塔皮纳洛夫，79338-84-4，10mM in DMSO

中文名：塔皮纳洛夫

英文名：Tapinarof

英文别名：Benvitimod|Tapinarof|79338-84-4|3,5-Dihydroxy-4-isopropylstilbene|Vtama|WBI-1001|GSK2894512|3,5-DH4IS|WBI 1001|GSK-2894512|3,5-dihydroxy-4-isopropyl-trans-stilbene|Tapinarof [USAN]|UNII-84HW7D0V04|2-Isopropyl-5-styrylbenzene-1,3-diol|(E)-2-(1-Methylethyl)

纯度：10mM in DMSO

货号：T425990

Cas号：79338-84-4

存储温度：-80℃储存

产品介绍：

Information

Tapinarof Tapinarof (GSK2894512, Benvitimod, WBI 1001, DHPS, DMVT 505) is a natural agonist of aryl hydrocarbon receptor (AhR) and induces nuclear translocation of AhR in immortalized keratinocytes (HaCaT) with EC50 of 0.16 nM. Tapinarof induces cellular apoptosis in CD4+ T cells in a dosedependent manner with IC50 of 5.2 μM.

Targets

AhR (in immortalized keratinocytes); apoptosis (in CD4+ T cells) 0.16 nM(EC50); 5.2 μM

In vitro

Tapinarof binds and activates AhR in multiple cell types, including cells of the target tissue –human skin. In addition, tapinarof moderates proinflammatory cytokine expression in stimulated peripheral blood CD4+ T cells and ex vivo human skin, and impacts barrier gene expression in primary human keratinocytes; both of these processes are likely to be downstream of AhR activation based on current evidence.

In vivo

The anti-inflammatory properties of tapinarof derive from AhR agonism is conclusively demonstrated using the mouse model of imiquimod-induced psoriasiform skin lesions. Topical treatment of AhR-sufficient mice with tapinarof leads to compound-driven reductions in erythema, epidermal thickening and tissue cytokine levels. In contrast, tapinarof has no impact on imiquimod-induced skin inflammation in AhR-deficient mice.

Cell Research(from reference)

Cell lines：HaCaT cells 

Concentrations：0.01 pM - 1 μM 

Incubation Time：30 min 

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