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 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.
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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)