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About This Item
Empirical Formula (Hill Notation):
C22H20ClN3O2
CAS Number:
Molecular Weight:
393.87
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
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.
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
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
Disclaimer
Toxicity: Standard Handling (A)
Storage Class Code
11 - Combustible Solids
WGK
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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