2. ERAP1-IN-4

ERAP1-IN-4 是一种口服有效的内质网氨肽酶 1 (ERAP1) 抑制剂。ERAP1-IN-4 可抑制 ERAP1 对肽底物的水解作用，对 Allotype1 和 Allotype2 活性较强，对其他同种异型的效力降低。ERAP1-IN-4 可调控 ERAP1 介导的肽加工过程，从而抑制抗原表位呈递。ERAP1-IN-4 可用于癌症研究。

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ERAP1-IN-4

ERAP1-IN-4 Chemical Structure

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Customer Review

ERAP1-IN-4 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ERAP1-IN-4 is an orally acvtive endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor. 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].

体外研究
(In Vitro)

ERAP1-IN-4 (Compound 40) 可强效抑制 ERAP1 同种异型 2 的酶活性，其 pIC50 为 7.9，LLE 为 5.3[1]。
ERAP1-IN-4 可抑制 HeLa 细胞中的抗原呈递，测得的 pIC50 为 7.3，未结合细胞的 pIC50 为 7.8[1]。
ERAP1-IN-4 (0.5-5 μM；4 小时) 在大鼠血液中的游离分数为 0.04，在人肝微粒体中的游离分数为 0.83[1]。

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

ERAP1-IN-4 相关抗体:
药代动力学
(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
体内研究
(In Vivo)

ERAP1-IN-4 (Compound 40) (1-3 mg/kg；静脉注射或口服) 在健康大鼠中表现出 47%的口服生物利用度，在 3 mg/kg 口服剂量下的游离口服 AUC0-t,u 为 10.9 ng·h/mL[1]。

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.
分子量

467.26

Formula

C16H14BrF3N2O4S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

ERAP1-IN-4 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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-4human hepatocyteshuman liver microsomesHeLa cellsEndoplasmic Reticulum Aminopeptidase 1cancerrat hepatocytesAllotype2Allotype1Caco-2ERAP1Inhibitorinhibitorinhibit

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目录号：
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