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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].

For research use only. We do not sell to patients.

Formula: C₁₆H₁₄BrF₃N₂O₄S
Molecular Weight:467.26

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

ERAP1-IN-4 Chemical Structure

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Sample (0.1mg)

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(In Japan)

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

All Aminopeptidase Isoforms :

CD13
LTA4H

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

Species	Dose	Route	CL	T_1/2	V_dss	F	AUC_0-t	C_max
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 AUC_0-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.

Chemical Information

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

Handling Instructions (2659 KB)

References

[1]. Law RP, et al. Automated Molecular Design in BRADSHAW, Applied to the Optimization of ERAP1 Inhibitors. J Med Chem. 2026;69(8):8869-8896. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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