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DS-1040 tosylate

CAS No. 1335138-89-0

DS-1040 tosylate( DS 1040 | DS1040 )

Catalog No. M11340 CAS No. 1335138-89-0

DS-1040 tosylate (DS1040) is a small molecule inhibitor of the activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50 of 1.7 ng/mL for rabbit TAFIa.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    DS-1040 tosylate
  • Note
    Research use only, not for human use.
  • Brief Description
    DS-1040 tosylate (DS1040) is a small molecule inhibitor of the activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50 of 1.7 ng/mL for rabbit TAFIa.
  • Description
    DS-1040 tosylate (DS1040) is a small molecule inhibitor of the activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50 of 1.7 ng/mL for rabbit TAFIa; a novel fibrinolysis-enhancing agent has favorable pharmacokinetic/pharmacodynamic properties and a favorable safety profile.Stroke Phase 2 Clinical.
  • In Vitro
    DS-1040 Tosylate inhibits human carboxypeptidase N (CPN) in vitro with an IC50 of 3.02 mM.
  • 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. 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. 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. Animal Model:Male Slc:Wistar rats 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.
  • Synonyms
    DS 1040 | DS1040
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Other Targets
  • Research Area
    Neurological Disease
  • Indication
    Stroke

Chemical Information

  • CAS Number
    1335138-89-0
  • Formula Weight
    465.609
  • Molecular Formula
    C23H35N3O5S
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (214.77 mM)
  • SMILES
    CC1CCC(CC1)N2C=C(N=C2)CC(CCCN)C(=O)O.CC1=CC=C(C=C1)S(=O)(=O)O
  • Chemical Name
    (S)-5-amino-2-((1-((1r,4S)-4-methylcyclohexyl)-1H-imidazol-4-yl)methyl)pentanoic acid compound with 4-methylbenzenesulfonic acid (1:1)

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Zhou J, et al. J Thromb Haemost. 2017 May;15(5):961-971. 2. Gurewich V, et al. J Thromb Haemost. 2017 Oct;15(10):2080-2081. 3. Paul A Lapchak, et al. Abstract WP282: DS-1040 an Inhibitor of the Activated Thrombin Activatable Fibrinolysis Inhibitor Improves Behavior in Embolized Rabbits, Stroke. 2016;47:AWP282.
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