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  3. DS-1040 Tosylate

DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.

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

DS-1040 Tosylate Chemical Structure

DS-1040 Tosylate Chemical Structure

CAS No. : 1335138-89-0

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 209 In-stock
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10 mg USD 325 In-stock
50 mg USD 970 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases[1].

IC50 & Target

IC50: 5.92 nM (human TAFIa) and 8.01 nM (rat TAFIa)[1]

In Vitro

DS-1040 Tosylate inhibits human carboxypeptidase N (CPN) in vitro with an IC50 of 3.02 mM[1].

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

In Vivo

DS-1040 Tosylate (0.0005-0.5 mg/kg; IV) significantly reduces the microthrombi index at doses of 0.005 mg/kg and greater[1].
DS1040 (0.016, 0.031, 0.063, 0.13, 0.25, 0.50 mg/kg; i.v.) increases plasma D-dimer levels in a dose-dependent manner in the microthrombosis model. ED50 and EDmax are 122 and 221 nmol/L, respectively[1].
DS-1040 (0.25, 0.5, 1, 2, 4, 8, 16 mg/kg; orally) also increases plasma D-dimer levels. EC50 and ECmax values are 114 and 231 nmol/L, respectively[1].

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

Animal Model: Male Slc:Wistar rats[1]
Dosage: 0.0005, 0.005, 0.05, 0.5 mg/kg
Administration: IV
Result: Significantly reduced the microthrombi index at doses of 0.005 mg/kg and greater.
Molecular Weight

465.61

Formula

C23H35N3O5S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)[C@H](CC1=CN([C@H]2CC[C@H](C)CC2)C=N1)CCCN.CC3=CC=C(S(=O)(O)=O)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (214.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 50 mg/mL (107.39 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1477 mL 10.7386 mL 21.4772 mL
5 mM 0.4295 mL 2.1477 mL 4.2954 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (10.74 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (10.74 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (214.77 mM); Clear solution; Need ultrasonic

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
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
H2O / DMSO 1 mM 2.1477 mL 10.7386 mL 21.4772 mL 53.6930 mL
5 mM 0.4295 mL 2.1477 mL 4.2954 mL 10.7386 mL
10 mM 0.2148 mL 1.0739 mL 2.1477 mL 5.3693 mL
15 mM 0.1432 mL 0.7159 mL 1.4318 mL 3.5795 mL
20 mM 0.1074 mL 0.5369 mL 1.0739 mL 2.6847 mL
25 mM 0.0859 mL 0.4295 mL 0.8591 mL 2.1477 mL
30 mM 0.0716 mL 0.3580 mL 0.7159 mL 1.7898 mL
40 mM 0.0537 mL 0.2685 mL 0.5369 mL 1.3423 mL
50 mM 0.0430 mL 0.2148 mL 0.4295 mL 1.0739 mL
60 mM 0.0358 mL 0.1790 mL 0.3580 mL 0.8949 mL
80 mM 0.0268 mL 0.1342 mL 0.2685 mL 0.6712 mL
100 mM 0.0215 mL 0.1074 mL 0.2148 mL 0.5369 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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DS-1040 Tosylate Related Classifications

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  • 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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DS-1040 Tosylate
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