Tapinarof 是一种从发光杆菌中提取的天然产物,可消除炎症。它是芳烃受体 (AhR) 激动剂,EC50为 13 nM。
产品描述
Tapinarof is targeted as a topical cream treatment for psoriasis, a chronic autoimmune skin disease.
体外活性
Tapinarof activates the AhR pathway through direct binding. Tapinarof induces nuclear translocation of AhR in immortalized keratinocytes (HaCaT) in a dose-dependent way.
体内活性
Tapinarof acts through AhR to reduce inflammation in IMQ-treated mice. AhR-sufficient mice on a C57Bl/6 background exhibit a reduced clinical score after treatment with Tapinarof or 6-formylindolo(3,2-b)carbazole (FICZ). On the contrary, AhR KO mice do not respond to the anti-inflammatory effects of Tapinarof. FICZ is used as a comparator in these studies and yields similar results, with dramatically reduced inflammatory responses in wild-type, but not AhR KO mice.
Cas No.
79338-84-4
分子式
C17H18O2
分子量
254.32
别名
Benvitimod;苯烯莫德;GSK2894512;WBI 1001
储存和溶解度
DMSO:150 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years