Tapinarof

製品コードS9700 バッチS970001

印刷

化学情報

Synonyms

GSK2894512, Benvitimod, WBI 1001, DHPS, DMVT 505

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₁₇H₁₈O₂

分子量

254.32

CAS No.

79338-84-4

Solubility (25°C)*

体外

DMSO

51 mg/mL (200.53 mM)

Ethanol

51 mg/mL (200.53 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution	5% DMSO 1 95% Corn oil	0.85mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 17 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	2.5mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	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.
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.^[1]
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.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HaCaT cells
	濃度	0.01 pM - 1 μM
	反応時間	30 min
	実験の流れ	HaCaT cells (10,000 cells/well) are cultured in 96-well plates in 100 μL DMEM with HEPES, Glutamax and 10% FBS to confluence. Media is replaced with 100 μl media containing 0.2% heat-inactivated, charcoal-stripped FBS and incubated overnight. Titrating concentrations of tapinarof 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, then washed again in PBS with 0.1% Tween-20. Next, cells are stained with 50μL of 1:50 dilution anti-AhR antibody in 3% BSA, followed by 50 μl secondary antibody in 3% BSA/PBS.
動物実験	動物モデル	8 week-old BALB/c JByRj female mice
	投薬量	0.1%, 0.3%, 1%
	投与方法	Topical

参考

[1] Susan H Smith, et al. J Invest Dermatol. 2017 Oct;137(10):2110-2119.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

The Highly Potent AhR Agonist Picoberin Modulates Hh-Dependent Osteoblast Differentiation [ J Med Chem, 2022, 2]	PubMed: 36459434
A whole genome CRISPR screen identifies AHR loss as a mechanism of PARP7 inhibitor resistance [ Mol Cancer Ther, 2022, molcanther.0841.2021]	PubMed: 35439318

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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