| CAS NO: | 79338-84-4 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Name: Benvitimod CAS#: 79338-84-4 Chemical Formula: C17H18O2 Exact Mass: 254.1307 Molecular Weight: 254.329 | |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Technical Information | Synonym: WBI-1001; Benvitimod; GSK 2894512; WB1001; GSK2894512; WBI 1001; GSK-2894512; 3,5-DH4IS; tapinarof Chemical Name: 3,5-Dihydroxy-4-isopropylstilbene InChi Key: ZISJNXNHJRQYJO-CMDGGOBGSA-N InChi Code: InChI=1S/C17H18O2/c1-12(2)17-15(18)10-14(11-16(17)19)9-8-13-6-4-3-5-7-13/h3-12,18-19H,1-2H3/b9-8+ SMILES Code: CC(C1=C(O)C=C(C=C1O)/C=C/C2=CC=CC=C2)C |
| Target | EC50: 13 nM (AhR)[1] |
|---|---|
| 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)[1]. |
| 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[1]. |
| Cell Assay | HaCaT cells (10,000 cells/well) are cultured in 96-well Greiner μCLEAR plates in 100 μL DMEM with HEPES, Glutamax and 10% fetal bovine serum to confluence. Media is replaced with 100 μL media containing 0.2% heat-inactivated, charcoal-stripped fetal bovine serum and incubated overnight. Titrating concentrations of Tapinarof (10-8 μM ,10-6 μM, 10-4 μM, 0.01 μM, and 1 μM) are added for 30 minutes followed by washing and fixing in ice-cold methanol:acetone (50:50). Samples are blocked with 3% BSA for 1 hour, and then washed again in phosphate buffered saline with 0.1% Tween-20. Next, cells are stained with 50 μL of 1:50 dilution anti-AhR antibody in 3% BSA, followed by 50 μL secondary antibody (1:500 dilution chicken anti-rabbit AlexaFluor488 and 1:2,000 dilution Hoechst 33342) in 3% BSA/phosphate buffered saline. Images are acquired on InCell 2000 and/or Opera. Image analysis is performed using InCell Analyzer Workstation and/or Columbus[1]. |
| Animal Protocol | Mice[1] Female BALB/c mice (BALB/cByJRj) are used. Studies are performed using 100 μL of Tapinarof (1%) or FICZ (0.01%, at the limit of solubility) in 60% ethanol: 40% water[1]. |
| References | [1]. Tapinarof Is a Natural AhR Agonist that Resolves Skin Inflammation in Mice and Humans. J Invest Dermatol. 2017 Oct;137(10):2110-2119 |
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