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 an IC50 of 68 nM, while being only weakly active in the HepG2 cell assay which is devoid of active OATPs with an IC50 of ~1 ¦ÌM. MK-8245 displays highly selective activity for the ¦¤-5 and ¦¤-6 desaturases (i.e., >100000 ¦ÌM vs rat and human ¦¤5D and ¦¤6D as assessed in the HepG assay.

June 21, 2017

prudect name : 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 an IC50 of 68 nM, while being only weakly active in the HepG2 cell assay which is devoid of active OATPs with an IC50 of ~1 ¦ÌM. MK-8245 displays highly selective activity for the ¦¤-5 and ¦¤-6 desaturases (i.e., >100000 ¦ÌM vs rat and human ¦¤5D and ¦¤6D as assessed in the HepG assay.
MK-8245

Synonyms: MERK-8245CAS NO: 1030612-90-8Molecular Formula: C17H16BrFN6O4Molecular Weight: 466.04Purity: 97% minSolubility: In DMSOStorage: −20°C


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References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18528277