2. GPCR/G Protein Stem Cell/Wnt MAPK/ERK Pathway
  3. Protease Activated Receptor (PAR) ERK
  4. I-287

I-287 是一种具有口服活性的 PAR2 的选择性抑制剂，对 Gαq 和 Gα12/13 活性及其下游效应物起负异构调节作用。I-287 可减轻 Complete Freund's adjuvant (HY-153808) 诱导的小鼠炎症，可用于免疫炎症研究。

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I-287 Chemical Structure

I-287 Chemical Structure

CAS No. : 2014368-93-3

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规格 价格 是否有货
1 mg ￥2960
询问价格 & 货期
5 mg ￥7400
询问价格 & 货期

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I-287 相关抗体

Top Publications Citing Use of Products

查看 ERK 亚型特异性产品:

查看所有亚型
ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

I-287 is a orally active selective PAR2 inhibitor that acting as a negative allosteric regulator on Gαq and Gα12/13 activity and their downstream effectors. I-287 reduces Complete Freund's adjuvant (HY-153808)-induced inflammation in mice and can be used for inflammation/immunology research[1].

IC50 & Target[1]

ERK1

 

ERK2

 

体外研究
(In Vitro)

I-287 (0-60 μM; 15-30 分钟) 抑制在 HEK-293 细胞中 PAR2 介导的 Gαq 和 Gα12/13 而不是 Gi/o 蛋白的激活，而对 PAR2 介导的 β arrestin 2 募集和受体内化没有影响[1]。
I-287 (0-60 μM; 15-30 分钟) 抑制 PAR2 介导的 ERK1/2 激活[1]。
I-287 (10 μM；30 分钟) 可抑制 HCT-116 和 A549 细胞中 PAR2 诱导的 IL-8 细胞因子的分泌[1]。

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

I-287 相关抗体:

Western Blot Analysis[1]

Cell Line: HEK-293 cells
Concentration: 0-60 μM
Incubation Time: 15 min
Result: Inhibited PAR2-mediated ERK1/2 activation in HEK293 cells.
体内研究
(In Vivo)

I-287(口服，50 mg/kg) 降低 C57BL/6J 小鼠中 Complete Freund's adjuvant (HY-153808) 诱导的炎症反应[1]。

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

Animal Model: CFA-induced paw inflammation in adult male C57BL/6J mice [1]
Dosage: 50 mg/kg
Administration: Oral gavage (p.o.) following the CFA
Result: Reduces CFA-induced inflammation in C57BL/6J mice
分子量

565.04

Formula

C30H30ClFN4O4
CAS 号
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

I-287 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:

I-2872014368-93-3I287I 287Protease Activated Receptor (PAR)ERKThrombin receptorsExtracellular signal regulated kinasesPAR2 inhibitorCFA-induced inflammationHEK-293ERK1/2GαqGα12/13Inhibitorinhibitorinhibit

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产品名称：
I-287
目录号：
HY-148016
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