BMS-303141 ≥98% (HPLC)
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| 包装规格: | 5mg 25mg 100mg in glass bottle |
| 溶解性: | 溶于DMSO(20mg/mL) |
| 产品描述: | 基本信息 产品编号: B10022 产品名称: BMS 303141 CAS: 943962-47-8 储存条件 粉末 2-8℃ 四年 分子式: C19H15Cl2NO4S 溶于液体 -80℃ 两年 分子量 424.30 -20℃ 一个月 化学名: 3,5-Dichloro-2-hydroxy-N-(4-methoxy[1,1′-biphenyl]-3-yl)-benzenesulfonamide Solubility (25°C): 体外: DMSO 85mg/mL(200.32mM) Ethanol Insoluble Water Insoluble 体内(现配现用): 1.请依序添加每种溶剂:10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility:2.5mg/mL(5.89mM);Suspended solution; Need ultrasonic 此⽅案可获得2.5mg/mL(5.89mM)的均匀悬浊液,悬浊液可⽤于⼝服和腹腔注射。以1mL⼯作液为例,取100μL25.0mg/mL的澄清DMSO储备液加到400μL PEG300中,混合均匀;向上述体系中加⼊50μL Tween-80,混合均匀;然后继续加⼊450μL⽣理盐⽔定容⾄1mL。 2.请依序添加每种溶剂:10% DMSO→90% (20% SBE-β-CD in saline) Solubility:2.5mg/mL(5.89mM);Suspended solution; Need ultrasonic 此⽅案可获得2.5mg/mL(5.89mM)的均匀悬浊液,悬浊液可⽤于⼝服和腹腔注射。以1mL⼯作液为例,取100μL25.0mg/mL的澄清DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶液中,混合均匀。 3.请依序添加每种溶剂:10% DMSO→90% corn oil Solubility:2.5mg/mL(5.89mM);Suspended solution; Need ultrasonic 此⽅案可获得2.5mg/mL(5.89mM)的均匀悬浊液,悬浊液可⽤于⼝服和腹腔注射。以1mL⼯作液为例,取100μL25.0mg/mL的澄清DMSO储备液加到900μL⽟⽶油中,混合均匀。 <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 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。 制备储备液 浓度 溶液体积 质量 1mg 5mg 10mg 1mM 2.3568mL 11.7841mL 23.5682mL 5mM 0.4714mL 2.3568mL 4.7136mL 10mM 0.2357mL 1.1784mL 2.3568mL 50mM 0.0471mL 0.2357mL 0.4714mL 生物活性 产品描述 一种强效的ATP柠檬酸裂合酶(ACL)抑制剂。 靶点 ACL (Cell-free assay) 0.13μM 体外研究 In HepG2 cells, BMS-303141 shows inhibition of total lipid syntheses with an IC50 of 8μM. 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 体内研究 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 推荐实验方法(仅供参考) Animal Administration Mice: Effect of BMS-303141 in high-fat fed mice is studied. There are a total of four groups in the study; mice on normal diet and high-fat diet controls, and two treated groups that are supplemented with BMS-303141 in their high-fat diet to an equivalent daily dose of 10 or 100 mg/kg. The study is continued for a total of 34 days. Food consumption and body weight gain are tracked along with weekly assessment of lipid and glucose plasma chemistries |
| 保存条件: | 2-8℃ |
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