产品描述
DS-1040 Tosylate is an oral active, selective thrombolytic inhibitor with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa, 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].
体外活性
Ds-1040 Tosylate inhibited human carboxypeptidase N (CPN) in vitro with an IC50 of 3.02 mM.
体内活性
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.
Cas No.
1335138-89-0
分子式
C23H35N3O5S
分子量
465.61
别名
DS-1040 Tosylate
储存和溶解度
H2O:100 mg/mL (214.77 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years