MK-8245

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更新时间： 2025-09-07 18:21:53

CAS号：1030612-90-8

常用名： 2H-四唑乙酸,5-[3-[4-(2-溴-5-氟苯氧基)-1-哌啶基]-5-异恶唑]-

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纯度： 98.0%

备货期： 10天

库存： 现货

其他详情（用途，包装）：
用途： MK-8245 is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy.IC50 value: 1 nM (hSCD1) [1]Target: SCD1in vitro: MK-8245, a phenoxy piperidine isoxazole derivative, has been identified as a potent and liver-specific SCD inhibitor. It contains a tetrazole acetic acid moiety, which is the key molecule for OATPs recognition and liver-targeting. MK-8245 displays similar potencies against human, rat and mouse SCD1 with IC50 values of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1. MK-8245 exhibits a significant SCD inhibition in the rat hepatocyte assay which contains functional, active OATPs with IC50 of 68 nM, while being only weakly active in the HepG2 cell assay which is devoid of active OATPs with IC50 of ~1 μM. MK-8245 displays highly selective activity for the Δ-5 and Δ-6 desaturases (i.e., >100000 μM vs rat and human Δ5D and Δ6D as assessed in the HepG assay [1].in vivo: Administration of MK-8245 at 10 mg/kg in mice exhibits a tissue distribution profile concentrated in the liver. It shows a liver-to-Harderian gland ratio of 21, suggesting a high degree of liver-targeting compared to a systemically distributed compound with liver-to-Harderian gland ratio of 1.5. Oral dosing of MK-8245 in mice, rats, dogs, and rhesus monkeys demonstrates that MK-8245 is distributed mainly to the liver, with low exposure in tissues associated with potential adverse events. The liver-to-skin ratios are >30:1 in all four species. Administration of MK-8245 to eDIO mice before the glucose challenge improves glucose clearance in a dose-dependent manner with ED50 of 7 mg/kg. 物理化学性质： CAS号：1030612-90-8 常用中文名：2H-四唑乙酸,5-[3-[4-(2-溴-5-氟苯氧基)-1-哌啶基]-5-异恶唑]- 常用英文名：MK-8245 分子式：C17H16BrFN6O4 分子量：467.249 密度：1.8±0.1 g/cm3 沸点：698.3±65.0 °C at 760 mmHg 熔点：N/A 闪点：376.1±34.3 °C 储存条件：室温，干燥，密封

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公司名：上海化源世纪贸易有限公司推荐

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其他供应商价格：

2022-02-19 价格：￥682.9 MK-8245

2023-09-19 价格：￥需询单 MK8245

2020-12-08 价格：￥1425.0 MK-8245

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2H-四唑乙酸,5-[3-[4-(2-溴-5-氟苯氧基)-1-哌啶基]-5-异恶唑]-价格

MK-8245

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