TP-020 (Synonyms: MGAT2-IN-1)
目录号: PL14726 纯度: ≥98%
CAS No. :1800025-30-2
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中文名称
TP-020
英文名称
TP-020
英文别名
MGAT2-IN-1;N-(4-Chloro-2,6-difluorophenyl)-1-[5-[1-methyl-3-(trifluoromethyl)-1H-pyrazole-5-yl]-2-pyrimidinyl]-7-(2-oxopyrrolizino)indoline-5-sulfonamide;N-(4-chloro-2,6-difluorophenyl)-1-[5-[2-methyl-5-(trifluoromethyl)pyrazol-3-yl]pyrimidin-2-yl]-7-(2-oxopyrrolidin-1-yl)-2,3-dihydroindole-5-sulfonamide;TP-020
Cas No.
1800025-30-2
分子式
C27H21ClF5N7O3S
分子量
654.01
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
TP-020 (MGAT2-IN-1) 是一种可口服的单酰甘油酰基转移酶 (MGAT2) 抑制剂,对人和小鼠 MGAT2 的 IC50 值分别为 7.8 和 2.4 nM。
生物活性
TP-020 (MGAT2-IN-1) is an orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC 50 of 7.8 and 2.4 nM for human and mouse MGAT2, respectively.
性状
Solid
IC50 & Target[1][2]
IC50: 7.8 nM (Human MGAT2), 2.4 nM (Mouse MGAT2)
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : ≥ 125 mg/mL (191.13 mM)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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