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Cat. No.: HY-183267

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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].

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화학식: C₁₆H₁₄BrF₃N₂O₄S
분자량:467.26

보관:

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

ERAP1-IN-4 Chemical Structure

Amount: USD 0.00

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Use of MCE Products

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

Biological Activity
- 제품 설명
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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

분자량 467.26
화학식 C₁₆H₁₄BrF₃N₂O₄S
SMILES

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

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

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

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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