BMS-986278
Based on 1 publication(s) in Google Scholar
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.
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- Purity: 99.93%
- CAS No.: 2170126-74-4
- 화학식: C22H31N5O5
- 분자량:445.51
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Publications Citing Use of MedChemExpress (MCE) BMS-986278
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Biological Activity
Kb: 6.9 nM (human LPA1), 4.0 nM (mouse LPA1)[1]
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.
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.
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Animal Model:Male Sprague-Dawley rats (10 weeks) were administered Bleomycin[1]
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Dosage:3, 10, and 30 mg/kg
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Administration:P.o. twice daily for 14 days
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2170126-74-4
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Appearance Solid
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분자량 445.51
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화학식 C22H31N5O5
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Color White to light yellow
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SMILES
CCCN(C)C(OCC1=C(N=NN1C)C(C=C2)=NC(C)=C2O[C@H]3CCC[C@H](C(O)=O)C3)=O
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Synonyms
Admilparant
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Pediatr Res
Bronchopulmonary dysplasia demonstrates dysregulated autotaxin/lysophosphatidic acid signaling in a neonatal mouse model. [Abstract]2025 Jun;97(7):2462-2474. PMID: 39415037
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.
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 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.
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.
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.
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.
순도&문서
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Data Sheet (291 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
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Handling Instructions (2659 KB)
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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