For research use only.
Catalog No.S9700 Synonyms: GSK2894512, Benvitimod, WBI 1001, DHPS, DMVT 505
CAS No. 79338-84-4
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.
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|Description||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.|
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.
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.
|In vitro||DMSO||51 mg/mL (200.53 mM)|
|Ethanol||51 mg/mL (200.53 mM)|
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|Synonyms||GSK2894512, Benvitimod, WBI 1001, DHPS, DMVT 505|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04634695||Recruiting||--||Pregnancy Malaria||Obafemi Awolowo University|University of Copenhagen|LSHTM|European and Developing Countries Clinical Trials Partnership (EDCTP)||August 10 2020||--|
|NCT04042103||Completed||Drug: Tapinarof cream 1%||Plaque Psoriasis||Dermavant Sciences GmbH||July 23 2019||Phase 2|
|NCT02637206||Completed||Drug: GSK2894512 Cream|Drug: Vehicle Cream|Drug: Empty Patch||Dermatitis Atopic||GlaxoSmithKline||October 27 2015||Phase 1|
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