
| Result: | Caused a sustained dose-dependent weight loss of -6.2%, -12.1%, and -13.1%, respectively, relative to vehicle controls. |