中文名称 | PF-04620110 |
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英文名称 | trans-4-[4-(4-Amino-7,8-dihydro-5-oxopyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl]-cyclohexaneacetic acid |
CAS号 | 1109276-89-2 |
分子式 | C21H24N4O4 |
分子量 | 396.44 |
外观 | White to off-white powder |
储存条件 | Dry, dark and at 0 - 4 ℃ for short term (days to weeks) or -20 ℃ for long term (months to years). |
PF-04620110 (PF04620110; PF 04620110) is a novel, potent, orally bioactive, and selective diglyceride acyltransferase-1 (DGAT1) inhibitor with the potential to treat type 2 diabetes mellitus. It inhibits DGAT1 with an IC50 of 19 nM. PF-04620110 has been advanced to clinical trials on the basis of the excellent pharmacologic and pharmacokinetic profiles. F-04620110 shows high selectivity versus a broad panel of off-target pharmacologic end points. In vivo DGAT-1 inhibition has been demonstrated through reduction of plasma triglyceride levels in rodents at doses of ≥0.1 mg/kg following a lipid challenge.
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