MD2-TLR4-IN-1
产品说明书
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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 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 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 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.37mL 0.47mL 0.24mL |
11.87mL 2.37mL 1.19mL |
23.74mL 4.75mL 2.37mL |
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