MD2-TLR4-IN-1

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Chemical Structure| 2249801-12-3 同义名 : -
CAS号 : 2249801-12-3
货号 : A1177209
分子式 : C22H14Cl2N4O
纯度 : 99%+
分子量 : 421.28
MDL号 : MFCD32067977
存储条件:

Pure form Keep in dark place, sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.37mL

0.47mL

0.24mL

11.87mL

2.37mL

1.19mL

23.74mL

4.75mL

2.37mL

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