1. GPCR/G Protein
  2. LPL Receptor
  3. BMS-986278

BMS-986278 is a potent and orally active lysophosphatidic acid receptor 1 (LPA1) antagonist, with Kbs of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively. BMS-986278 can be used for the research of pulmonary fibrotic diseases.

For research use only. We do not sell to patients.

CAS No. : 2170126-74-4

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE BMS-986278

Histological Imaging/Staining
WB
Bio/Physico-chemical Assay

    BMS-986278 purchased from MedChemExpress. Usage Cited in: Pediatr Res. 2025 Jun;97(7):2462-2474.  [Abstract]

    BMS-986278 (10 mg/kg; ip; on alternate days, for a total of 14 days) protectd neonates from HYX-induced lung injury C57BL/6 neonatal mouse on PN 3.

    BMS-986278 purchased from MedChemExpress. Usage Cited in: Pediatr Res. 2025 Jun;97(7):2462-2474.  [Abstract]

    BMS-986278 (10 mg/kg; ip; on alternate days, for a total of 14 days) ameliorated HYX-induced expression of LOX in mouse lung tissue.

    BMS-986278 purchased from MedChemExpress. Usage Cited in: Pediatr Res. 2025 Jun;97(7):2462-2474.  [Abstract]

    BMS-986278 (10 mg/kg; ip; on alternate days, for a total of 14 days) mitigated HYX-induced LOX activity in the BALF of neonatal mouse pups.

    BMS-986278 purchased from MedChemExpress. Usage Cited in: Pediatr Res. 2025 Jun;97(7):2462-2474.  [Abstract]

    BMS-986278 (10 μM; 1+6 h; 1 hour prior to 6-hour exposure to Hyperoxia (HYX)) attenuated HYX-induced expression of COLI and LOX in HLF cells.

    BMS-986278 purchased from MedChemExpress. Usage Cited in: Pediatr Res. 2025 Jun;97(7):2462-2474.  [Abstract]

    BMS-986278 (10 μM; 1+6 h; 1 hour prior to 6-hour exposure to Hyperoxia (HYX)) attenuated HYX-induced p-AKT expression in HLF cells.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    BMS-986278 is a potent and orally active lysophosphatidic acid receptor 1 (LPA1) antagonist, with Kbs of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively. BMS-986278 can be used for the research of pulmonary fibrotic diseases[1].

    IC50 & Target

    Kb: 6.9 nM (human LPA1), 4.0 nM (mouse LPA1)[1]

    In Vitro

    BMS-986278 is a high-affinity LPA1 antagonist, with Kbs of 6.9 nM and 4.0 nM for human and mouse LPA1 in CHO cells overexpressing LPA1[1].
    BMS-986278 antagonizes Lysophosphatidic acid (LPA)-stimulated calcium flux in normal human lung fibroblasts, with a Kb of 5.8 nM[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    BMS-986278 (0.1-10 mg/kg; a single p.o.) completely inhibits LPA-stimulated systemic histamine release in a concentration-dependent manner in CD1 mice[1].
    BMS-986278 (3-30 mg/kg; p.o. twice daily for 14 d) decreases Bleomycin-induced collagen deposition/lung fibrosis in rats[1].

    Pharmacokinetics of BMS-986278 in preclinical species[1]

    plasma clearance ((mL/min)/kg) Vss (L/kg) oral bioavailability (%) T1/2 (h) plasma protein binding (% free)
    mouse 37 5.5 70 2.5 31.4
    rat 15 3.5 100 4.5 12.6
    monkey 2.0 1.6 79 11 0.8

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Male Sprague-Dawley rats (10 weeks) were administered Bleomycin[1]
    Dosage: 3, 10, and 30 mg/kg
    Administration: P.o. twice daily for 14 days
    Result: Resulted in significant decreases in the lung section percent fibrotic area for the 3 mg/kg (48%) and 10 mg/kg (56%) dose groups.
    Clinical Trial
    Molecular Weight

    445.51

    Formula

    C22H31N5O5

    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    CCCN(C)C(OCC1=C(N=NN1C)C(C=C2)=NC(C)=C2O[C@H]3CCC[C@H](C(O)=O)C3)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (224.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2446 mL 11.2231 mL 22.4462 mL
    5 mM 0.4489 mL 2.2446 mL 4.4892 mL
    View the 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

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    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation

    Purity: 99.95%

    References

    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. 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 2.2446 mL 11.2231 mL 22.4462 mL 56.1155 mL
    5 mM 0.4489 mL 2.2446 mL 4.4892 mL 11.2231 mL
    10 mM 0.2245 mL 1.1223 mL 2.2446 mL 5.6115 mL
    15 mM 0.1496 mL 0.7482 mL 1.4964 mL 3.7410 mL
    20 mM 0.1122 mL 0.5612 mL 1.1223 mL 2.8058 mL
    25 mM 0.0898 mL 0.4489 mL 0.8978 mL 2.2446 mL
    30 mM 0.0748 mL 0.3741 mL 0.7482 mL 1.8705 mL
    40 mM 0.0561 mL 0.2806 mL 0.5612 mL 1.4029 mL
    50 mM 0.0449 mL 0.2245 mL 0.4489 mL 1.1223 mL
    60 mM 0.0374 mL 0.1871 mL 0.3741 mL 0.9353 mL
    80 mM 0.0281 mL 0.1403 mL 0.2806 mL 0.7014 mL
    100 mM 0.0224 mL 0.1122 mL 0.2245 mL 0.5612 mL
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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
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    Cat. No.:
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