DS-1040 Tosylate_product_DataBase

Bioactivity	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].
Target	IC50: 5.92 nM (human TAFIa) and 8.01 nM (rat TAFIa)
Invitro	DS-1040 Tosylate inhibits human carboxypeptidase N (CPN) in vitro with an IC50 of 3.02 mM[1].
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]. Animal Model:
Name	DS-1040 Tosylate
CAS	1335138-89-0
Formula	C23H35N3O5S
Molar Mass	465.61
Appearance	Solid
Transport	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)
Reference	[1]. Noguchi K, et al. Fibrinolytic potential of DS-1040, a novel orally available inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa). Thromb Res. 2018 Aug;168:96-101.

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