5.08957
PDE5 Inhibitor, Cpd7a
Synonym(s):
PDE5 Inhibitor, Cpd7a
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About This Item
Empirical Formula (Hill Notation):
C22H20ClN3O2
CAS Number:
Molecular Weight:
393.87
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
assay
≥98% (HPLC)
Quality Level
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.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Primary Target
PDE5
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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