1. Metabolic Enzyme/Protease
  2. Thrombin
  3. Thrombin inhibitor 11

Thrombin inhibitor 11 is an orally active, competitive and selective α-Thrombin inhibitor, with a Ki value of 65 nM against h-αThrombin and a Ki value of 10.3 nM against rat-derived α-thrombin. Thrombin inhibitor 11 can be used for the research of thrombotic diseases.

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

Thrombin inhibitor 11

Thrombin inhibitor 11 Chemical Structure

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Description

Thrombin inhibitor 11 is an orally active, competitive and selective α-Thrombin inhibitor, with a Ki value of 65 nM against h-αThrombin and a Ki value of 10.3 nM against rat-derived α-thrombin. Thrombin inhibitor 11 can be used for the research of thrombotic diseases[1].

In Vitro

Thrombin inhibitor 11 (Compound 46) inhibits h-αThrombin (Ki = 65 nM) and rat α-Thrombin (Ki = 10.3 nM)[1].
Thrombin inhibitor 11 (8 h) exhibits high proteolytic stability in simulated gastric fluid and simulated intestinal fluid[1].

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

Parmacokinetics
Species Dose Route Cmax Bioavailability
Rat[1] 10 mg/kg p.o. 400 nM 18.4 %
In Vivo

Thrombin inhibitor 11 (1-10 mg/kg; intravenous injection, oral administration; single dose) has an oral bioavailability of 18.4% in male Wistar Han rats, and its peak plasma concentration reaches 400 nM after a single oral gavage dose of 10 mg/kg[1].

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

Animal Model: Wistar Han (male, 10-11 weeks old, 250-350 g)[1]
Dosage: 1 mg/kg; 10 mg/kg
Administration: i.v.; single dose; p.o.; single dose
Result: Reached a maximal plasma concentration (Cmax) of 400 nM after oral administration.
Achieved an absolute oral bioavailability of 18.4%.
Molecular Weight

579.13

Formula

C32H39ClN4O4

Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC=C(C(N[C@H](C(N[C@@H](CC2=CC=CC=C2)C(N3[C@@H](C4)CCC3)=O)=O)CC/C=C/CCCCNC4=O)=O)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (172.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7267 mL 8.6336 mL 17.2673 mL
5 mM 0.3453 mL 1.7267 mL 3.4535 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7267 mL 8.6336 mL 17.2673 mL 43.1682 mL
5 mM 0.3453 mL 1.7267 mL 3.4535 mL 8.6336 mL
10 mM 0.1727 mL 0.8634 mL 1.7267 mL 4.3168 mL
15 mM 0.1151 mL 0.5756 mL 1.1512 mL 2.8779 mL
20 mM 0.0863 mL 0.4317 mL 0.8634 mL 2.1584 mL
25 mM 0.0691 mL 0.3453 mL 0.6907 mL 1.7267 mL
30 mM 0.0576 mL 0.2878 mL 0.5756 mL 1.4389 mL
40 mM 0.0432 mL 0.2158 mL 0.4317 mL 1.0792 mL
50 mM 0.0345 mL 0.1727 mL 0.3453 mL 0.8634 mL
60 mM 0.0288 mL 0.1439 mL 0.2878 mL 0.7195 mL
80 mM 0.0216 mL 0.1079 mL 0.2158 mL 0.5396 mL
100 mM 0.0173 mL 0.0863 mL 0.1727 mL 0.4317 mL
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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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Product Name:
Thrombin inhibitor 11
Cat. No.:
HY-162109
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