BMS-303141
目录号 : GC10884An ACL inhibitor
Cas No.:943962-47-8
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment [1]: | |
Cell lines |
HepG2 cells |
Preparation method |
The solubility of this compound in DMSO is > 21.2 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
Reacting condition |
8 μM; 6 hrs |
Applications |
In HepG2 cells, BMS-303141 inhibited total lipid synthesis with an IC50 value of 8 μM. Moreover, BMS-303141 showed no cytotoxicity up to 50 μM. |
Animal experiment [1]: | |
Animal models |
High-fat fed mice |
Dosage form |
10 and 100 mg/kg; p.o. |
Applications |
In high-fat fed mice, BMS-303141 modestly reduced both plasma cholesterol and triglyceride 20 days after treatment. In addition, fasting plasma glucose started to decrease from day 7 to completion of the study. |
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Li JJ, Wang H, Tino JA, et al. 2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors. Bioorg Med Chem Lett, 2007, 17(11): 3208-3211. |
BMS-303141 is a potent inhibitor of ATP-citrate lyase with IC50 value of 0.13 μM [1].
ATP-citrate lyase (ACL) is a cytosolic enzyme that responsible for the production of cytosolic acetyl-CoA, a precursor required for de novo biosyntheses of cholesterol and fatty acids. Inhibition of ACL is used to treat dyslipidemia and obesity [1].
BMS-303141 is a potent ATP-citrate lyase inhibitor. In HepG2 cells, BMS-303141 inhibited total lipid syntheses with IC50 value of 8 μM. Also, BMS-303141 showed no cytotoxicity up to 50 μM [1].
In mice, BMS-303141 exhibited an oral bioavailability of 55%. In high-fat fed mice, BMS-303141 reduced the levels of plasma triglyceride, cholesterol by 20-30% and glucose by 30-50% and inhibited weight gain [1]. BMS-303141 inhibited ACL with IC50 value of 0.94 μM for human ACL in a concentration dependant way [2].
References:
[1]. Li JJ, Wang H, Tino JA, et al. 2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors. Bioorg Med Chem Lett, 2007, 17(11): 3208-3211.
[2]. Ma Z, Chu CH, Cheng D. A novel direct homogeneous assay for ATP citrate lyase. J Lipid Res, 2009, 50(10): 2131-2135.
Cas No. | 943962-47-8 | SDF | |
化学名 | 3,5-dichloro-2-hydroxy-N-(4-methoxy-[1,1'-biphenyl]-3-yl)benzenesulfonamide | ||
Canonical SMILES | COC1=C(NS(C2=CC(Cl)=CC(Cl)=C2O)(=O)=O)C=C(C3=CC=CC=C3)C=C1 | ||
分子式 | C19H15Cl2NO4S | 分子量 | 424.3 |
溶解度 | ≥ 21.2mg/mL in DMSO | 储存条件 | 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℃,然后在超声波浴中震荡一段时间。 |
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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。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.3568 mL | 11.7841 mL | 23.5682 mL |
5 mM | 0.4714 mL | 2.3568 mL | 4.7136 mL |
10 mM | 0.2357 mL | 1.1784 mL | 2.3568 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。