Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BMS-986278 是一种具有口服活性和高效性的血磷脂酸受体 1 (LPA1) 拮抗剂,对人和小鼠 LPA1 的 Kb 值分别为 6.9 nM 和 4.0 nM。BMS-986278 可用于研究用于特发性肺纤维化。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 5,820 | 现货 | ||
10 mg | ¥ 7,860 | 现货 | ||
25 mg | ¥ 11,600 | 现货 | ||
50 mg | ¥ 15,700 | 现货 | ||
100 mg | ¥ 21,200 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 5,690 | 现货 |
产品描述 | BMS-986278 is an orally active and potent hemophosphatidic acid receptor 1 (LPA1) antagonist with Kb values of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively.BMS-986278 may be investigated for use in idiopathic pulmonary fibrosis. |
体外活性 | With Kbs of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively, BMS-986278 is a high-affinity LPA1 antagonist. These values were determined in CHO cells overexpressing LPA1[1]. BMS-986278 also antagonizes Lysophosphatidic acid (LPA)-stimulated calcium flux in normal human lung fibroblasts, exhibiting a Kb of 5.8 nM[1]. |
体内活性 | In CD1 mice, a single oral administration of BMS-986278 (0.1-10 mg/kg) completely inhibits LPA-stimulated systemic histamine release in a concentration-dependent manner[1]. Furthermore, when administered orally twice daily for 14 days at doses ranging from 3 to 30 mg/kg, BMS-986278 reduces Bleomycin-induced collagen deposition and lung fibrosis in rats[1]. |
分子量 | 445.51 |
分子式 | C22H31N5O5 |
CAS No. | 2170126-74-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 90 mg/mL (202.02 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2446 mL | 11.2231 mL | 22.4462 mL | 56.1155 mL |
5 mM | 0.4489 mL | 2.2446 mL | 4.4892 mL | 11.2231 mL | |
10 mM | 0.2245 mL | 1.1223 mL | 2.2446 mL | 5.6115 mL | |
20 mM | 0.1122 mL | 0.5612 mL | 1.1223 mL | 2.8058 mL | |
50 mM | 0.0449 mL | 0.2245 mL | 0.4489 mL | 1.1223 mL | |
100 mM | 0.0224 mL | 0.1122 mL | 0.2245 mL | 0.5612 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
BMS-986278 2170126-74-4 GPCR/G Protein LPA Receptor BMS986278 BMS 986278 Inhibitor inhibitor inhibit