BMS-986020
产品说明书
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同义名 : | AM152; AM-000152; AP-3152 free acid |
| CAS号 : | 1257213-50-5 | |
| 货号 : | A748322 | |
| 分子式 : | C29H26N2O5 | |
| 纯度 : | 99%+ | |
| 分子量 : | 482.53 | |
| MDL号 : | MFCD30489743 | |
| 存储条件： |
Pure form Sealed in dry,2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Idiopathic pulmonary fibrosis (IPF) causes irreversible loss of lung function. The lysophosphatidic acid receptor 1 (LPA1) pathway is implicated in IPF etiology. BMS-986020 is a high-affinity LPA1 antagonist under assessment in a phase 2 study in patients with IPF[2]. A BMS-986020 concentration-dependent displacement of [18F]BMT-083133 binding was observed in LPA1+ cells and lung sections. At 0.1 nM of BMS-986020, the percent displacement in healthy mice, bleomycin mice, and IPF lungs was 18%, 24%, and 31%, respectively; and at 10 nM, the percent displacement was 73%, 76%, and 64%, respectively[3]. Patients treated with BMS-986020 (600 mg for 26 weeks) experienced a significantly slower rate of decline in FVC vs placebo. Dose-related elevations in hepatic enzymes were observed in both BMS-986020 treatment groups[2]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.07mL 0.41mL 0.21mL |
10.36mL 2.07mL 1.04mL |
20.72mL 4.14mL 2.07mL |
| 参考文献 |
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