An orally bioavailable

Capadenoson – 10 mg

Brand:
Cayman
CAS:
544417-40-5
Storage:
-20
UN-No:
Non-Hazardous - /

Capadenoson is an orally bioavailable, non-nucleoside adenosine (A) receptor partial agonist.{45534,45535} 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.{45534} Capadenoson (0.6 μM) decreases electrical field-stimulated norepinephrine (Item No. 16673) release from isolated perfused hearts from spontaneously hypertensive rats (SHR) but not from control rats.{50106} 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.{45535} Capadenoson (7.5 mg twice per day) also increases the left ventricular ejection fraction (LVEF) in a dog model of microembolization-induced heart failure.{45536}  

 

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Description

An orally bioavailable, non-nucleoside partial adenosine receptor agonist; 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; decreases electrical field-stimulated norepinephrine release from isolated perfused hearts from SHR but not from control rats at 0.6 μM; protects against stress-induced increases in heart rate in SHR but not control rats at 0.15 mg/kg for 5 days prior to stress induction; decreases cardiac infarct size from 28.7 to 22% in a LAD-induced ischemia mouse model at 0.1 mg/kg; increases LVEF in a microembolization-induced heart failure dog model at 7.5 mg twice daily

Formal name: 2-amino-6-[[[2-(4-chlorophenyl)-4-thiazolyl]methyl]thio]-4-[4-(2-hydroxyethoxy)phenyl]-3,5-pyridinedicarbonitrile

Synonyms:  BAY 68-4986

Molecular weight: 520

CAS: 544417-40-5

Purity: ≥98%

Formulation: A solid

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