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Art. -Nr.: HY-137561A

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Bexotegrast hydrochloride

Name: Bexotegrast hydrochloride
Brand: MedChemExpress
SKU: HY-137561A
Availability: PreOrder

(Synonyms: PLN-74809 hydrochloride)

5 Cited Publications

Kundenbewertung

Based on 5 publication(s) in Google Scholar

Bexotegrast (PLN-74809) hydrochloride is an orally active, potent dual αvβ6/αvβ1 integrin inhibitor with K_d of 5.7 nM and 3.4 nM, respectively. Bexotegrast hydrochloride inhibits αvβ6- and αvβ1-induced TGF-β activation with IC₅₀ values of 29.8 nM and 19.2 nM, respectively. Bexotegrast hydrochloride has antifibrogenic effects and block multiple avenues of TGF-β activation in the fibrotic lung.

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CAS. Nr.: 2775365-40-5
Formel: C₂₇H₃₈Cl₂N₆O₃
Molecular Weight:565.54

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (275 KB)

Bexotegrast hydrochloride Chemical Structure

CAS. Nr.: 2775365-40-5

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Bexotegrast

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

αvβ6

5.7 nM (Kd)

αvβ1

3.4 nM (Kd)

Alle Integrin Isoform-spezifische Produkte anzeigen :

In Vitro

Bexotegrast (PLN-74809; 1.82 µM; 7-day incubation) hydrochloride significantly reduces collagen type I alpha I (COL1A1) mRNA expression by 54% in precision-cut lung slices (PCLSs). Bexotegrast hydrochloride shows an approximately 50% reduction in Smad2 phosphorylation^[2].
Bexotegrast (1.82 µM; 3-day incubation) hydrochloride dose-dependently reduces Col1a1 mRNA expression in PCLSs prepared from fibrotic mouse lungs by up to 71%^[2].
Bexotegrast hydrochloride 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.

In Vivo

Bexotegrast (PLN-74809; orally; 100, 250, and 500 mg/kg twice daily; from Day 7 to Day 21) hydrochloride shows a dose-dependent, significant reduction in interstitial fibrillar collagen deposition in Bleomycin-challenged mice. Bexotegrast hydrochloride dose-dependently blocks Smad3 phosphorylation^[2].

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

Animal Model:

C57BL/6 mice^[2]
Dosage:

100, 250, and 500 mg/kg
Administration:

Orally; twice daily; from Day 7 to Day 21
Result:

Showed a dose-dependent, significant reduction in interstitial fibrillar collagen deposition in Bleomycin (3 units/kg)-challenged mice.
Dose-dependently blocked Smad3 phosphorylation.

Chemical Information

CAS. Nr. 2775365-40-5
Molecular Weight 565.54
Formel C₂₇H₃₈Cl₂N₆O₃
SMILES

COCCN(CCCCC(N1)=CC=C2C1=NCCC2)CC[C@@H](C(O)=O)NC3=NC=NC4=C3C=CC=C4.Cl.Cl
Synonyms

PLN-74809 hydrochloride
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (5)

All Cell Imaging/StainingRT-PCRIF

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Journal Impact Factor

Science

Antifibrotic drug finerenone restores fertility in premature ovarian insufficiency. [Abstract]

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
Int J Surg

2026 Jul;112(7):p 13073-13091.
Cancers (Basel)

Role of EDA Fibronectin and Toll-like Receptor 5 in the Development of the Tumor Microenvironment in Triple Negative Breast Cancer. [Abstract]

2026 Aug 20;18(16):2693. PMID: 42650004
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 hydrochloride purchased from MedChemExpress. Usage Cited in: bioRxiv. 2026 Jan 31:2026.01.30.702837. [Abstract]

SFTPC^tdTomato and ACTA2^GFP fluorescence in live co-cultures of SFTPC^I73T 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 hydrochloride 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 SFTPC^I73T 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 hydrochloride 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 SFTPC^I73T 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 SFTPC^I73T mutant iAT2s. Scale bars = 100 μm. Hoechst = nuclei.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

Bexotegrast hydrochloride

5 Cited Publications

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Reinheit & Dokumentation
Verweise

1/16
1/16

Bexotegrast hydrochloride purchased from MedChemExpress. Usage Cited in: bioRxiv. 2026 Jan 31:2026.01.30.702837. [Abstract]

Customer Validation
SFTPC^tdTomato and ACTA2^GFP fluorescence in live co-cultures of SFTPC^I73T 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.
1/16

Bexotegrast hydrochloride purchased from MedChemExpress. Usage Cited in: bioRxiv. 2026 Jan 31:2026.01.30.702837. [Abstract]

Customer Validation
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 SFTPC^I73T 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.
1/16

Bexotegrast hydrochloride purchased from MedChemExpress. Usage Cited in: bioRxiv. 2026 Jan 31:2026.01.30.702837. [Abstract]

Customer Validation
Immunofluorescence staining for KRT17 protein in co-cultures of SFTPCI73T mutant iAT2s and iLM. The results showed that treatment of co-cultures of SFTPC^I73T 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 SFTPC^I73T mutant iAT2s. Scale bars = 100 μm. Hoechst = nuclei.

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Bexotegrast hydrochloride

Other In-stock Forms of Bexotegrast hydrochloride

Publications Citing Use of MedChemExpress (MCE) Bexotegrast hydrochloride

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