Bexotegrast
Based on 3 publication(s) in Google Scholar
Bexotegrast (PLN-74809) is an orally active, potent dual αvβ6/αvβ1 integrin inhibitor with Kd of 5.7 nM and 3.4 nM, respectively. Bexotegrast inhibits αvβ6- and αvβ1-induced TGF-β activation with IC50 values of 29.8 nM and 19.2 nM, respectively. Bexotegrast has antifibrogenic effects and block multiple avenues of TGF-β activation in the fibrotic lung.
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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: 99.74%
- CAS 番号: 2376257-44-0
- 分子式: C27H36N6O3
- 分子量:492.61
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保管条件:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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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 Bexotegrast
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Cell Imaging/Staining
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RT-PCR
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IF
生物活性
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αvβ6 5.7 nM (Kd) |
αvβ1 3.4 nM (Kd) |
Bexotegrast (PLN-74809; 1.82 µM; 7-day incubation) significantly reduces collagen type I alpha I (COL1A1) mRNA expression by 54% in precision-cut lung slices (PCLSs). PLN-74809 shows an approximately 50% reduction in Smad2 phosphorylation[2].
Bexotegrast (1.82 µM; 3-day incubation) dose-dependently reduces Col1a1 mRNA expression in PCLSs prepared from fibrotic mouse lungs by up to 71%[2].
Bexotegrast fully inhibits αvβ6 integrin-mediated adhesion to LAP by normal human bronchial epithelial cells with an IC50 of 39.3 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice[2]
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Dosage:100, 250, and 500 mg/kg
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Administration:Orally; twice daily; from Day 7 to Day 21
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Result:Showed a dose-dependent, significant reduction in interstitial fibrillar collagen deposition in Bleomycin (3 units/kg)-challenged mice.
Dose-dependently blocked Smad3 phosphorylation.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2376257-44-0
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性状 Solid
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分子量 492.61
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分子式 C27H36N6O3
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Color White to light yellow
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SMILES
OC([C@H](CCN(CCOC)CCCCC(N1)=CC=C2C1=NCCC2)NC3=NC=NC4=C3C=CC=C4)=O
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別名
PLN-74809
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (3)
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Journal Impact Factor
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Most Recent
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Science
2026 Feb 5;391(6785):eadz4075. PMID: 41643022 -
Phytomedicine
Jiawei yanghe decoction alleviates osteoporotic osteoarthritis by promoting MSC osteogenic differentiation and homing via ITGB6/TGF-β/CXCR4 pathway. [Abstract]2025 Nov:147:157203. PMID: 40929885 -
bioRxiv
Bidirectional fibrogenic cross-talk revealed in a human iPSC-derived epithelial-mesenchymal co-culture model of pulmonary fibrosis. [Abstract]2026 Jan 31:2026.01.30.702837. PMID: 41659605
Bexotegrast purchased from MedChemExpress. Usage Cited in: bioRxiv. 2026 Jan 31:2026.01.30.702837. [Abstract]
SFTPCtdTomato and ACTA2GFP fluorescence in live co-cultures of SFTPCI73T mutant iAT2s and iLM treated with 2 μM Bexotegrast for 1 week, as compared to vehicle control (treatment starting on the first day of co-culture). Scale bars = 400 μm.
Bexotegrast purchased from MedChemExpress. Usage Cited in: bioRxiv. 2026 Jan 31:2026.01.30.702837. [Abstract]
RT-qPCR analysis showing fold change expression (normalized to iLM co-cultured control) of fibrotic markers in EPCAM- sorted cells from co-cultures of iLM with SFTPCI73T mutant iAT2s or iLM cultured alone. N = 5 for SB525334 (1 μM; 1 week), N = 6 for Bexotegrast (2 μM; 1 week), symbol shapes indicate experimental replicates, i.e. multiple wells of the same experiment.
Bexotegrast purchased from MedChemExpress. Usage Cited in: bioRxiv. 2026 Jan 31:2026.01.30.702837. [Abstract]
Immunofluorescence staining for KRT17 protein in co-cultures of SFTPCI73T mutant iAT2s and iLM. The results showed that treatment of co-cultures of SFTPCI73T mutant iAT2s and iLM for 7 days with either SB525334 (1 μM; 1 week) or Bexotegrast (2 μM; 1 week), compared to vehicle-treated controls, abolished KRT17 protein expression in co-cultured SFTPCI73T mutant iAT2s. Scale bars = 100 μm. Hoechst = nuclei.
溶剤 & 溶解度
DMSO : 100 mg/mL (203.00 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 and light). 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 and light). 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: ≥ 2.08 mg/mL (4.22 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.22 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: PBS
Solubility: 12.5 mg/mL (25.38 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
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 and light)
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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参考文献
[1]. Anindya Roy, et al. De novo design of highly selective miniprotein inhibitors of integrins αvβ6 and αvβ8. Nat Commun. 2023 Sep 13;14(1):5660. [Content Brief]
[2]. Martin L Decaris, et al. Dual inhibition of αvβ6 and αvβ1 reduces fibrogenesis in lung tissue explants from patients with IPF. Respir Res. 2021 Oct 19;22(1):265. [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 and light). 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 | 2.0300 mL | 10.1500 mL | 20.3000 mL | 50.7501 mL |
| 5 mM | 0.4060 mL | 2.0300 mL | 4.0600 mL | 10.1500 mL | |
| 10 mM | 0.2030 mL | 1.0150 mL | 2.0300 mL | 5.0750 mL | |
| 15 mM | 0.1353 mL | 0.6767 mL | 1.3533 mL | 3.3833 mL | |
| 20 mM | 0.1015 mL | 0.5075 mL | 1.0150 mL | 2.5375 mL | |
| 25 mM | 0.0812 mL | 0.4060 mL | 0.8120 mL | 2.0300 mL | |
| 30 mM | 0.0677 mL | 0.3383 mL | 0.6767 mL | 1.6917 mL | |
| 40 mM | 0.0508 mL | 0.2538 mL | 0.5075 mL | 1.2688 mL | |
| 50 mM | 0.0406 mL | 0.2030 mL | 0.4060 mL | 1.0150 mL | |
| 60 mM | 0.0338 mL | 0.1692 mL | 0.3383 mL | 0.8458 mL | |
| 80 mM | 0.0254 mL | 0.1269 mL | 0.2538 mL | 0.6344 mL | |
| 100 mM | 0.0203 mL | 0.1015 mL | 0.2030 mL | 0.5075 mL |
Bexotegrast 関連分類
HY-137561 関連分類
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