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United States

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製品番号: 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].

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

分子式: C₁₆H₁₄BrF₃N₂O₄S
分子量:467.26

保管条件:

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

ERAP1-IN-4 構造式

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

生物活性
- 製品説明
- 体外実験
- Parmacokinetics
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

Aminopeptidase アイソフォーム固有の製品をすべて表示 :

CD13
LTA4H

体外実験

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

体内実験

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.

化学情報

分子量 467.26
分子式 C₁₆H₁₄BrF₃N₂O₄S
SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[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

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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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