| 产品描述: | LPA 受体拮抗剂;LPA Receptor Antagonists;;InformationBMS-986020 BMS-986020 (AM152, AP-3152 free acid) is a potent and selective antagonist of lysophosphatidic acid receptor 1 (LPA1) . BMS-986020 inhibits bile acid and phospholipid transporters with IC50 of 4.8 μM, 6.2 μM, and 7.5 μM for BSEP, MRP4, and MDR3, respectively. BMS-986020 has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).TargetsLPA1 ; BSEP (Cell-free assay); MRP4 (Cell-free assay); MDR3 (Cell-free assay) ; 4.8 μM; 6.2 μM; 7.5 μM |
| 靶点: |
IC50: 4.8 µM (BSEP); 6.2 µM (MRP4); 7.5 µM (MDR3) |
| 参考文献: |
1. Kihara Y, et al. Lysophospholipid receptors in drug discovery. Exp Cell Res. 2015 May 1;333(2):171-7. 2. Glenn Rosen, et al. LPA1 antagonists BMS-986020 and BMS-986234 for idiopathic pulmonary fibrosis: Preclinical evaluation of hepatobiliary homeostasis. European Respiratory Journal.3. Palmer SM, et al. Randomized, Double-Blind, Placebo-Controlled, Phase 2 Trial of BMS-986020, a Lysophosphatidic Acid Receptor Antagonist for the Treatment of Idiopathic Pulmonary Fibrosis. Chest. 2018 Nov;154(5):1061-1069. 4. Adrienne Pena, et al. Autoradiographic evaluation of [18F]BMT-083133, a lysophosphatidic acid receptor 1 (LPA1) radioligand. The jornal of nuclear medicine. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.072 ml |
10.362 ml |
20.724 ml |
| 5 mM |
0.414 ml |
2.072 ml |
4.145 ml |
| 10 mM |
0.207 ml |
1.036 ml |
2.072 ml |
| 50 mM |
0.041 ml |
0.207 ml |
0.414 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |