| CAS NO: | 943962-47-8 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 2mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 424.3 |
|---|---|
| Formula | C19H15Cl2NO4S |
| CAS No. | 943962-47-8 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: ≥ 47 mg/mL |
| Water: <1 mg/mL | |
| Ethanol: N/A | |
| SMILES Code | O=S(C1=CC(Cl)=CC(Cl)=C1O)(NC2=CC(C3=CC=CC=C3)=CC=C2OC)=O |
| Synonyms | BMS-303141; BMS303141; BMS 303141 |
| In Vitro | In vitro activity: In HepG2 cells, BMS-303141 shows inhibition of total lipid syntheses with an IC50 of 8 μM. BMS-303141 shows no cytotoxicity up to 50 lM under a cell based Alamar Blue cytotoxicity assay, indicating the observed inhibition of lipid synthesis is not a result of compound-induced cytotoxicity. Kinase Assay: BMS-303141 is a potent, cell-permeable ATP-citrate lyase (ACL) inhibitor with an IC50 value of 0.13 μM. Cell Assay: In HepG2 cells, BMS-303141 shows inhibition of total lipid syntheses with an IC50 of 8 μM. BMS-303141 shows no cytotoxicity up to 50 lM under a cell based Alamar Blue cytotoxicity assay, indicating the observed inhibition of lipid synthesis is not a result of compound-induced cytotoxicity. |
|---|---|
| In Vivo | Chronic oral dosing of BMS-303141 in high-fat fed mice lowers approximate 20-30% plasma cholesterol and triglycerides, as well as 30-50% fasting plasma glucose. Chronic treatment with BMS-303141 shows a gradual inhibition of weight gain along with a reduction in adiposity without apparent changes in food intake. BMS-303141 shows an oral bioavailability of 55% but a relatively short half-life of 2.1 h. |
| Animal model | high-fat fed mice |
| Formulation & Dosage | 10 or 100 mg/kg; oral dose |
| References | Bioorg Med Chem Lett. 2007 Jun 1;17(11):3208-11. Epub 2007 Mar 12. |
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