M62812_product_DataBase

Bioactivity	M62812 is a toll-like receptor 4 (TLR4) signaling inhibitor. M62812 inhibits endothelial and leukocyte activation and prevents lethal septic shock in mice. M62812 can reduces LPS-induced coagulation and inflammatory responses. M62812 can be used for the research of sepsis[1].
Invitro	M62812 (10 μg/mL; 6 h) 在 NF-κB 荧光素酶表达细胞中完全抑制 LPS 诱导的 NF-κB 的活化的 IC50 为 2.4 μg/mL[1]。M62812 (3 μg/mL; 6 h) 在外周血单核细胞中完全抑制经 LPS 刺激后诱导产生 TNF-α 的 IC50 为 0.7 μg/mL[1]。M62812 (3 μg/mL; 6 h) 在人内皮细胞中完全抑制 IL-6 和 E-selection 产生的 IC50 分别为 0.43 μg/mL 和 1.4 μg/mL[1]。
In Vivo	M62812 (i.v.; 10-20 mg/kg; 单剂量) 在 D-氨基半乳糖致敏的内毒素休克小鼠模型中具有保护作用，并可降低炎症和凝血参数[1]。M62812 (i.v.; 20 mg/kg; 每天 1 次, 共 3 天) 在小鼠盲肠结扎和穿刺模型中防止小鼠死亡[1]。 Animal Model:
Name	M62812
CAS	613263-00-6
Formula	C13H13Cl2N3OS
Molar Mass	330.23
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[1]. Nakamura M, et al. Toll-like receptor 4 signal transduction inhibitor, M62812, suppresses endothelial cell and leukocyte activation and prevents lethal septic shock in mice. Eur J Pharmacol. 2007 Aug 27;569(3):237-43.

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