Mizoribine

製品コードS1384 バッチS138408

印刷

化学情報

 Chemical Structure Synonyms NSC 289637,HE 69 Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C9H13N3O6

分子量 259.22 CAS No. 50924-49-7
Solubility (25°C)* 体外 DMSO 52 mg/mL (200.6 mM)
Water 52 mg/mL (200.6 mM)
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。

2.600mg/ml (10.03mM) Taking the 1 mL working solution as an example, add 50 μL of 52 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。

2.600mg/ml (10.03mM) Taking the 1 mL working solution as an example, add 50 μL of 52 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 Mizoribine is an imidazole nucleoside and an immunosuppressant that inhibits HCV RNA replication with IC50 of ~ 100 μM for anti-HCV activity. Mizoribine is a selective inhibitor of inosine-5'-monophosphate dehydrogenase (IMPDH) and guanosine monophosphate synthetase. Mizoribine also inhibits SARS-CoV.
in vitro

Mizoribine (1-50 mg/mL) is able to inhibit T cell proliferation by 10-100% in a dose-dependent fashion to all stimuli tested. This compound leads to a decrease in intracellular GTP levels, and that repletion of GTP reversed its antiproliferative effects. [1] It causes a dose-dependent inhibition of T cell proliferation, which is reversible with the addition of 50 mM guanosine to replete guanine ribonucleotide pools. This chemical selectively inhibits guanine ribonucleotide formation in purified T cells, whereas the effect of 6-mercaptopurine (6MP) appears to be more dependent on adenine ribonucleotide depletion. [2] It inhibits HCV RNA replication with IC50 of 100 μM. [3]

in vivo

Mizoribine (5 or 10 mg/kg) suppresses urinary albumin excretion in the rats. This compound inhibits the development of glomerulosclerosis, interstitial fibrosis and macrophage infiltration in the kidney in the rats. It increases the expression of MCP-1, OPN and TGF-β1 mRNA in untreated OLETF rats. [4]

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/1999502/
  • https://pubmed.ncbi.nlm.nih.gov/1569921/
  • https://pubmed.ncbi.nlm.nih.gov/15809077/
  • https://pubmed.ncbi.nlm.nih.gov/15905195/

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:

IDH2 stabilizes HIF-1α-induced metabolic reprogramming and promotes chemoresistance in urothelial cancer [ EMBO J, 2023, e110620.] PubMed: 36637036
Unmasking the Role of SARS-CoV-2 Nsp14 on the Host Cell Gene Expression Changes and Adapting Cas13 to Drosophila melanogaster [ ProQuest, 2023, ] PubMed: None
Unmasking the Role of SARS-CoV-2 Nsp14 on the Host Cell Gene Expression Changes and Adapting Cas13 to Drosophila melanogaster [ The Faculty of the Graduate School of Arts and Sciences Brandeis University, 2023, ] PubMed: None
Unmasking the Role of SARS-CoV-2 Nsp14 on the Host Cell Gene Expression Changes and Adapting Cas13 toDrosophila melanogaster [ Brandeis University, 2023, ] PubMed: None
SARS-CoV-2 Nsp14 mediates the effects of viral infection on the host cell transcriptome [ bioRxiv, 2022, 2021.07.02.450964] PubMed: 35194610
Stress-induced inflammation evoked by immunogenic cell death is blunted by the IRE1α kinase inhibitor KIRA6 through HSP60 targeting [ Cell Death Differ, 2021, 10.1038/s41418-021-00853-5] PubMed: 34453119
Stress-induced inflammation evoked by immunogenic cell death is blunted by the IRE1α kinase inhibitor KIRA6 through HSP60 targeting [ Cell Death Differ, 2021, 10.1038/s41418-021-00853-5] PubMed: 34453119
IMPDH Inhibitors for Antitumor Therapy in Tuberous Sclerosis Complex [ JCI Insight, 2020, 9;5(7):e135071] PubMed: 32271165
mTORC1 Couples Nucleotide Synthesis to Nucleotide Demand Resulting in a Targetable Metabolic Vulnerability. [ Cancer Cell, 2017, 32(5):624-638] PubMed: 29056426

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。