MGAT2-IN-1

目录号: GC31362纯度: >99.00%同义词: MGAT2-IN-1
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2.4nM。

MGAT2-IN-1
Cas No.: 1800025-30-2
规格价格库存数量操作
1mg¥1,339.00现货
1
5mg¥4,016.00现货
1
10mg¥6,694.00现货
1
25mg¥13,388.00现货
1
50mg¥19,635.00现货
1
100mg¥31,238.00现货
1
10mM (in 1mL DMSO)¥5,779.00现货
1

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产品描述 Description

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.

MGAT2-IN-1 (3, 10 mg/kg, p.o.) dose-dependently suppresses plasma TG elevation, and plasma CM/TG AUC in mice. MGAT2-IN-1 does not decrease MG absorption but inhibits MGAT2-dependent TG/DG resynthesis. In the lipid utilization analysis, MGAT2-IN-1 significantly increases free fatty acid (FFA) and acylcarnitine levels. MGAT2-IN-1 (30 mg/kg) also significantly reduces food intake dose dependently, suppresses BW gains. MGAT2-IN-1 shows anti-diabetic effects in mice[1].

[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.

实验参考方法 Experimental Reference Method

Animal experiment:

Mice: Overnight-fasted mice undergo MTT in the morning. First, they are orally administered vehicle (0.5% methylcellulose solution) or MGAT2-IN-1 suspended in 0.5% methylcellulose. Six or 16 h after dosing, they are intraperitoneally injected 500 mg/kg Pluronic F-127 to inhibit plasma TG hydrolysis by lipoprotein lipase (LPL). Thirty minutes after injection, the mice are given an oral liquid meal (10 mL/kg) comprising an admixture of corn oil and Ensure-H (3:17 v/v). Blood samples are collected at 0, 2 and 4 h after oral gavage of the liquid meal. Area under the curve (AUC) of chylomicron TG (CM/TG), which is synthesised from dietary fat in the small intestine, is calculated by subtracting plasma TG levels of a liquid meal-untreated group from plasma TG levels of each treated group.

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.

产品文档 Product Documents

Purity:>99.00%

化学性质Chemical Properties

CAS 号
1800025-30-2
同义词
MGAT2-IN-1
SMILES
O=S(C1=CC2=C(N(C3=NC=C(C4=CC(C(F)(F)F)=NN4C)C=N3)CC2)C(N5C(CCC5)=O)=C1)(NC6=C(F)C=C(Cl)C=C6F)=O
分子式
C27H21ClF5N7O3S
分子量
654.01 g/mol
溶解性
DMSO : ≥ 125 mg/mL (191.13 mM)
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol