DS-1040 Tosylate

• CAT Number: I013219
• CAS Number: 1335138-89-0
• Molecular Formula: C23H35N3O5S
• Molecular Weight: 465.61
• Purity: ≥95%
• Synonyms: (2S)-5-amino-2-[[1-(4-methylcyclohexyl)imidazol-4-yl]methyl]pentanoic acid;4-methylbenzenesulfonic acid
• InChI: InChI=1S/C16H27N3O2.C7H8O3S/c1-12-4-6-15(7-5-12)19-10-14(18-11-19)9-13(16(20)21)3-2-8-17;1-6-2-4-7(5-3-6)11(8,9)10/h10-13,15H,2-9,17H2,1H3,(H,20,21);2-5H,1H3,(H,8,9,10)/t12?,13-,15?;/m0./s1
• InChIKey: BEUWOXSXOMMLGF-JYGFLIHTSA-N
• SMILES: CC1CCC(CC1)N2C=C(N=C2)CC(CCCN)C(=O)O.CC1=CC=C(C=C1)S(=O)(=O)O

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

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.
 [Content Brief]