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Purity: ≥98%
BMS-986020 (also known as AM152 and AP-3152 free acid) is a novel, potent and selective LPA1 (lysophosphatidic acid) antagonist. For the treatment of idiopathic pulmonary fibrosis, BMS-986020 is currently undergoing a Phase 2 clinical trial. BMS-986020 specifically inhibits the LPA receptor, which is involved in the binding of the signaling molecule lysophosphatidic acid. This molecule is involved in a complex range of biological functions, including the invasion of tumor cells, smooth muscle contraction, platelet aggregation, cell proliferation, and chemotaxis.
| Targets |
BSEP ( IC50 = 4.8 μM ); MRP4 ( IC50 = 6.2 μM ); MDR3 ( IC50 = 7.5 μM ); LPA1
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| ln Vitro |
In the lungs of healthy mice, bleomycin-treated mice, and IPF mice, the percent displacement at 0.1 nM is 18%, 24%, and 31%, respectively. The percentages of displacement at 10 nM are 73%, 76%, and 64%, in that order. As a translational research tool, [18F]BMT-083133, a radioligand that targets LPA1, is designed to measure lung LPA1 engagement of BMS-986020 through in vitro autoradiography (ARG)[4].
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| Cell Assay |
Dulbecco's Modified Eagle Medium (DMEM) + GlutaMax supplemented with 0.4% fetal bovine serum, 37.5 mg/mL Ficoll 70, 25 mg/mL Ficoll 400, and 1% ascorbic acid was used to cultivate human lung fibroblasts in 48-well plates. The cells were stimulated in four replicates with either 1 ng/mL of transforming growth factor beta 1 (TGF-β1) or 20 µM LPA with or without BMS-986020 (0.01, 0.05, 0.1, 0.5, 1, or 5 µM) diluted in dimethyl sulfoxide (DMSO) or vehicle (0.05% DMSO). For twelve days, cells were grown at 37 °C in a 95% O2 and 5% CO2 environment. On days four and eight, the culture media were replaced. Until the biomarker measurements, supernatants were kept at −20 °C in storage. On Day 0 (before starting medication treatment) and Day 12, alamarBlue was utilized to measure cellular metabolism. Lactate dehydrogenase (LDH) release was measured on Days 4, 8, and 12.
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| References |
| Molecular Formula |
C29H26N2O5
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|---|---|
| Molecular Weight |
482.5271
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| Exact Mass |
482.18
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| Elemental Analysis |
C, 72.19; H, 5.43; N, 5.81; O, 16.58
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| CAS # |
1257213-50-5
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| Related CAS # |
BMS-986020 sodium; 1380650-53-2
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| Appearance |
Solid powder
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| SMILES |
CC1=NOC(=C1NC(=O)O[C@H](C)C2=CC=CC=C2)C3=CC=C(C=C3)C4=CC=C(C=C4)C5(CC5)C(=O)O
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| InChi Key |
GQBRZBHEPUQRPL-LJQANCHMSA-N
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| InChi Code |
InChI=1S/C29H26N2O5/c1-18-25(30-28(34)35-19(2)20-6-4-3-5-7-20)26(36-31-18)23-10-8-21(9-11-23)22-12-14-24(15-13-22)29(16-17-29)27(32)33/h3-15,19H,16-17H2,1-2H3,(H,30,34)(H,32,33)/t19-/m1/s1
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| Chemical Name |
1-[4-[4-[3-methyl-4-[[(1R)-1-phenylethoxy]carbonylamino]-1,2-oxazol-5-yl]phenyl]phenyl]cyclopropane-1-carboxylic acid
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| Synonyms |
AM152; AM 152; AM-152; AP-3152 free acid; BMS-986020; BMS986020; BMS 986020
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 97~125 mg/mL (201.0~259.1 mM)
Ethanol: ~97 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.31 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.31 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0724 mL | 10.3621 mL | 20.7241 mL | |
| 5 mM | 0.4145 mL | 2.0724 mL | 4.1448 mL | |
| 10 mM | 0.2072 mL | 1.0362 mL | 2.0724 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02068053 | Completed | Drug: [14C] BMS-986020 | Immunosuppression For Disease | Bristol-Myers Squibb | March 2014 | Phase 1 |
| NCT02017730 | Completed | Drug: BMS-986020 Drug: [11C]BMT-136088 |
Immunology | Bristol-Myers Squibb | January 2014 | Phase 1 |
| NCT02227173 | Completed | Drug: BMS-986020 Drug: Montelukast |
Drug-drug Interaction Study | Bristol-Myers Squibb | September 2014 | Phase 1 |
| NCT01766817 | Completed | Drug: BMS-986020 Drug: Placebo matching with BMS-986020 |
Idiopathic Pulmonary Fibrosis | Bristol-Myers Squibb | January 31, 2013 | Phase 2 |
| NCT02101125 | Completed | Drug: BMS-986020 Drug: Rosuvastatin |
Immunosuppression For Disease | Bristol-Myers Squibb | March 2014 | Phase 1 |
 Chronology of the LP field, LP and other lipid receptors, and overview of proximal LP signaling features.Exp Cell Res.2015 May 1;333(2):171-7. |
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 Disease mechanisms being accessed by LP-based drug discovery and compounds in clinical development.Exp Cell Res.2015 May 1;333(2):171-7. |
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