Sigma-Aldrich Pde5 Inhibitor Cpd7a

Assay

≥98% (HPLC)

Quality Level

100

Form

solid

Potency

270 pM IC₅₀

Manufacturer/Tradename

Calbiochem^®

Storage Condition

OK to freeze
protect from light

Color

cream

Solubility

DMSO: 100 mg/mL

Storage Temp.

2-8°C

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
PDE5Reversible: 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.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany