943962-47-8
中文名稱
BMS303141
英文名稱
BMS 303141
CAS
943962-47-8
分子式
C19H15Cl2NO4S
分子量
424.3
MOL 文件
943962-47-8.mol
更新日期
2024/12/24 22:26:49
943962-47-8 結(jié)構(gòu)式
基本信息
中文別名
3,5-二氯-2-羥基-N-(4-甲氧基[1,1'-聯(lián)苯]-3-基)苯磺酰胺 英文別名
CS-887BMS30314
BMS 303141
BMS 303141, >=98%
BMS303141
BMS 303141
BMS-303141 >=98% (HPLC)
3,5-dichloro-2-hydroxy-N-(4-Methoxybiphenyl-3-yl)benzenesulfonaMide
3,5-dichloro-2-hydroxy-N-(2-methoxy-5-phenylphenyl)benzenesulfonamide
3,5-Dichloro-2-hydroxy-N-(4-methoxy[1,1'-biphenyl]-3-yl)benzenesulfonamide
Benzenesulfonamide, 3,5-dichloro-2-hydroxy-N-(4-methoxy[1,1'-biphenyl]-3-yl)-
所屬類別
生物化工：激動劑抑制劑物理化學性質(zhì)
沸點591.5±60.0 °C(Predicted)
密度1.462±0.06 g/cm3(Predicted)
儲存條件2-8°C
溶解度在DMSO中的溶解度為20mg/mL，澄清
酸度系數(shù)(pKa)4.94±0.48(Predicted)
形態(tài)粉末
顏色白色至米色
穩(wěn)定性可在-20°C下的DMSO或乙醇溶液保存長達3個月。
常見問題列表
生物活性
BMS-303141 是一種有效的細胞滲透性的 ATP-citrate lyase (ACL) 抑制劑，其IC50值為0.13 μM。BMS-303141 可在HepG2細胞中抑制總脂質(zhì)合成，其IC50值為8 μM。靶點
| Target | Value |
|
ACL
(Cell-free assay) | 0.13 μM |
體外研究
In HepG2 cells, BMS-303141 shows inhibition of total lipid syntheses with an IC 50 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.
體內(nèi)研究
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.