JJ1
JJ1 is a selective α-thrombin inhibitor with a Ki of 0.019 μM. JJ1 directly binds to the active site of α-thrombin to block its catalytic activity. JJ1 exhibits antithrombotic effects and prolongs activated partial thromboplastin time, prothrombin time, and tail bleeding time in mice. JJ1 can be used for the research of thrombotic diseases.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1225170-16-0
- 分子式: C18H19N5
- 分子量:305.39
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
α-thrombin 0.019 μM (Ki) |
体外実験
JJ1 (1 h) potently and selectively inhibits α-thrombin with a Ki value of 0.019 μM, and exhibits a selectivity of over 10000-fold against other tested human serine proteases[1].
JJ1 (0-2.5 μM; 1 min) inhibits the amidolytic activity of thrombin in a dose-dependent manner, with an IC50 value of 0.15 μM[1].
JJ1 (0-5 μM; 0-60 min) inhibits the activity of human thrombin bound to blood clots in a dose-dependent manner, with an IC50 of 2.45 μM[1].
JJ1 (0.5-5 μM; 1-10 min) dose-dependently inhibits thrombin-induced aggregation of washed platelets, with significant inhibitory effects observed at concentrations ≥0.5 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | AUC | T1/2 |
|---|---|---|---|---|
| Mice[1] | 2 mg/kg | i.v. | 6.1 μg·h/mL | 3.1 h |
体内実験
JJ1 (0.31-3.06 μg/mouse; intravenous injection; single administration) dose-dependently prolongs tail bleeding time, ex vivo activated partial thromboplastin time (aPTT), and ex vivo prothrombin time (PT) in healthy male C57BL/6 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 6-7 weeks old, 27 g, ferric chloride-induced arterial thrombosis model)[1]
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Dosage:0.61 μg/mouse; 1.23 μg/mouse; 3.06 μg/mouse
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Administration:i.v.; single dose
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Result:Significantly slowed thrombus growth.
Reduced thrombus size score.
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Animal Model:C57BL/6 (male, 6-7 weeks old, 27 g)[1]
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Dosage:0.31 μg/mouse; 0.61 μg/mouse; 1.23 μg/mouse; 3.06 μg/mouse
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Administration:i.v.; single dose
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Result:Prolonged tail bleeding time to 37.2 seconds at 0.61 μg/mouse, 44.8 seconds at 1.23 μg/mouse, and 52.2 seconds at 3.06 μg/mouse (control time was 30.2 seconds).
Prolonged ex vivo aPTT to 40.1 seconds at 0.61 μg/mouse, 49.4 seconds at 1.23 μg/mouse, and 55.8 seconds at 3.06 μg/mouse (control aPTT was 32.1 seconds).
Prolonged ex vivo PT to 17.2 seconds at 0.61 μg/mouse, 22.3 seconds at 1.23 μg/mouse, and 26.8 seconds at 3.06 μg/mouse (control PT was 12.0 seconds).
化学情報
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CAS 番号 1225170-16-0
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分子量 305.39
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分子式 C18H19N5
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SMILES
N=1C=CC(=CC1)NC=2N=C3C=CC=CC3=C(N2)NC4CCCC4
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
JJ1 関連分類
HY-165360 関連分類
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Keywords
- JJ1
- 1225170-16-0
- JJ 1
- JJ-1
- Thrombin
- serine proteases
- collagen + epinephrine-induced acute pulmonary thrombosis model
- human α-thrombin
- human plasma
- endothelial cells
- thrombotic disorders
- ferric chloride-induced arterial thrombosis model
- human umbilical vein endothelial cells
- C57BL/6 mice
- human platelets
- Inhibitor
- inhibitor
- inhibit