A922500|959122-11-3|(DGAT-1 Inhibitor 4a)-陌孚医药/Medlife

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A922500 (Synonyms: DGAT-1 Inhibitor 4a)

目录号: PC12526 纯度: ≥98%

CAS No. :959122-11-3

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中文名称

A922500

中文别名

(1R,2R)-2-[[4'-[[(苯基氨基)羰基]氨基][1,1'-联苯]-4-基]甲酰基]环戊烷羧酸;DGAT-1 抑制剂;(1R,2R)-2-[[4-[[(苯基氨基)羰基]氨基][1,1-联苯]-4-基]甲酰基]环戊烷羧酸;花旗松素.黄杉素.紫杉叶素

英文名称

A922500

英文别名

(1R,2R)-2-(4'-(3-Phenylureido)-[1,1'-biphenyl]-4-carbonyl)cyclopentanecarboxylic acid;Diacyl glycerolacyltransferase 1 inhibitor;DGAT-1 inhibitor;A922500;(1R,2R)-2-(4'-(3-phenylureido)biphenylcarbonyl)cyclopentanecarboxylic acid;(1R,2R)-2-[4-[4-(phenylcarbamoylamino)phenyl]benzoyl]cyclopentane-1-carboxylic acid;A-922500;A922500(DGAT-1inhibitor);Cyclopentanecarboxylic acid, 2-[[4'-[[(phenylamino)carbonyl]amino][1,1'-biphenyl]-4-yl]carbonyl]-, (1R,2R)-;DGAT-1 Inhibitor 4a;Urea-based Analogue,4a;(1R,2R)-2-[[4'-[[(Phenylamino)carbonyl]amino][1,1'-biphenyl]-4-yl]carbonyl]cyclopentanecarboxylic acid

Cas No.

959122-11-3

分子式

C₂₆H₂₄N₂O₄

分子量

428.48

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

A 922500 (DGAT-1 Inhibitor 4a) is a potent, selective, and orally bioavailable diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC₅₀s of 9 and 22 nM against human and mouse DGAT-1, respectively.

性状

Solid

IC50 & Target[1][2]

IC50: 9 nM (human DGAT-1), 22 nM (mouse DGAT-1)

体外研究(In Vitro)

A 922500 (A-922500) demonstrates excellent selectivity over other acyltransferases, including DGAT-2 (IC₅₀=53 μM) and the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 (IC₅₀=296 μM) .

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

体内研究(In Vivo)

DGAT-1 inhibitor A 922500 (A-922500) reduces serum triglyceride levels from baseline at all doses tested; however, this is only statistically significant at the 3 mg/kg dose, which lowers serum triglycerides by 53%. Similarly, the 3 mg/kg dose of A 922500 significantly reduces serum FFA concentrations by 55% and total cholesterol by 25%. DGAT-1 inhibition has no significant effect on body weight at any dose tested. Although A 922500 dpes not significantly affect LDL-cholesterol or HDL-cholesterol individually, the serum LDL/HDL-cholesterol ratio is significantly improved by A 922500 at 0.3 and 3 mg/kg. Similar to the dyslipidemic hamster, treatment with 3 mg/kg A 922500 significantly reduces serum triglyceride concentrations (39%). FFA levels significantly increase over the 14-day period in vehicle-treated animals. This increase is inhibited in a dose-dependent manner by A 922500 such that FFA concentrations are 32% lower after 14 days of treatment with the DGAT-1 inhibitor at 3 mg/kg, compared with the vehicle group (p < 0.05). HDL-cholesterol is significantly increased from baseline levels by A 922500 at 0.3 and 3 mg/kg; however, this is only significantly increased compared with vehicle at the 3 mg/kg dose. Body weight significantly increases over the 2-week period in vehicle-treated rats, and this is not affected by A 922500. LDL-cholesterol is significantly reduced in the vehicle treated group. DGAT-1 inhibition does not further reduce LDL-cholesterol and has no effect on total cholesterol.

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

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. King AJ, et al. Diacylglycerol acyltransferase 1 inhibition lowers serum triglycerides in the Zucker fatty rat and the hyperlipidemic hamster. J Pharmacol Exp Ther. 2009 Aug;330(2):526-31. [Information]

溶解度数据

体外研究:

DMSO : ≥ 50 mg/mL (116.69 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3338 mL	11.6692 mL	23.3383 mL
5 mM	0.4668 mL	2.3338 mL	4.6677 mL
10 mM	0.2334 mL	1.1669 mL	2.3338 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.83 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 ddH?O 中，得到澄清透明的生理盐水溶液

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产品使用指南

Data Sheet

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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