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

For research use only. We do not sell to patients.

JJ1

JJ1 Chemical Structure

CAS No. : 1225170-16-0

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Description

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)

In Vitro

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
In Vivo

JJ1 (0.61-3.06 μg/mouse; intravenous injection; single administration) dose-dependently delays the time to large thrombus formation and reduces thrombus size in a mouse model of ferric chloride-induced arterial thrombosis[1].
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.

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).
Molecular Weight

305.39

Formula

C18H19N5

CAS No.
SMILES

N=1C=CC(=CC1)NC=2N=C3C=CC=CC3=C(N2)NC4CCCC4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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    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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