2. Metabolic Enzyme/Protease
  3. Aminopeptidase
  4. 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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ERAP1-IN-4

ERAP1-IN-4 Chemical Structure

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ERAP1-IN-4 Related Antibodies

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Description

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].

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.

ERAP1-IN-4 Related Antibodies
Parmacokinetics
Species Dose Route CL T1/2 Vdss F AUC0-t Cmax
Rat[1] 1 mg/kg i.v. 29 mL/min/kg 7.1 h 5.0 L/kg / / /
Rat[1] 2 mg/kg p.o. / / / 47 % 272 ng·h/mL 22 ng/mL
In Vivo

ERAP1-IN-4 (Compound 40) (1-3 mg/kg; i.v. or p.o.) demonstrates an oral bioavailability of 47% in healthy rats, with an unbound oral AUC0-t,u of 10.9 ng·h/mL following a 3 mg/kg oral dose[1].

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

Animal Model: Wistar Han[1]
Dosage: 1 mg/kg (i.v.); 3 mg/kg (p.o.)
Administration: i.v. or p.o.
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.
Molecular Weight

467.26

Formula

C16H14BrF3N2O4S
SMILES

OC(C1(NC(CN2C3=C(SC2=O)C(F)=CC(Br)=C3)=O)CCC(F)(CC1)F)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ERAP1-IN-4 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ERAP1-IN-4Aminopeptidasehuman hepatocyteshuman liver microsomesHeLa cellsEndoplasmic Reticulum Aminopeptidase 1cancerrat hepatocytesAllotype2Allotype1Caco-2ERAP1Inhibitorinhibitorinhibit

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