Benvitimod

SKU: orb1223993

Description

A natural aryl hydrocarbon receptor (AhR) agonist with anti-inflammatory properties; binds and activates AhR in multiple cell types, 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; shows no impact on imiquimod-induced skin inflammation in AhR-deficient mice.Psoriasis Phase 3 Clinical(In Vitro):Tapinarof activates the AhR pathway through direct binding. Tapinarof dose-dependently induces nuclear translocation of AhR in immortalized keratinocytes (HaCaT) (EC50=0.16 nM).(In Vivo):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). In contrast, 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.

Key Properties

• CAS Number: 79338-84-4
• MW: 254.329
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₈O₂
• SMILES: CC(C1=C(O)C=C(C=C1O)/C=C/C2=CC=CC=C2)C
• Target: AhR
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  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). In contrast, 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.
• In Vitro:
  Tapinarof activates the AhR pathway through direct binding. Tapinarof dose-dependently induces nuclear translocation of AhR in immortalized keratinocytes (HaCaT) (EC50 = 0.16 nM).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

WBI-1001 | WB-1001 | GSK-2894512 | Tapinarof

Quick Database Links

Gene Symbol

AhR