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CAS No.: 243984-11-4

Resatorvid/瑞沙托维 Catalog No. CSN15947

Synonyms: TAK-242;CLI-095;瑞沙托维

TAK-242, a small-molecule-specific inhibitor of Toll-like receptor (TLR)4 signaling, inhibits the production of lipopolysaccharide-induced inflammatory mediators by binding to the intracellular domain of TLR4.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述TAK-242 is a novel TLR4 (Toll-like receptor 4) inhibitor with IC50 values of 1.1-33nM for inhibition of LPS-induced production of NO, TNF-α and IL-6 in RAW264.7 cells, mouse peritoneal macrophages and PBMCs. TAK-242 inhibited both MyD88-independent and -dependent pathway, independent of LPS concentration and types of TLR4 ligands. It did not affect LPS-induced conformational change of TLR4-MD-2 and TLR4 homodimerization. A 60-μg dose of TAK-242 to neonatal CCM (cerebral cavernous malformations) disease model (susceptible Krit1^ECKO mice) reduced CCM lesion volume by 80%. Intravenous administration of TAK-242 at dose of 1mg/kg and 3mg/kg 1 h before LPS challenge could protect mice from LPS-induced lethality.

动物研究
剂量	Mice: 3 mg/kg^[3] (i.p.), 0.3 mg/kg^[4] (i.p.), 10 mg/kg - 30 mg/kg^[5] (i.p>); 30 mg/kg, 100 mg/kg^[5] (p.o.) Rat: 0.5 mg/kg^[1] (i.v.), 0.1 mg/kg - 1 mg/kg^[6] (i.v.)
给药途径	i.p., p.o., i.v

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00143611	Sepsis	Phase 3	Completed	-	-
NCT00633477	Sepsis	Phase 3	Terminated(Business Decision; ... more >>No Safety Or Efficacy Concerns.) Collapse <<	-	Japan ... more >> Nagasaki, Japan Collapse <<
NCT00633477	-	-	Terminated(Business Decision; ... more >>No Safety Or Efficacy Concerns.) Collapse <<	-	-

参考文献

[1] Garate I, Garcia-Bueno B, et al. Toll-like 4 receptor inhibitor TAK-242 decreases neuroinflammation in rat brain frontal cortex after stress. J Neuroinflammation. 2014 Jan 11;11:8.
[2] Ni JQ, Ouyang Q, et al. Role of toll-like receptor 4 on lupus lung injury and atherosclerosis in LPS-challenge ApoE⁻/⁻ mice. Clin Dev Immunol. 2013;2013:476856.

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
- 2.7638 mL
- 13.8190 mL
- 27.6381 mL
- 5 mM
- 0.5528 mL
- 2.7638 mL
- 5.5276 mL
- 10 mM
- 0.2764 mL
- 1.3819 mL
- 2.7638 mL

技术信息

CAS号

243984-11-4

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H17ClFNO4S

运输

蓝冰

分子量

361.82

别名

TAK-242;CLI-095;瑞沙托维

溶解度

DMSO	140.0 mg/mL (386.9 mM)

动物实验配方

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