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NSP-805

Catalog No. T12267   CAS 125068-54-4

NSP-805 is a potent and selective guinea pig cardiac phosphodiesterase 3 (PDE3) inhibitor.

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NSP-805 Chemical Structure
NSP-805, CAS 125068-54-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 80.00
2 mg In stock $ 118.00
5 mg In stock $ 197.00
10 mg In stock $ 337.00
25 mg In stock $ 572.00
50 mg In stock $ 818.00
100 mg In stock $ 1,130.00
500 mg In stock $ 2,280.00
1 mL * 10 mM (in DMSO) In stock $ 217.00
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Purity: 99.10%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description NSP-805 is a potent and selective guinea pig cardiac phosphodiesterase 3 (PDE3) inhibitor.
In vitro In isolated guinea pig left atria, the positive inotropic EC50 values (microM) in order of potency were about 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)[1].
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 the drugs were 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 improved the hemodynamic state of heart failure to normal levels.?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, and NSP-804 was a potent and selective inhibitor of PDE III similar to indolidan[1].
Molecular Weight 297.35
Formula C17H19N3O2
CAS No. 125068-54-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 20 mg/ml (67.26 mM)

TargetMolReferences and Literature

1. Mochizuki N, et al. Cardiovascular effects of NSP-804 and NSP-805, novel cardiotonic agents with vasodilator properties. J Cardiovasc Pharmacol. 1993 Jun;21(6):983-95. 2. Uchida H, et al. [The effect of phosphodiesterase type 3 inhibitor on chorio-retinal blood flow in rabbits eyes]. Nippon Ganka Gakkai Zasshi. 2002 Oct;106(10):615-20.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Bioactive Compounds Library Max Metabolism Compound Library ReFRAME Related Library Bioactive Compound Library NO PAINS Compound Library Cuproptosis Compound Library

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Keywords

NSP-805 125068-54-4 Metabolism PDE Inhibitor NSP 805 inhibit Phosphodiesterase (PDE) NSP805 inhibitor

 

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