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DS-1040 Tosylate 

Cat. No.: HY-101918
Handling Instructions

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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10 mM * 1 mL in DMSO USD 209 In-stock
Estimated Time of Arrival: December 31
5 mg USD 190 In-stock
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10 mg USD 325 In-stock
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50 mg USD 970 In-stock
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100 mg USD 1650 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].

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].

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.

1335138-89-0

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (214.77 mM; Need ultrasonic)

H2O : 100 mg/mL (214.77 mM; Need ultrasonic)

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
10 mM 0.2148 mL 1.0739 mL 2.1477 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

DS-1040DS1040DS 1040Othersorallythrombin-activatablefibrinolysisinhibitorTAFIathromboembolicdiseasesInhibitorinhibit

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Product Name:
DS-1040 Tosylate
Cat. No.:
HY-101918
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