Resatorvid

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

Resatorvid (TAK-242) 是 Toll 样受体 4 (TLR4) 的选择性抑制剂。 Resatorvid 抑制 IL-6、TNF-R 和 NO 产生（IC50：1.3 nM、1.9 nM 和 1.8 nM）。Resatorvid 抑制 LPS 刺激的人外周血单核细胞产生 NO、TNF-α 和 IL-6 （PBMC，IC50：11-33 nM）。

Resatorvid (TAK-242) is a selective inhibitor of Toll-like receptor 4 (TLR4). Resatorvid inhibits IL-6, TNF-R and NO production (IC50s: 1.3 nM, 1.9 nM, and 1.8 nM).Resatorvid suppresses the production of NO, TNF-α, and IL-6 from LPS-stimulated human peripheral blood mononuclear cells (PBMCs, IC50s: 11-33 nM). Resatorvid (1-100 nM; 15 minutes; PBMCs cells) markedly inhibits the LPS-induced phosphorylation of extracellular signal-regulated kinase 1/2 (Erk1/2), p38, and JNK/SAPK as well as degradation of IκBβ at a concentration of 100 nM. Resatorvid (1-100 nM; 4 hours) inhibits mRNA expression of IL-6 and TNF-α induced by LPS and IFN-γ in RAW264.7 cells.In ApoE knockout and wild-type mice, Resatorvid (0.3?mg/kg; intraperitoneal injection; twice a week; for 4 weeks) treatment inhibits serum autoantibodies (ANA and anti-dsDNA), cytokines (IFN-γ, TNF-α, IL-1β), lung inflammation, and intima-media thickness in brachiocephalic artery.

RT-PCRCell Line:RAW264.7 cells Concentration:1 nM, 10 nM, 100 nM Incubation Time:4 hours Result:TNF-α and IL-6 mRNA expression levels were clearly suppressed at concentrations of 10 to 100 nM.Western Blot Analysis Cell Line:PBMCs cells Concentration:1 nM, 10 nM, 100 nM Incubation Time:15 minutes Result:The phosphorylation of mitogen-activated protein kinases induced by LPS was also inhibited in a concentration-dependent manner.

Animal Model:Male C57BL/6 mice (8-12 weeks of age) treated with lipopolysaccharide (LPS)Dosage:3?mg/kg Administration:Intraperitoneal injection; for 2 days Result:Pretreatment of mice reduced or reversed all the detrimental effects of LPS.

TAK-242,CLI-095

Immunology/Inflammation

TLR

TLR4|TNF-R

Inflammation

Septic shock

243984-11-4

361.82

C15H17ClFNO4S

>98% (HPLC)

DMSO:100 mg/mL (276.38 mM; Need ultrasonic)

O=S([C@H]1C(C(OCC)=O)=CCCC1)(NC2=CC=C(C=C2Cl)F)=O

——

(-20℃)

With Ice Pack

≥ 2 years