864756-35-4
中文名稱(chēng)
TC-MCH 7C
英文名稱(chēng)
TC-MCH 7c
CAS
864756-35-4
分子式
C24H25FN2O3
分子量
408.47
MOL 文件
864756-35-4.mol
更新日期
2025/01/01 20:20:40
864756-35-4 結(jié)構(gòu)式
基本信息
中文別名
化合物 T13101 英文別名
TC-MCH 7c4-(4-Fluoro-benzyloxy)-1-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-1H-pyridin-2-one
4-[(4-Fluorophenyl)methoxy]-1-[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-2(1H)-pyridinone
物理化學(xué)性質(zhì)
熔點(diǎn)124-126 °C
沸點(diǎn)606.3±55.0 °C(Predicted)
密度1.27±0.1 g/cm3(Predicted)
儲(chǔ)存條件Store at RT
溶解度Soluble to 100 mM in 1eq. HCl and to 50 mM in DMSO
酸度系數(shù)(pKa)9.60±0.20(Predicted)
形態(tài)粉末
顏色Light yellow to yellow
常見(jiàn)問(wèn)題列表
生物活性
TC-MCH 7c 是一種苯基吡啶酮衍生物，一種口服有效的，選擇性的且可穿透血腦屏障的 MCH1R 拮抗劑，對(duì) hMCH1R 的 IC50 為 5.6 nM。TC-MCH 7c 對(duì)人和小鼠 MCH1R 的 Ki 分別為 3.4 nM 和 3.0 nM。靶點(diǎn)
IC50: 5.6 nM (hMCH
1
R)
Ki: 3.4 nM (hMCH
1
R) and 3.0 nM (mouse MCH
1
R)
體外研究
TC-MCH 7c has an IC
50
of 9.7 μM for MCH
1
R in [Ca
2+
]i mobilization.
TC-MCH 7c has IC
50
s of 23 nM and 9.0 μM for FLIPR and hERG, respectively.
體內(nèi)研究
TC-MCH 7c (oral; 3-30 mg/kg; once-daily for 1.5 months) exhibits excellent body weight reduction in a dose-dependent manner in DIO mice model.
TC-MCH 7c (oral; 3-30 mg/kg) with 30 mg/kg has plasma concentrations of 5.1, 1.8, and 0.7 μM at 2, 15, and 24 hours, respectively.
| Animal Model: | C57BL/6J DIO mice |
| Dosage: | 3, 10 and 30 mg/kg |
| Administration: | Oral; once-daily for 1.5 months |
| Result: | Exhibited excellent body weight reduction in a dose-dependent manner. |
| Animal Model: | Diet-induced obesity mice |
| Dosage: | 3, 10 and 30 mg/kg (Pharmacokinetic Analysis) |
| Administration: | Oral |
| Result: | Plasma concentrations at 2, 15, and 24 hours were 5.1, 1.8, and 0.7 μM, respectively. |