NSP-805

SKU: orb1309313

Description

NSP-805 is a selective phosphodiesterase 3 (PDE3) inhibitor characterized in guinea pig cardiac tissue. This small molecule research tool is used in vitro to study cardiac contractility and in vivo within cardiovascular disease models to investigate PDE3's role in cyclic nucleotide signaling.

Research Area

Metabolism Research

Key Properties

• CAS Number: 125068-54-4
• MW: 297.35
• Purity: 99.85% (May vary between batches)
• Formula: C₁₇H₁₉N₃O₂
• SMILES: CC1CC(=O)NN=C1c1ccc(NC2=C(C)C(=O)CC2)cc1
• Target: PDE
• Solubility: DMSO:20 mg/mL (67.26 mM)

Bioactivity

• In Vivo:
  In anesthetized dogs, intravenous (i.v.) injection of NSP-804 and NSP-805 produced dose-dependent increases in left ventricular VVdp/dtmax and decreases in aortic blood pressure (ABP) with relatively small increases in heart rate (HR). The ED50 values (micrograms/kg) for LVdP/dtmax of NSP-804, NSP-805, denopamine, milrinone, MCI-154, and indolidan were 15, 12, 22, 23, 15, and 7.3, respectively. When administered intraduodenally to anesthetized dogs, the ED50 values (micrograms/kg) for LVdP/dtmax of NSP-804, NSP-805, milrinone, and indolidan were approximately 30, 10, 200, and 25, respectively. In the propranolol-induced heart failure model, NSP-804 and NSP-805 completely normalized the hemodynamic state. The in vitro positive inotropic effects of NSP-804 and NSP-805 were accompanied by increases in tissue cyclic AMP and abolished by carbachol. NSP-805 was the most potent and selective inhibitor of guinea pig cardiac phosphodiesterase (PDE) III among the agents examined, while NSP-804 was a potent and selective inhibitor of PDE III similar to indolidan.
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• In Vitro:
  In isolated guinea pig left atria, the positive inotropic EC50 values (microM) ranked by potency were approximately 0.18 (NSP-805), 0.39 (indolidan), 1.1 (MCI-154), 1.7 (NSP-804, milrinone), 2.0 (denopamine), 4.0 (papaverine), 4.4 3-isobutyl-1-methylxanthine (IBMX), 6.5 (imazodan), and 27 (amrinone).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, PDE3, NSP805, NSP-805, NSP 805, Phosphodiesterase (PDE)

Compound Identifiers

PubChem CID

130349