BMS-986020
CAS No. : 1257213-50-5
(Synonyms: AM152)
| Size | Price | Stock |
|---|---|---|
| 1mg | $60 | In-stock |
| 5mg | $95 | In-stock |
| 10mg | $150 | In-stock |
| 25mg | $300 | In-stock |
| 50mg | $450 | In-stock |
| 100mg | $660 | In-stock |
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| 500 mg | Get quote | |
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| Cat. No. : | HY-100619 |
| M.Wt: | 482.53 |
| Formula: | C29H26N2O5 |
| Purity: | >98 % |
| Solubility: | DMSO : 125 mg/mL (ultrasonic) |
BMS-986020 (AM152) is a high-affinity and selective 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 has the potential for the treatment of idiopathic pulmonary fibrosis (IPF)[3]. IC50 & Target:IC50: 4.8 µM (BSEP); 6.2 µM (MRP4); 7.5 µM (MDR3)[2] In Vitro:BMS-986020 (0.1-10 nM; pre-incubated) concentration-dependent displacement of [18F]BMT-083133 binding is observed in LPA1+ cells and lung sections.?At 0.1 nM, the percent displacement in healthy mice, bleomycin mice, and IPF lungs is 18%, 24%, and 31%, respectively. At 10 nM, the percent displacement is 73%, 76%, and 64%, respectively.[18F]BMT-083133, a radioligand targeting LPA1 is developed as a translational research tool for assessment of lung LPA1 engagement of BMS-986020 using in vitro autoradiography (ARG)[4].
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