AZD 3988 is a potent and selective diacylglycerol acyltransferase (DGAT-1) inhibitor (IC50 = 0.6 nM). Exhibits selectivity for DGAT-1 over DGAT-2, Kv11.1 (hERG) and cytochrome P450 enzymes. Suppresses triacylglyceride (TAG) plasma excursion and adipose tissue TAG synthesis in rats. Reduces body weight of diet-induced obese rats. Cell permeable and orally bioavailable.
| Molecular Weight | 456.44 |
| Formula | C23H22F2N4O4 |
| CAS Number | 892489-52-0 |
| Solubility (25°C) | 1eq. NaOH 4.56 mg/mL (with gentle warming) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related DGAT Products |
|---|
| PF-07202954
PF-07202954 is an orally active, weakly basic DGAT2 inhibitor with an IC50 of 10 nM for human DGAT2.PF-07202954 reduces hepatic triglycerides in an obese rat model. |
| ION224
ION224 is an antisense compound that targets DGAT-2 for studies related to non-alcoholic steatohepatitis (NASH). |
| PF-07055341
PF-07055341 is a DGAT1/2 inhibitor that can be used in studies related to non-alcoholic steatohepatitis (NASH). |
| Ervogastat
Ervogastat is a DGAT2 inhibitor that can be used in studies related to non-alcoholic steatohepatitis (NASH). |
| Pradigastat
Pradigastat (LCQ-908) is a potent, selective and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor. Pradigastat has anti-obesity and anti-diabetic effects. |
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