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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Tapinarof
Dangerous GoodsCAS number:79338-84-4 molecular formula:C17H18O2
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compound introduction
Specs
| Chinese alias | 本维莫德 | (E)-2-异丙基-5-苯乙烯基苯-1,3-二醇 | 2-异丙基-5-[(E)-2-苯基乙烯基]-1,3-苯二醇 | ||
| English alias | 5-((1E)-2-PHENYLETHEN-1-YL)-2-(PROPAN-2-YL)BENZENE-1,3-DIOL | Tapinarof (USAN) | 5-[(1E)-2-Phenylethen-1-yl]-2-(propan-2-yl)benzene-1,3-diol | GTPL9686 | AKOS025296109 | s9700 | TAPINAROF [INN] | BCP13569 | Sinefunginum [INN-Latin] | 2-Isopropyl-5-styrylb | ||
| CAS number | 79338-84-4 | molecular formula | C17H18O2 |
| molecular weight | 254.32 g/mol | Exact mass | - |
| PSA | 40.500 Ų | logp | 4.526 |
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physicochemical properties
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Safety information
pictogram:
GHS09
Signal word:
Warning
Hazard Statement:
H400: 对水生生物有剧毒 H410: 对水生生物有剧毒并具有长期持续影响
Statement of Preventive Measures:
P273: 避免释放到环境中。 P501: 将内容物/容器处理到。。。 P391: 收集溢出物
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