| Bioactivity | TP-020 (MGAT2-IN-1) is an orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC50 of 7.8 and 2.4 nM for human and mouse MGAT2, respectively. | ||||||||||||
| Target | IC50: 7.8 nM (Human MGAT2), 2.4 nM (Mouse MGAT2) | ||||||||||||
| In Vivo | TP-020 (3, 10 mg/kg, p.o.) dose-dependently suppresses plasma TG elevation, and plasma CM/TG AUC in mice. TP-020 does not decrease MG absorption but inhibits MGAT2-dependent TG/DG resynthesis. In the lipid utilization analysis, TP-020 significantly increases free fatty acid (FFA) and acylcarnitine levels. TP-020 (30 mg/kg) also significantly reduces food intake dose dependently, suppresses BW gains. TP-020 shows anti-diabetic effects in mice[1]. | ||||||||||||
| Name | TP-020 | ||||||||||||
| CAS | 1800025-30-2 | ||||||||||||
| Formula | C27H21ClF5N7O3S | ||||||||||||
| Molar Mass | 654.01 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Take K, et al. Pharmacological Inhibition of Monoacylglycerol O-Acyltransferase 2 Improves Hyperlipidemia, Obesity, and Diabetes by Change in Intestinal Fat Utilization. PLoS One. 2016 Mar 3;11(3):e0150976. |
TP-020
CAS: 1800025-30-2 F: C27H21ClF5N7O3S W: 654.01
TP-020 (MGAT2-IN-1) is an orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC50 of 7.8 and 2.4 n
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