DGAT1-IN-3|cas:939375-07-2|西域试剂

DGAT1-IN-3,99.86%

产品编号：Bellancom-16434| CAS NO：939375-07-2| 分子式：C₂₀H₁₉F₃N₄O₃| 分子量：420.39

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-16434	￥4200.00	杭州北京（现货）
Bellancom-16434	￥7000.00	杭州北京（现货）
Bellancom-16434	￥19000.00	杭州北京（现货）
Bellancom-16434	￥30000.00	杭州北京（现货）

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DGAT1-IN-3

产品介绍

DGAT1-IN-3 是一种有效的，选择性的，具有口服活性的 DGAT-1 抑制剂，抑制人类和大鼠 DGAT-1 的 IC₅₀ 值分别为 38 nM 和 120 nM。DGAT1-IN-3 可用于研究肥胖，血脂异常和代谢综合征。

生物活性

DGAT1-IN-3 is a potent, selective and orally bioavailable inhibitor of DGAT-1, with IC₅₀s of 38 nM for human DGAT-1 and 120 nM for rat DGAT-1. DGAT1-IN-3 could be used to research of obesity, dyslipidemia, and metabolic syndrome.

体外研究

DGAT1-IN-3 blocks the human ether-a-go-go-related gene (hERG) encoded potassium channel with an IC₂₀ of 0.2 μM.
DGAT1-IN-3 inhibits human DGAT-1 in CHOK1 cells with an EC₅₀ of 0.66 μM.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

DGAT1-IN-3 (5-50 mg/kg; p.o once daily for three weeks) reduces weight gain and plasma triglycerides, and improves lipid profile.
DGAT1-IN-3 (50 mg/kg; p.o) exhibits good oral bioavailability (77%) and the maximum exposure level in plasma (C_max) is 24 μM.
DGAT1-IN-3 (5 mg/kg; i.v) exhibits terminal elimination half-lives (1.95 h) and low clearance (13.5 mL/min/kg).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Three-month-old male Sprague Dawley DIO rats (fed with a high-fat diet)
Dosage:	0, 5, 25, 50 mg/kg; once daily for three weeks
Administration:	P.o. administration
Result:	Reduced cumulative body weight gain in a dose-dependent manner and was well tolerated in rats.

Animal Model:	Male Wistar rats
Dosage:	50 mg/kg for p.o. and 5 mg/kg for i.v. (Pharmacokinetic Analysis)
Administration:	P.o. and i.v. administration
Result:	C_max (24 μM); T_1/2 (1.95 h).

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Three-month-old male Sprague Dawley DIO rats (fed with a high-fat diet)
Dosage:	0, 5, 25, 50 mg/kg; once daily for three weeks
Administration:	P.o. administration
Result:	Reduced cumulative body weight gain in a dose-dependent manner and was well tolerated in rats.

Animal Model:	Male Wistar rats
Dosage:	50 mg/kg for p.o. and 5 mg/kg for i.v. (Pharmacokinetic Analysis)
Administration:	P.o. and i.v. administration
Result:	C_max (24 μM); T_1/2 (1.95 h).

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (237.87 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3787 mL	11.8937 mL	23.7874 mL
5 mM	0.4757 mL	2.3787 mL	4.7575 mL
10 mM	0.2379 mL	1.1894 mL	2.3787 mL

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, 6 months; -20°C, 1 month (protect from light)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.95 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液