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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.93%
- CAS 番号: 2170126-74-4
- 分子式: C22H31N5O5
- 分子量:445.51
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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生物活性
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溶剤 & 溶解度
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 BMS-986278
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生物活性
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 |
化学情報
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CAS 番号 2170126-74-4
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性状 Solid
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分子量 445.51
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分子式 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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別名
Admilparant
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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.
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
純度とドキュメンテーション
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取扱説明書 (2659 KB)
参考文献
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 |
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| 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 |
BMS-986278 関連分類
HY-139853 関連分類
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