Tirofiban

製品コードS3085 バッチS308501

印刷

化学情報

Chemical Structure Synonyms MK-383 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C22H36N2O5S
分子量 440.6 CAS No. 144494-65-5
Solubility (25°C)* 体外 5%TFA 3.02 mg/mL (6.85 mM)
DMSO 0.005 mg/mL (0.01 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 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。

 0.15mg/ml (0.34mM) Taking the 1 mL working solution as an example, add 50 μL of 3 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 Tirofiban (MK-383) is a selective platelet GPIIb/IIIa antagonist which inhibits platelet aggregation with IC50 of 9 nM.
in vitro

Tirofiban (MK-383, Aggrastat) is a nonpeptide derivative of tyrosine that selectively inhibits the GP-IIb/IIIa receptor, with minimal effects on the ɑvβ3 vitronectin receptor. [1][2] This compound inhibits platelet aggregation of gel-filtered platelets induced by 10 μM ADP with IC50 of 9 nM, but the IC50 for inhibition of human umbilical vein adhesion to vitronectin, which depends on ɑvβ3 vitronectin receptors, is 62 μmol/L. [2]
in vivo

Tirofiban (10 to 500 mg/kg or 360-min continuous i.v. infusions of 1 to 10 micrograms/kg/min) inhibits platelet aggregation responses to ADP and collagen in canine models. [3] When administered to humans at 0.15μg/kg/min for 4 h, this compound produced a 2.5-fold increase in bleeding time and 97% inhibition of ADP-induced platelet aggregation. [4][5]

プロトコル(参考用のみ)

キナーゼアッセイ Binding assay
125 I-labeling of human fibrinogen is done usinglodogen reagent as described.22 Platelets are isolated from freshhuman blood drawn into acid/citrate/dextrose by differential centrifugation followed by gel filtration in a modified Tyrode buffer (pH 7.2) containing 2% bovine serum albumin, as previously described.23 Binding of 125I-fibrinogen (25 000 cpm/.g) to washed platelets is performed with 108 cells/mL in the presence of 0.5 mM calcium, 25 μM ADP, and this compound at the indicated concentration. After an incubation period of 30 minutes, the bound ligand is separated from the free ligand by centrifugation of 80-tuL aliquots of the reaction mixture through a 15% sucrose solution andis quantitated by measuring the radioactivity associated with platelets.

参考

  • http://www.ncbi.nlm.nih.gov/pubmed?term=1469694
  • http://www.ncbi.nlm.nih.gov/pubmed?term=8057299
  • https://eresources.library.mssm.edu/login?url=http://www.ncbi.nlm.nih.gov/pubmed?term=7815334
  • http://www.ncbi.nlm.nih.gov/pubmed?term=7955799
  • http://www.ncbi.nlm.nih.gov/pubmed?term=8403299

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：

Coenzyme Q10 attenuates platelet integrin αIIbβ3 signaling and platelet hyper-reactivity in ApoE-deficient mice. [ Food Funct, 2020, 11(1):139-152] PubMed: 31755492

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。