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.
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- CAS. Nr.: 2226557-15-7
- Formel: C22H26N6O2
- Molecular Weight:406.48
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Help & FAQs
Biologische Aktivität
Beschreibung
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.
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. Nr. 2226557-15-7
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Molecular Weight 406.48
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
αvβ5 integrin-IN-3 Related Classifications
HY-189093 Related Classifications
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