TC-MCH 7c 是一种苯基吡啶酮衍生物,一种口服有效的,选择性的且可穿透血脑屏障的MCH1R拮抗剂,对 hMCH1R 的IC50为 5.6 nM。TC-MCH 7c 对人和小鼠 MCH1R 的Ki分别为 3.4 nM 和 3.0 nM。
生物活性 | TC-MCH 7c, a phenylpyridone derivative, is an orally available, selective and brain-penetrableMCH1Rantagonist with anIC50of 5.6 nM for hMCH1R[1]. TC-MCH 7c hasKis of 3.4 nM and 3.0 nM of human and mouse MCH1R, respectively[2]. |
IC50& Target | IC50: 5.6 nM (hMCH1R)[1] Ki: 3.4 nM (hMCH1R) and 3.0 nM (mouse MCH1R)[1] |
体外研究 (In Vitro) | TC-MCH 7c has an IC50of 9.7 μM for MCH1R in [Ca2+]i mobilization[1]. TC-MCH 7c has IC50s of 23 nM and 9.0 μM for FLIPR and hERG, respectively[2].
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体内研究 (In Vivo) | 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[1]. 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[2].
Animal Model: | C57BL/6J DIO mice[1] | 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[2] | 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. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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