1. Metabolic Enzyme/Protease
  2. Thrombin
  3. JJ1

JJ1 是一种选择性 α-thrombin 抑制剂,其 Ki 为 0.019 μM。JJ1 可直接结合 α-凝血酶的活性位点以阻断其催化活性。JJ1 具有抗血栓作用,可延长活化部分凝血活酶时间、凝血酶原时间及小鼠的尾部出血时间。JJ1 可用于血栓性疾病的研究。

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JJ1

JJ1 Chemical Structure

CAS No. : 1225170-16-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1].

IC50 & Target[1]

α-thrombin

0.019 μM (Ki)

体外研究
(In Vitro)

JJ1 (1 h) 可强效且选择性抑制 α-凝血酶,其 Ki 值为 0.019 μM,对其他受试人丝氨酸蛋白酶的选择性可达 10000 倍以上[1]
JJ1 (0-2.5 μM; 1 min) 可剂量依赖性地抑制凝血酶的酰胺水解活性,其 IC50 为 0.15 μM[1]
JJ1 (0-5 μM; 0-60 min) 可呈剂量依赖性抑制结合于血凝块的人凝血酶活性,其 IC50 为 2.45 μM[1]
JJ1 (0.5-5 μM; 1-10 min) 可剂量依赖性地抑制凝血酶诱导的洗涤血小板聚集,在浓度 ≥0.5 μM 时观察到显著抑制作用[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

药代动力学
(Parmacokinetics)
Species Dose Route AUC T1/2
Mice[1] 2 mg/kg i.v. 6.1 μg·h/mL 3.1 h
体内研究
(In Vivo)

JJ1 (0.61-3.06 μg/mouse;静脉注射;单次) 在小鼠氯化铁诱导的动脉血栓形成模型中剂量依赖性地延迟大血栓形成时间并使血栓大小降低[1]
JJ1 (0.31-3.06 μg/mouse;静脉注射;单次) 可在健康雄性 C57BL/6 小鼠中呈剂量依赖性延长尾部出血时间,ex vivo 活化部分凝血活酶时间 (aPTT),ex vivo 凝血酶原时间 (PT)[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (male, 6-7 weeks old, 27 g, ferric chloride-induced arterial thrombosis model)[1]
Dosage: 0.61 μg/mouse; 1.23 μg/mouse; 3.06 μg/mouse
Administration: i.v.; single dose
Result: Significantly slowed thrombus growth.
Reduced thrombus size score.
Animal Model: C57BL/6 (male, 6-7 weeks old, 27 g)[1]
Dosage: 0.31 μg/mouse; 0.61 μg/mouse; 1.23 μg/mouse; 3.06 μg/mouse
Administration: i.v.; single dose
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).
分子量

305.39

Formula

C18H19N5

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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JJ1
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HY-165360
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