Network Version
PF-04620110 Data Sheet
| Product Name: | PF-04620110 |
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| CAS No.: | 1109276-89-2 | |
| Cat. No.: | HY-13009 | |
| MWt: | 396.43966 | |
| Formula: | C21H24N4O4 | |
| Purity : | >98% | |
| Solubility: | DMSO : 12.5 mg/mL (ultrasonic) | |
| Mechanisms: | Target: Metabolic Disease | |
| Biological Activity: | ||
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PF-04620110 is a potent, selective and orally bioavailable diglyceride acyltransferase-1 (DGAT-1) inhibitor with an IC50 of 19 nM[1].
IC50 & Target: IC50: 19 nM (DGAT-1)[1]
In Vitro: PF-04620110 is orally bioavailable, has passive permeability(1x10-6 cm/s)[1]. PF-04620110 inhibits DGAT-1 with an IC50 of 19 nM, and inhibits triglyceride synthesis with an IC50 of 8 nM in HT-29 cells[2]. PF-04620110 is a highly selective inhibitor of DGAT-1 with >100-fold selectivity against a panel of lipid processing enzymes (human DGAT-2, several human acyl-CoA: cholesterol acyltransferase-1, wax alcohol acyltransferase-1/-2 and monacylglycerol acyltransferase-2/-3, and mouse MGAT-1)[2]. In Vivo: PF-04620110 (0.1-10 mg/kg; p.o.) reduces plasma triglyceride levels at doses of ≥0.1 mg/kg following a lipid challenge in rat[2]. |
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