A3051 是一种有效的和具有口服活性的CXXC5-DVL的抑制剂，IC50值为 63.06 nM。A3334 可用于研究高脂肪饮食 (HFD) 和蛋氨酸-胆碱缺乏饮食 (MCD) 诱导的疾病，例如肥胖，糖尿病和NASH。详细信息请参考专利文献 WO2020079569。
| 生物活性 | A3051 is a potent and orally active inhibtor ofCXXC5-DVLextracted from patent WO2020079569, has anIC50of 63.06 nM. A3334 can be used for the research of high fat diet (HFD)-induced and methionine-choline deficient diet (MCD)-induced phenotypes such as obesity, diabetes, and NASH[1]. |
| IC50& Target | IC50: 63.06 nM (CXXC5-DVL)[1] |
体外研究
(In Vitro) | A3334 (1-10 μM) efficiently inhibits the adipogenic differentiation of 3T3-L1 preadipocytes via the Wnt/β-eatenin signaling pathway[1].
A3334 (1-10 μM; 24 h) enhances the TOPFlash reporter activity in HEK293-TOP cells[1].
|
体内研究
(In Vivo) | A3334 (25 mg/kg; p.o. once daily for 16 weeks) has anti-obesity effects in the HFD mice, and has no effect on mice fed with normal diet[1].
A3334 (25 mg/kg; p.o. once daily for 5 days) significantly reduces fasting glucose and the levels of glucose tolerance (GTT) and insulin tolerance (ITT) in serum in mice[1].
A3334 (25 mg/kg; p.o. once daily for 3 weeks) significantly abolishes hepatosteatosis and the increased levels of alanine transaminase (ALT) and aspartatetransaminase (AST) in mice[1].
| Animal Model: | Male C57BL/6N mice (6-week-old) are fed on the high fat die (HFD) for 16 weeks[1] | | Dosage: | 25 mg/kg | | Administration: | P.o. daily for 16 weeks | | Result: | Not observed the HFD-induced body weight gain and abdominal obesity.
Reduced the level of triglyceride and total cholesterol and increased the level of HDL-cholesterol.
Suppressed the increase in adipocyte cell sizes and enhancement of inflammation. |
|
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 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 | | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
| 溶解性数据 | In Vitro: DMSO : 250 mg/mL(813.54 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.2541 mL | 16.2707 mL | 32.5415 mL | | 5 mM | 0.6508 mL | 3.2541 mL | 6.5083 mL | | 10 mM | 0.3254 mL | 1.6271 mL | 3.2541 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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: ≥ 2.08 mg/mL (6.77 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.77 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 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。 *以上所有助溶剂都可在本网站选购。
|
m.cnreagent.com