MK-8245 Trifluoroacetate
| CAS号 | 1415559-41-9 | 货号 | BCP17297 |
| 中文名 | MK-8245 Trifluoroacetate | ||
| 英文名 | MK-8245 Trifluoroacetate | ||
| 中文别名 | |||
| 英文别名 | MK 8245 Trifluoroacetate;MK8245 Trifluoroacetate; | ||
| 分子式 | C19H17BrF4N6O6 | 分子量 | 581.27 |
| 生物活性 | in 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. 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 | ||
| 信号通路 | Protease/Metabolic Enzyme | ||
| 靶 点 | SCD | ||
结构式
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