| BMS-303141ATP-citrate lyase inhibitor,potent |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
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- Purity = 99.51%
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Chemical structure
| 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. | |
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| Cas No. | 943962-47-8 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | 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 | ||
| Formula | C19H15Cl2NO4S | M.Wt | 424.3 |
| Solubility | ≥21.2mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| 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. | ||
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.
