|N-(3-(1H-吲哚-5-基)-1H-吲唑-5-基)-2,6-二氯苯甲酰胺|CsnPharm

CAS No.: 2249801-12-3

MD2-TLR4-IN-1 Catalog No. CSN26177

Synonyms: MD2-TLR4-IN-1

MD2-TLR4-IN-1 is an inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex may be a promising target in the treatment of Gram-negative bacterial-induced inflammatory disorders. MD2-TLR4-IN-1 is a 3-(indol-5-yl)-indazole analogue that acts as an MD2-TLR4 complex inhibitor. It inhibited lipopolysaccharides-induced expression of TNF-α and interleukin (IL)-6 in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively. Pretreatment of macrophages subjected to LPS exposure with MD2-TLR4-IN-1 (10 μM) suppressed the nuclear levels of NF-κB p65 subunit. MD2-TLR4-IN-1 binds to recombinant MD2 and TLR4 protein with KD values of 185 μM and 146 μM, respectively. MD2-TLR4-IN-1 (10 μM) significantly inhibited the dimerization of the MD2-TLR4 complex in LPS-activated mouse primary macrophages. A single injection of MD2-TLR4-IN-1 (5 mg/kg) significantly decreased macrophage infiltration, myeloperoxidase activity, and expression of inflammatory cytokines in LPS-challenged C57BL/6 mice^[1].
作用机制MD2-TLR4-IN-1 is an inhibitor of the MD2-TLR4 complex. It binds directly to the complex and disrupts its activity^[1].
参考文献

[1] Liu Z, Chen L, Yu P, Zhang Y, Fang B, Wu C, Luo W, Chen X, Li C, Liang G. Discovery of 3-(Indol-5-yl)-indazole Derivatives as Novel Myeloid Differentiation Protein 2/Toll-like Receptor 4 Antagonists for Treatment of Acute Lung Injury. J Med Chem. 2019 Jun 13;62(11):5453-5469. doi: 10.1021/acs.jmedchem.9b00316

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3737 mL
- 11.8686 mL
- 23.7372 mL
- 5 mM
- 0.4747 mL
- 2.3737 mL
- 4.7474 mL
- 10 mM
- 0.2374 mL
- 1.1869 mL
- 2.3737 mL

技术信息

CAS号

2249801-12-3

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H14Cl2N4O

运输

蓝冰

分子量

421.28

别名

MD2-TLR4-IN-1

溶解度

DMSO	84.0 mg/mL (199.4 mM)
Water	Insoluble
Ethanol	5.0 mg/mL (11.9 mM)

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

MD2-TLR4-IN-1 Catalog No. CSN26177

靶点选择性

请登录您的专属账户

确认信息