Tapinarof-WBI-1001-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETapinarofCat. No.: HY-109044CAS No.: 79338-84-4Synonyms: WBI 1001; Benvitimod; GSK2894512分式: CHO分量: 254.32作靶点: Aryl Hydrocarbon Receptor作通路: Immunology/Inflammation储存式: 4C, protect from light* In solvent : -80C, 6 months; -20C,

2、1 month (protect fromlight)溶解性数据体外实验 DMSO : 125 mg/mL (491.51 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.9321 mL 19.6603 mL 39.3205 mL5 mM 0.7864 mL 3.9321 mL 7.8641 mL10 mM 0.3932 mL 1.9660 mL 3.9321 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。

3、体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (9.83 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL

4、 (9.83 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (9.83 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Tapinarof种天然的芳烃受体 (AhR) 激动剂，EC50 为 13 nM。IC50 & Target EC50: 13 nM (AhR) 1体外研究 Tapinarof activates the AhR pathway throu

5、gh direct binding. Tapinarof dose-dependently induces nucleartranslocation of AhR in immortalized keratinocytes (HaCaT) (EC50=0.16 nM) 1.体内研究 Tapinarof acts through AhR to reduce inflammation in IMQ-treated mice. AhR-sufficient mice on a C57Bl/6background exhibit a reduced clinical score after treat

6、ment 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 usedas a comparator in these studies and yields similar results, with dramatically reduced inflammatoryresponses in wild-type, but not AhR KO mi

7、ce 1.PROTOCOLCell Assay 1 HaCaT cells (10,000 cells/well) are cultured in 96-well Greiner CLEAR plates in 100 L DMEM with HEPES,Glutamax and 10% fetal bovine serum to confluence. Media is replaced with 100 L media containing 0.2%heat-inactivated, charcoal-stripped fetal bovine serum and incubated ov

8、ernight. Titrating concentrations ofTapinarof (10-8 M ,10-6 M, 10-4 M, 0.01 M, and 1 M) are added for 30 minutes followed by washingand fixing in ice-cold methanol:acetone (50:50). Samples are blocked with 3% BSA for 1 hour, and thenwashed again in phosphate buffered saline with 0.1% Tween-20. Next,

9、 cells are stained with 50 L of 1:50dilution anti-AhR antibody in 3% BSA, followed by 50 L secondary antibody (1:500 dilution chicken anti-rabbit AlexaFluor488 and 1:2,000 dilution Hoechst 33342) in 3% BSA/phosphate buffered saline. Images areacquired on InCell 2000 and/or Opera. Image analysis is p

10、erformed using InCell Analyzer Workstation and/orColumbus 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 1Administration 1 Female BALB/c mice (BALB/cByJRj) are used. Studies are performed using 100 L of Tapinarof (1%) orFICZ (0.01%, at th

11、e limit of solubility) in 60% ethanol: 40% water 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Smith SH, et al. Tapinarof Is a Natural AhR Agonist that Resolves Skin Inflammation in Mice and Humans. J Invest Dermatol. 2017Oct;137(10):2110-2119.McePdfHeight2/2 Master of Small Molecules 您边的抑制剂师www.MedChemECaution: Product has n