ERAP1-IN-4
ERAP1-IN-4 is an orally acvtive endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor with a pIC50 of 7.9 and an LLE of 5.3. ERAP1-IN-4 inhibits hydrolysis of peptide substrates by ERAP1, with high activity against Allotype1 and Allotype2. ERAP1-IN-4 reduced efficacy against other allotypes, and modulates ERAP1-mediated peptide processing to inhibit antigenic epitope presentation. ERAP1-IN-4 can be used for the research of cancer[1].
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- Fòrmula: C16H14BrF3N2O4S
- Peso molecular:467.26
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
In Vitro
ERAP1-IN-4 (Compound 40) potently inhibits ERAP1 allotype 2 enzymatic activity with a pIC50 of 7.9 and an LLE of 5.3[1].
ERAP1-IN-4 inhibits antigen presentation in HeLa cells with a measured pIC50 of 7.3 and an unbound cellular pIC50 of 7.8[1].
ERAP1-IN-4 (0.5-5 μM; 4 h) has a fraction unbound of 0.04 in rat blood and 0.83 in human liver microsomes[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:Wistar Han[1]
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Dosage:1 mg/kg (i.v.); 3 mg/kg (p.o.)
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Administration:i.v. or p.o.
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Result:Exhibited unbound clearance (CLu) of 725 mL/min/kg, half-life (t1/2) of 7.1 h, and unbound volume of distribution at steady state (Vd,ss,u) of 125 L/kg following intravenous dosing at 1 mg/kg.
Achieved oral bioavailability (F%) of 47%, dose-normalized unbound area under the curve (AUCt,u) of 10.9 ng·h/mL, and dose-normalized unbound peak concentration (Cmax,u) of 0.87 ng/mL following oral dosing at 3 mg/kg.
Chemical Information
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Peso molecular 467.26
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Fòrmula C16H14BrF3N2O4S
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SMILES
OC(C1(NC(CN2C3=C(SC2=O)C(F)=CC(Br)=C3)=O)CCC(F)(CC1)F)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ERAP1-IN-4 Related Classifications
HY-183267 Related Classifications
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