BMS-986020 (AM152) 是一种高亲和力和选择性溶血磷脂酸受体 1 (LPA1) 拮抗剂。
| Cas No. | 1257213-50-5 |
| 别名 | AM152 |
| Canonical SMILES | O=C(C1(C2=CC=C(C3=CC=C(C4=C(NC(O[C@@H](C5=CC=CC=C5)C)=O)C(C)=NO4)C=C3)C=C2)CC1)O |
| 分子式 | C29H26N2O5 |
| 分子量 | 482.53 |
| 溶解度 | DMSO : ≥ 64 mg/mL (132.63 mM) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | BMS-986020 is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist[1]. BMS-986020 inhibits bile acid and phospholipid transporters with IC50s of 4.8 μM, 6.2 μM, and 7.5 μM for BSEP, MRP4, and MDR3, respectively[2]. BMS-986020 is used for the treatment of idiopathic pulmonary fibrosis (IPF) [3]. References:
[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. |
