BMS-986020 sodium
Based on 9 publication(s) in Google Scholar
BMS-986020 (AM152) sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 sodium 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. BMS-986020 sodium has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).
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- Pureza : 99.88%
- No. CAS: 1380650-53-2
- Fòrmula: C29H25N2NaO5
- Peso molecular:504.51
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) BMS-986020 sodium
More- Sci Adv. 2021 Sep 17;7(38):eabb5933. [Abstract]
- Cell Commun Signal. 2023 Sep 25;21(1):257. [Abstract]
- Cell Rep. 2019 Nov 12;29(7):1832-1847.e8. [Abstract]
- Cells. 2024 Jul 6;13(13):1152. [Abstract]
- Commun Biol. 2024 May 23;7(1):621. [Abstract]
- Carcinogenesis. 2021 Apr 30;42(4):611-620. [Abstract]
- J Appl Toxicol. 2024 Nov;44(11):1725-1741. [Abstract]
- J Pharmacol Sci. 2025 Jun;158(2):139-142. [Abstract]
- Seoul National University. 2024 Feb.
Actividad biológica
Descripciòn
IC50 & Target
IC50: 4.8 μM (BSEP); 6.2 μM (MRP4); 7.5 μM (MDR3)[2]
In Vitro
BMS-986020 sodium (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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1380650-53-2
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Appearance Solid
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Peso molecular 504.51
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Fòrmula C29H25N2NaO5
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Color White to yellow
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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[Na]
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Synonyms
AM152 sodium
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (9)
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Journal Impact Factor
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Most Recent
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Sci Adv
Targeting lysophospholipid acid receptor 1 and ROCK kinases promotes antiviral innate immunity. [Abstract]2021 Sep 17;7(38):eabb5933. PMID: 34533996 -
Cell Commun Signal
LPA1-mediated inhibition of CXCR4 attenuates CXCL12-induced signaling and cell migration. [Abstract]2023 Sep 25;21(1):257. PMID: 37749552 -
Cell Rep
Single-Cell Transcriptomics Uncovers Zonation of Function in the Mesenchyme during Liver Fibrosis. [Abstract]2019 Nov 12;29(7):1832-1847.e8. PMID: 31722201 -
Cells
2024 Jul 6;13(13):1152. PMID: 38995003 -
Commun Biol
2024 May 23;7(1):621. PMID: 38783088 -
Carcinogenesis
Lysophosphatidic acid mediated PI3K/Akt activation contributed to esophageal squamous cell cancer progression. [Abstract]2021 Apr 30;42(4):611-620. PMID: 33367557 -
J Appl Toxicol
Oleanolic acid induces hepatic injury by disrupting hepatocyte tight junction and dysregulation of farnesoid X receptor-mediated bile acid efflux transporters. [Abstract]2024 Nov;44(11):1725-1741. PMID: 39030772 -
J Pharmacol Sci
A novel lysophosphatidic acid receptor 1 antagonist with high brain penetrability has a curative effect in the empathic pain-related fibromyalgia model. [Abstract]2025 Jun;158(2):139-142. PMID: 40288824 -
Solvente y solubilidad
In Vitro:
DMSO : 150 mg/mL (297.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 7.5 mg/mL (14.87 mM); Clear solution
This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 7.5 mg/mL (14.87 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 7.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 25 mg/mL (49.55 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Kihara Y, et al. Lysophospholipid receptors in drug discovery. Exp Cell Res. 2015 May 1;333(2):171-7. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9821 mL | 9.9106 mL | 19.8212 mL | 49.5530 mL |
| 5 mM | 0.3964 mL | 1.9821 mL | 3.9642 mL | 9.9106 mL | |
| 10 mM | 0.1982 mL | 0.9911 mL | 1.9821 mL | 4.9553 mL | |
| 15 mM | 0.1321 mL | 0.6607 mL | 1.3214 mL | 3.3035 mL | |
| 20 mM | 0.0991 mL | 0.4955 mL | 0.9911 mL | 2.4777 mL | |
| 25 mM | 0.0793 mL | 0.3964 mL | 0.7928 mL | 1.9821 mL | |
| 30 mM | 0.0661 mL | 0.3304 mL | 0.6607 mL | 1.6518 mL | |
| 40 mM | 0.0496 mL | 0.2478 mL | 0.4955 mL | 1.2388 mL | |
| 50 mM | 0.0396 mL | 0.1982 mL | 0.3964 mL | 0.9911 mL | |
| 60 mM | 0.0330 mL | 0.1652 mL | 0.3304 mL | 0.8259 mL | |
| 80 mM | 0.0248 mL | 0.1239 mL | 0.2478 mL | 0.6194 mL | |
| 100 mM | 0.0198 mL | 0.0991 mL | 0.1982 mL | 0.4955 mL |
BMS-986020 sodium Related Classifications
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