MGAT2-IN-1
MGAT2-IN-1 Basic information
- Product Name:
- MGAT2-IN-1
- Synonyms:
-
- MGAT2-IN-1
- MGAT2 inhibitor 1
- 1H-Indole-5-sulfonamide, N-(4-chloro-2,6-difluorophenyl)-2,3-dihydro-1-[5-[1-methyl-3-(trifluoromethyl)-1H-pyrazol-5-yl]-2-pyrimidinyl]-7-(2-oxo-1-pyrrolidinyl)-
- MGAT2 IN 1,MGAT-2-IN-1,MGAT2IN1
- TP-020 (MGAT2-IN-1)
- TP-020
- CAS:
- 1800025-30-2
- MF:
- C27H21ClF5N7O3S
- MW:
- 654.01
- Mol File:
- 1800025-30-2.mol
MGAT2-IN-1 Chemical Properties
- Boiling point:
- 838.7±75.0 °C(Predicted)
- Density
- 1.66±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : ≥ 125 mg/mL (191.13 mM)
- form
- Solid
- pka
- 8.30±0.20(Predicted)
- color
- White to gray
MGAT2-IN-1 Usage And Synthesis
Uses
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.
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].
References
[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. DOI:10.1371/journal.pone.0150976
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