ABT-046|cas:1031336-60-3|西域试剂

ABT-046,98.13%

产品编号：Bellancom-15197| CAS NO：1031336-60-3| 分子式：C₂₀H₂₂N₄O₂| 分子量：350.41

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货号	价格	库存与货期
Bellancom-15197	￥2455.00	杭州北京（现货）
Bellancom-15197	￥4297.00	杭州北京（现货）
Bellancom-15197	￥15345.00	杭州北京（现货）
Bellancom-15197	￥22506.00	杭州北京（现货）

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ABT-046

产品介绍

ABT-046 是一种具有口服活性的选择性二酰基甘油酰基转移酶 1 (DGAT-1) 抑制剂，对人和小鼠 DGAT-1 的 IC₅₀ 均为 8 nM。

生物活性

ABT-046 is a potent, selective, and orally active acyl CoA:diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC₅₀s of both 8 nM against human and mouse DGAT-1.

体外研究

ABT-046 shows no inhibition against human DGAT-2 and inhibits triglyceride formation in HeLa cells expressing human DGAT-1 with an IC₅₀ of 78 nM.
ABT-046 exhibits high in vitro permeability values in Caco-2 cells with no evidence of active efflux (efflux ratio = 1.4 and 1.1 at 0.5 and 5 μM, respectively).
ABT-046 demonstrates negligible turnover in microsome preparations from mouse and human livers.

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

体内研究

ABT-046 (0.03-3 mg/kg; i.g.; once) significantly reduced postprandial triglycerides in CD-1 mice.
ABT-046 (0.3 mg/kg; i.g.; once) abolishes the postprandial triglyceride excursion in diet-induced obesity mice.

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

Animal Model:	Male CD-1 mice, postprandial hyperlipidemia model
Dosage:	0.03, 0.3, or 3 mg/kg
Administration:	Oral gavage, single dose
Result:	Showed a dose-dependent reduction in serum triglycerides starting at 0.03 mg/kg and increasing through the higher doses (40, 60, and 90% reduction from vehicle at 0.03, 0.3, and 3.0 mg/kg, respectively). The ascending pharmacodynamics correlated well with a linear increase in plasma exposure going from 0.03 to 3 mg/kg (C_2h = 0.033, 0.36, and 3.10 μg/mL at 0.03, 0.3, and 3.0 mg/kg, respectively).

Animal Model:	Male C57BL/6J diet-induced obesity (DIO) mice
Dosage:	0.3 mg/kg
Administration:	Oral gavage, single dose
Result:	Afforded a sustained reduction in serum triglyceride concentrations throughout the experiment.

Animal Model:

CD-1 mice and Sprague-Dawley rats

Dosage:

10 mg/kg or 5 mg/kg

Administration:

Intravenous injection or oral gavage (Pharmacokinetic Analysis)

Result:

Selected Pharmacokinetic Properties of ABT-046^a

	mouse (10 mg/kg)	rat (5 mg/kg)
	iv^b
T_1/2 (h)	4.6	3.8
V_ss (L/kg)	0.3	0.3
Clp (L/h/kg)	0.1	0.05
	po^b
T_1/2 (h)	5.1	5.6
C_max (μg/mL)	17.4	9.3
AUC (μg h/mL)	151	130
F (%)	78	91

^a All values are mean values ± SEMs (n = 3 unless specified otherwise).
^b 1% Tween-80 in water.

体内研究

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

Animal Model:	Male CD-1 mice, postprandial hyperlipidemia model
Dosage:	0.03, 0.3, or 3 mg/kg
Administration:	Oral gavage, single dose
Result:	Showed a dose-dependent reduction in serum triglycerides starting at 0.03 mg/kg and increasing through the higher doses (40, 60, and 90% reduction from vehicle at 0.03, 0.3, and 3.0 mg/kg, respectively). The ascending pharmacodynamics correlated well with a linear increase in plasma exposure going from 0.03 to 3 mg/kg (C_2h = 0.033, 0.36, and 3.10 μg/mL at 0.03, 0.3, and 3.0 mg/kg, respectively).

Animal Model:	Male C57BL/6J diet-induced obesity (DIO) mice
Dosage:	0.3 mg/kg
Administration:	Oral gavage, single dose
Result:	Afforded a sustained reduction in serum triglyceride concentrations throughout the experiment.

Animal Model:

CD-1 mice and Sprague-Dawley rats

Dosage:

10 mg/kg or 5 mg/kg

Administration:

Intravenous injection or oral gavage (Pharmacokinetic Analysis)

Result:

Selected Pharmacokinetic Properties of ABT-046^a

	mouse (10 mg/kg)	rat (5 mg/kg)
	iv^b
T_1/2 (h)	4.6	3.8
V_ss (L/kg)	0.3	0.3
Clp (L/h/kg)	0.1	0.05
	po^b
T_1/2 (h)	5.1	5.6
C_max (μg/mL)	17.4	9.3
AUC (μg h/mL)	151	130
F (%)	78	91

^a All values are mean values ± SEMs (n = 3 unless specified otherwise).
^b 1% Tween-80 in water.

性状

Solid

溶解性数据

In Vitro:

DMSO : 66.67 mg/mL (190.26 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8538 mL	14.2690 mL	28.5380 mL
5 mM	0.5708 mL	2.8538 mL	5.7076 mL
10 mM	0.2854 mL	1.4269 mL	2.8538 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。-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 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.67 mg/mL (4.77 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (4.77 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1.67 mg/mL (4.77 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (4.77 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。