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5.08957 Sigma-Aldrich

PDE5 Inhibitor, Cpd7a - Calbiochem

A cell-permeable, highly potent and selective inhibitor of phosphodiesterase 5 (PDEV; IC₅₀ = 270 pM).

Synonym: PDE5 Inhibitor, Cpd7a - Calbiochem

  • Empirical Formula (Hill Notation) C22H20ClN3O2

  • Molecular Weight 393.87

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Properties

Related Categories Cell Biology, Cell Signaling and Neuroscience, Cyclic Nucleotide Metabolism, G Proteins and Cyclic Nucleotides, Phosphodiesterase Inhibitors More...
Quality Level   100
assay   ≥98% (HPLC)
form   solid
potency   270 pM IC50
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   +2C to +8C
color   cream
solubility   DMSO: 100 mg/mL

Description

General description

A cell-permeable, brain permeant, quinoline-based compound that acts as a highly potent and selective inhibitor of phosphodiesterase 5 (PDEV; IC50 = 270 pM). Exhibits over 10,000 fold greater selectivity over various other phosphodiestrases and trivial activity against PDE VI (IC50 = 339 nM). Shown to increase cGMP levels in mouse hippocampus and attenuates long term potentiation and memory defects in mice with elevated levels of oligomeric Aβ42. It is rapidly absorbed with peak plasma concentration observed at 30 min. Displays desirable pharmacokinetic properties with plasma t1/2 = 1.33 h and brain t1/2 = 1.04 h.

A cell-permeable, brain permeant, quinoline-based compound that acts as a highly potent and selective inhibitor of phosphodiesterase 5 (PDEV; IC50 = 270 pM). Exhibits over 10,000 fold greater selectivity over various other phosphodiestrases and trivial activity against PDE VI (IC50 = 339 nM). Shown to increase cGMP levels in mouse hippocampus and attenuates long term potentiation and memory defects in mice with elevated levels of oligomeric Aβ42. It is rapidly absorbed with peak plasma concentration observed at 30 min. Displays desirable pharmacokinetic properties with plasma t1/2 = 1.33 h and brain t1/2 = 1.04 h.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biochem/physiol Actions

Primary Target
PDE5

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Fiorito, J., et al. 2013. Eur. J. Med. Chem.60, 285.

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.
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