αvβ5 integrin-IN-3
αvβ5 integrin-IN-3 is an orally active, selective αVβ5 integrin inhibitor with an IC50 value of 0.61 nM. αvβ5 integrin-IN-3 inhibits αVβ1, αVβ3 and αVβ6 integrins with IC50 values of 21 nM, 5.5 nM and 18 nM, respectively. αvβ5 integrin-IN-3 reduces total Collagen content in a mouse unilateral ureteral obstruction model. αvβ5 integrin-IN-3 can be used for the research of renal fibrosis.
For research use only. We do not sell to patients.
- CAS No.: 2226557-15-7
- Formula: C22H26N6O2
- Molecular Weight:406.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
αvβ5 0.61 nM (IC50) |
αvβ1 21 nM (IC50) |
αvβ3 5.5 nM (IC50) |
αvβ6 18 nM (IC50) |
αvβ8 2490 nM (IC50) |
αIIbβ3 186 nM (IC50) |
In Vitro
αvβ5 integrin-IN-3 (Compound 14) potently inhibits human αVβ6, αVβ1, αVβ3, and αVβ5 integrins with IC50 values ranging from 0.61 nM to 21 nM, and exhibits high selectivity over human αVβ8 and αIIbβ3 integrins[1].
αvβ5 integrin-IN-3 has reduced plasma protein binding across rat, mouse, and cynomolgus monkey plasma, with free fractions ranging from 9.0% to 21%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female)[1]
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Dosage:10 mg/kg
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Administration:p.o.; daily; 8 days
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Result:Reduced total kidney collagen content by 25% versus vehicle.
Reduced kidney expression of pro-fibrotic genes including Col1a1, Col3a1, fibronectin, and α-SMA.
Measured mean trough plasma concentration of 25 nM 16 hours after the final dose, corresponding to an estimated mean free concentration of 8.9 nM.
Chemical Information
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CAS No. 2226557-15-7
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Molecular Weight 406.48
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Formula C22H26N6O2
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SMILES
OC(C[C@@H](C1=CN=C(C)N=C1)N2C=CC(CCCC3=NC(NCCC4)=C4C=C3)=N2)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Fibrosis/Collagen Morphometry
Fibrosis and collagen morphometry is based on the quantitative visualization of fibrillar collagen deposition in tissue sections using histochemical stains such as Sirius Red (Picrosirius Red) or Masson's trichrome, followed by image-based or polarization-enhanced analysis to estimate collagen proportional area as a surrogate of extracellular matrix accumulation during fibrotic remodeling. Sirius Red combined with polarized light microscopy enhances detection of collagen fibers due to birefringence properties, enabling more specific visualization of collagen type I and III fibrils compared to conventional bright-field histology, while whole-section or region-restricted digital morphometry reduces field-selection bias in fibrosis assessment. Alternative quantitative approaches include second harmonic generation (SHG) and two-photon excited fluorescence microscopy, which enable label-free detection of fibrillar collagen and have been validated against histological staining and biochemica
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Collagen: Sirius Red Staining
Sirius Red or picrosirius red staining is a histochemical method for visualizing collagen-rich extracellular matrix in tissue sections, and collagen fibers are detected as red-stained structures under bright-field microscopy with enhanced birefringence under polarized light. Picrosirius red is useful for assessing total collagen organization, distribution, and fibrosis burden, but polarized color should not be interpreted as a definitive collagen type I versus type III readout because color is affected by fiber orientation, thickness, and packing.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
Masson’s Trichrome (collagen/trichrome staining) is a histological technique that differentially stains tissue compartments using sequential acidic dyes to distinguish collagen from muscle and cytoplasmic components based on dye affinity and tissue permeability differences, enabling visualization of fibrosis and connective tissue architecture in histological sections. The classical formulation typically uses Weigert's iron hematoxylin for nuclear staining, Biebrich scarlet-acid fuchsin for cytoplasm and muscle, and aniline blue (or light green variants) for collagen, producing a characteristic blue/green collagen signal contrasted against red cytoplasm and dark nuclei. The staining principle relies on selective displacement of smaller dye molecules by larger anionic dyes in collagen-rich regions under controlled acidified conditions, which enhances collagen-specific dye retention. This property makes the method widely used for fibrosis assessment in organs such as heart, liver, lung, a
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)