2. JAK/STAT Signaling Stem Cell/Wnt Immunology/Inflammation Apoptosis
  3. STAT Interleukin Related TNF Receptor
  4. ER-464195-01

ER-464195-01 是一种口服有效的 CRT 和 ITGAs 结合抑制剂。ER-464195-01 通过解离 CRT 和 ITGAs 之间的结合来抑制白细胞浸润和随后的炎症级联反应。ER-464195-01 下调由 DSS (HY-116282C) 诱导的促炎基因 (例如 TNF-α、IL-1β、IL-6、IL-17f) 的表达，并抑制 STAT3 的磷酸化和血清淀粉样蛋白 A (SAA) 的产生。ER-464195-01 可用于炎症性肠病 (IBD) 的研究。

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ER-464195-01

ER-464195-01 Chemical Structure

CAS No. : 859218-37-4

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规格 价格 是否有货 数量
5 mg ￥722
In-stock
10 mg ￥1148
In-stock
25 mg ￥2278
In-stock
50 mg ￥3638
In-stock
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Customer Review

ER-464195-01 相关抗体

Top Publications Citing Use of Products

查看 STAT 亚型特异性产品:

查看所有亚型
STAT3 STAT5 STAT6 STAT1

查看 Interleukin Related 亚型特异性产品:

查看所有亚型
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

查看 TNF Receptor 亚型特异性产品:

查看所有亚型
TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ER-464195-01 is an orally active calreticulin (CRT) and integrin α subunits (ITGAs) binding inhibitor. ER-464195-01 inhibits leukocyte infiltration and subsequent inflammatory cascade reactions by dissociating the binding between CRT and ITGA. ER-464195-01 down-regulates the expression of pro-inflammatory genes (such as TNF-α, IL-1β, IL-6, IL-17f) induced by DSS (HY-116282C), and inhibit the phosphorylation of STAT3 and the production of serum amyloid A (SAA). ER-464195-01 can be used for the study of inflammatory bowel disease (IBD)[1].

IC50 & Target[1]

STAT3

 

IL-1β

 

IL-6

 

IL-17F

 

体外研究
(In Vitro)

ER-464195-01 (5 μM) 可有效抑制 Jurkat 细胞内 CRT 与 ITGA4 的相互作用，并显著降低细胞表面 CRT 的水平[1]。
ER-464195-01 (0.01-10 μM，60 分钟) 可抑制 PMA (HY-18739) 刺激的 VCAM-1 细胞和 fMLP (HY-P0224) 刺激的 ICAM-1 细胞的粘附能力，IC50 值分别为 0.15 μM 和 0.19 μM，在 MnCl2 刺激下则无抑制效果[1]。

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

ER-464195-01 相关抗体:
体内研究
(In Vivo)

ER-464195-01 (5-10 mg/kg，口服，每日一次，连用 6-32 天) 通过预防和治疗给药均可改善 IBD 小鼠模型的病情严重程度[1]。

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

Animal Model: DSS induced IBD model established in female Balb/c mice (9- to 10-week-old)[1]
Dosage: 10 mg/kg (preventive administration) and 5 mg/kg (therapeutic administration)
Administration: Oral administration (p.o.), once daily for 6-7 days
Result: Effectively alleviated the weight loss, increased DAI, and shortened colon in mice under both administration methods.
Reduced the interaction signal between CRT and ITGA4.
Inhibited the upregulation of key pro-inflammatory cytokine mRNAs such as TNF-α, IL1-b, IL-6, and IL-17f induced by DSS.
Inhibited the phosphorylation of STAT3 (p-STAT3) induced by DSS and the production of serum amyloid A (SAA).
Animal Model: CD4+CD45RBhigh T-cell transfer model established in female Balb/c mice (6-week-old)[1]
Dosage: 10 mg/kg
Administration: Oral administration (p.o.), once daily for 32 days
Result: Significantly improved the weight loss in mice and the changes in their fecal characteristics (diarrhea).
分子量

379.02

Formula

C23H39ClN2
CAS 号
性状

固体

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献

ER-464195-01 相关分类

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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:

ER-464195-01859218-37-4STATInterleukin RelatedTNF ReceptorILTumor Necrosis Factor ReceptorTNFRInflammatory bowel diseaseCalreticulinIntegrin alphaNecrosulfonamideInhibitorinhibitorinhibit

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