產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 5mg 10mg 50mg 100mg
CAS	243984-11-4
別名	Resatorvid;TAK242;TAK 242
化學(xué)名	ethyl (6R)-6-[(2-chloro-4-fluorophenyl)sulfamoyl]cyclohexene-1-carboxylate
分子式	C15H17ClFNO4S
分子量	361.82
溶解度	≥ 18.091 mg/mL in DMSO, ≥ 100.6 mg/mL in EtOH
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

IC50: With IC50 of 1.1 to 11 nM, TAK-242 inhibited LPS-induced NO production, tumor necrosis factor-alpha and interleukin (IL)-6 in RAW264.7 cells and mouse peritoneal macrophages [1].

Toll, a member of the Toll-like receptor (TLR) family, was identified as a gene product essential for the development of embryonic dorsoventral polarity in Drosophila melanogaster. Moreover, it has been also found to play a critical role in the antifungal response of flies. TAK-242 (resatorvid), a cyclohexene derivative, is recongnizred as a novel small-molecule compound selectively inhibiting TLR4 signaling.

In vitro: A previous in-vitro study showed that TAK-242 could inhibit the production of lipopolysaccharide-induced inflammatory mediators by binding to the intracellular domain of TLR4 using coimmunoprecipitation approach. Among 10 different human TLRs, TAK-242 selectively bound to TLR4. These findings suggested that TAK-242 could selectively bind to TLR4 and disrupted the interaction of TLR4 with adaptor molecules, thereby inhibiting TLR4 signal transduction and its downstream signaling [2].

In vivo: Preclinical animal study demonostrated that the acute restraint stress exposure upregulateed TLR-4 expression both at the mRNA and protein level in rat. TAK-242 pre-stress administration prevented the accumulation of potentially deleterious inflammatory and oxidative/nitrosative mediators in the brain frontal cortex of rats. These finding s indicated that the use of TAK-242 or other TLR-4 signalling pathway inhibitory compounds could be considered as a potential therapeutic adjuvant strategy to constrain the inflammatory process taking place after stress exposure and in stress-related neuropsychiatric diseases [3].

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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