Capadenoson

Capadenoson is an orally bioavailable, non-nucleoside adenosine (A) receptor partial agonist. It binds selectively to human A1 and A2B (EC50s = 0.66 and 1.1 nM, respectively) over A2A and A3 receptors (EC50s = 1,413 and 240 nM, respectively) expressed in CHO cells. Capadenoson (0.6 µM) decreases electrical field-stimulated norepinephrine (Cay-16673) release from isolated perfused hearts from spontaneously hypertensive rats (SHR) but not from control rats. It does not affect baseline heart rate but protects against stress-induced increases in heart rate in SHR but not control rats when administered at a dose of 0.15 mg/kg for 5 days prior to stress induction. Capadenoson (0.1 mg/kg) decreases cardiac infarct size from 28.7 to 22% in a mouse model of ischemia induced by left anterior descending artery (LAD) occlusion. Capadenoson (7.5 mg twice per day) also increases the left ventricular ejection fraction (LVEF) in a dog model of microembolization-induced heart failure.Formal Name: 2-amino-6-[[[2-(4-chlorophenyl)-4-thiazolyl]methyl]thio]-4-[4-(2-hydroxyethoxy)phenyl]-3,5-pyridinedicarbonitrile. CAS Number: 544417-40-5. Synonyms: BAY 68-4986. Molecular Formula: C25H18ClN5O2S2. Formula Weight: 520.0. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. lambdamax: 295, 346 nm. SMILES: NC1=NC(SCC2=CSC(C3=CC=C(Cl)C=C3)=N2)=C(C#N)C(C4=CC=C(OCCO)C=C4)=C1C#N. InChi Code: InChI=1S/C25H18ClN5O2S2/c26-17-5-1-16(2-6-17)24-30-18(13-34-24)14-35-25-21(12-28)22(20(11-27)23(29)31-25)15-3-7-19(8-4-15)33-10-9-32/h1-8,13,32H,9-10,14H2,(H2,29,31). InChi Key: CITWCLNVRIKQAF-UHFFFAOYSA-N.