BMS-303141ATP-citrate lyase inhibitor,potent CAS# 943962-47-8 |
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Quality Control & MSDS
3D structure
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| Cas No. | 943962-47-8 | SDF | Download SDF |
| PubChem ID | 16747776 | Appearance | Powder |
| Formula | C19H15Cl2NO4S | M.Wt | 424.3 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 25 mg/mL (58.92 mM; Need ultrasonic) | ||
| Chemical Name | 3,5-dichloro-2-hydroxy-N-(2-methoxy-5-phenylphenyl)benzenesulfonamide | ||
| SMILES | COC1=C(C=C(C=C1)C2=CC=CC=C2)NS(=O)(=O)C3=CC(=CC(=C3O)Cl)Cl | ||
| Standard InChIKey | SIIPNDKXZOTLEA-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C19H15Cl2NO4S/c1-26-17-8-7-13(12-5-3-2-4-6-12)9-16(17)22-27(24,25)18-11-14(20)10-15(21)19(18)23/h2-11,22-23H,1H3 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | ATP citrate lyase (ACL) inhibitor (IC50 = 0.13 μM for human recombinant ACL); blocks lipid synthesis (IC50 = 8 μM in HepG2 cells). Displays no cytotoxicity up to a concentration of 50 μM. Lowers plasma glucose and triglycerides in a mouse model of hyperlipidemia. Orally bioavailable. |
BMS-303141 Dilution Calculator
BMS-303141 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.3568 mL | 11.7841 mL | 23.5682 mL | 47.1365 mL | 58.9206 mL |
| 5 mM | 0.4714 mL | 2.3568 mL | 4.7136 mL | 9.4273 mL | 11.7841 mL |
| 10 mM | 0.2357 mL | 1.1784 mL | 2.3568 mL | 4.7136 mL | 5.8921 mL |
| 50 mM | 0.0471 mL | 0.2357 mL | 0.4714 mL | 0.9427 mL | 1.1784 mL |
| 100 mM | 0.0236 mL | 0.1178 mL | 0.2357 mL | 0.4714 mL | 0.5892 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
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A novel direct homogeneous assay for ATP citrate lyase.[Pubmed:19286649]
J Lipid Res. 2009 Oct;50(10):2131-5.
ATP citrate lyase (ACL) is a cytosolic enzyme that catalyzes the synthesis of acetyl-CoA and oxaloacetate using citrate, CoA, and ATP as substrates and Mg(2+) as a necessary cofactor. The ACL-dependent synthesis of acetyl-CoA is thought to be an essential step for the de novo synthesis of fatty acids and cholesterol. For this reason, inhibition of ACL has been pursued as a strategy to treat dyslipidemia and obesity. Traditionally, ACL enzyme activity is measured indirectly by coupling to enzymes such as malate dehydrogenase or chloramphenicol acetyl transferase. In this report, however, we describe a novel procedure to directly measure ACL enzyme activity. We first identified a convenient method to specifically detect [(14)C]acetyl-CoA without detecting [(14)C]citrate by MicroScint-O. Using this detection system, we devised a simple, direct, and homogeneous ACL assay in 384-well plate format that is suitable for high-throughput screening. The current assay consists of 1) incubation of ACL enzyme with [(14)C]citrate and other substrates/cofactors CoA, ATP, and Mg(2+), 2) EDTA quench, 3) addition of MicroScint-O, the agent that specifically detects product [(14)C]acetyl-CoA, and 4) detection of signal by TopCount. This unique ACL assay may provide more efficient identification of new ACL inhibitors and allow detailed mechanistic characterization of ACL/inhibitor interactions.
2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors.[Pubmed:17383874]
Bioorg Med Chem Lett. 2007 Jun 1;17(11):3208-11.
A novel series of 2-hydroxy-N-arylbenzenesulfonamides were identified to be ATP-citrate lyase (ACL) inhibitors with compound 9 displaying potent in vitro activity (IC(50)=0.13 microM). Chronic oral dosing of compound 9 in high-fat fed mice lowered plasma cholesterol, triglyceride, and glucose, as well as inhibited weight gain.
