Acitretin

製品コードS1368 バッチS136804

印刷

化学情報

Chemical Structure Synonyms Etretin, RO 10-1670 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C21H26O3
分子量 326.43 CAS No. 55079-83-9
Solubility (25°C)* 体外 DMSO 65 mg/mL (199.12 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 1.600mg/ml (4.90mM) Taking the 1 mL working solution as an example, add 50 μL of 32 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. 
Clear solution
5% DMSO 95% Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 0.130mg/ml (0.40mM) Taking the 1 mL working solution as an example, add 50 μL of 2.6 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. 
* <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 Acitretin (Etretin, RO 10-1670) is a second generation retinoid used for psoriasis.
in vitro Acitretin stimulates ADAM10 promoter activity with an EC(50) of 1.5 mM and leads to an increase of mature ADAM10 protein that results in a two- to three-fold increase of the ratio between alpha- and beta-secretase activity in neuroblastoma cells. [1] This compound (5-20 μM) impairs mitochondrial phosphorylation efficiency as demonstrated by the decrease in the state 3 respiration and ATP levels, and by the increase in the lag phase of ADP phosphorylation cycle, without affecting the membrane potential. It induces Ca(2+)-mediated mitochondrial permeability transition (MPT) and decreased the adenine nucleotide translocase (ANT) content. [2] The chemical preferentially inhibits the growth of SCL-1 cells in a dose- and time-dependent manner, but not of non-malignant keratinocyte HaCaT cells. It increases the levels of CD95 (Fas), CD95-ligand and Fas-associated death domain. It is able to induce apoptosis in skin cancer cells possibly via death receptor CD95 apoptosis pathway without affecting the viability of normal keratinocyte. [3]
in vivo Acitretin undergoes alpha-oxidation, chain shortening O-demethylation, and glucuronidation in the perfused rat liver. [4] This compound rapidly appears in liver and muscle of rats, where it undergoes redistribution into skin and adipose tissue. [5]

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/19144697/
  • https://pubmed.ncbi.nlm.nih.gov/23384448/
  • https://pubmed.ncbi.nlm.nih.gov/18624760/
  • https://pubmed.ncbi.nlm.nih.gov/1492415/
  • https://pubmed.ncbi.nlm.nih.gov/8149885/

カスタマーフィードバック

Data from [Data independently produced by , , Antimicrob Agents Chemother, 2016, 61(11). pii: e01368-17]

Data from [Data independently produced by , , Saudi Pharm J, 2017, 25(4):620-624]

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：

Isolation of Reporter Cells That Respond to Vitamin A and/or D Using a piggyBac Transposon Promoter-Trapping Vector System [ Int J Mol Sci, 2022, 23(16)9366] PubMed: 36012634
Acitretin mitigates uroporphyrin-induced bone defects in congenital erythropoietic porphyria models [ Sci Rep, 2021, 11(1):9601] PubMed: 33953217
Evaluation of the Innate Immune Modulator Acitretin as a Strategy To Clear the HIV Reservoir. [Garcia-Vidal E, et al. Antimicrob Agents Chemother, 2017, 61(11). pii: e01368-17] PubMed: 28874382
Acitretin modulates HaCaT cells proliferation through STAT1- and STAT3-dependent signaling. [Qin X, et al. Saudi Pharm J, 2017, 25(4):620-624] PubMed: 28579901

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。