M62812

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TLR4抑制剂。抑制 HEK293 细胞中 LPS 诱导的 NF-κB 激活 (IC50 = 2.4 μg/mL)。还抑制 PBMC 和 HUVEC 中 LPS 诱导的细胞因子产生和促凝血作用。延长小鼠感染性休克模型的生存期。

TLR4 inhibitor. Inhibits LPS-induced NF-κB activation in HEK293 cells (IC50 = 2.4 μg/mL). Also inhibits LPS-induced cytokine production and procoagulant effects in PBMCs and HUVECs. Prolongs survival in a mouse septic shock model.(In Vitro):M62812 suppressed LPS-induced upregulation of inflammatory cytokines, adhesion molecules and procoagulant activity in human vascular endothelial cells and peripheral mononuclear cells. The half maximal inhibitory concentrations in these assays ranged from 1 to 3 μg/ml . Single intravenous administration of M62812 (10-20 mg/kg) protected mice from lethality and reduced inflammatory and coagulatory parameters in a murine d-galactosamine-sensitized endotoxin shock model . M62812 (20 mg/kg) also prevented mice from lethality in a murine cecal ligation and puncture model .

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Animal Model:D-galactosamine-sensitized endotoxin shock mouse modelDosage:10-20 mg/kg Administration:Intravenous administration (i.v.)Result:Prevented elevation of TNF-α, IL-6, soluble E-selectin, thrombin/antithrombin complexes and glutamic pyruvic transaminase activity at 20 mg/kg.Prolonged survival in a d-galactosamine-sensitized endotoxin shock mouse model.Animal Model:Cecal ligation and puncture mouse model Dosage:20 mg/kg Administration:Intravenous administration (i.v.); once a day for three days Result:Reduced mortality in a murine cecal ligation and puncture model.

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Immunology/Inflammation

TLR

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613263-00-6

330.23

C13H13Cl2N3OS

>98% (HPLC)

In Vitro:?0.1 M HCL : ≥ 50 mg/mL (151.4)

Cl.Cl.Nc1nsc2cc(Oc3ccccc3N)ccc12

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(-20℃)

With Ice Pack

≥ 2 years