產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 5mg 10mg 100mg
CAS	507475-17-4
別名
化學名	2-(carbamoylamino)-5-(4-fluorophenyl)thiophene-3-carboxamide
分子式	C12H10FN3O2S
分子量	279.29
溶解度	≥ 13.95mg/mL in DMSO, ≥ 2.53 mg/mL in EtOH with ultrasonic and warming
儲存條件	Desiccate 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：

TPCA-1 is a novel, potent, and selective inhibitor of human IKK-2.

Demonstration that IκB kinase 2 (IKK-2) plays a pivotal role in the nuclear factor-κB-regulated production of proinflammatory molecules by stimuli such as tumor necrosis factor (TNF)-α and interleukin (IL)-1 suggests that inhibition of IKK-2 may be beneficial in the treatment of rheumatoid arthritis.

In vitro: Determination of the activity of TPCA-1 against ten selected kinases, COX-1 and COX-2, showed the compound to be ~550-fold selective for IKK-2 versus ten of these enzymes. TPCA-1 inhibits lipopolysaccharide-induced human monocyte production of TNF-α, IL-6, and IL-8 with an IC50 of 170 to 320 nM [1].

In vivo: Prophylactic administration of TPCA-1 at 3, 10, or 20 mg/kg resulted in a dose dependent reduction in the severity of murine collagen-induced arthritis. The significantly reduced disease severity and delay of disease onset resulting from administration of TPCA-1 at 10 mg/kg were comparable to the effects of the antirheumatic drug, etanercept [1].

Clinical trial: No clinical data are available currently.

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原創(chuàng)作者：上海莼試生物技術有限公司

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