537012-M
Prolyl Endopeptidase Inhibitor III, KYP-2047
The Prolyl Endopeptidase Inhibitor III, KYP-2047 controls the biological activity of Prolyl Endopeptidase. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.
Synonym(s):
Prolyl Endopeptidase Inhibitor III, KYP-2047, (S)-1-((S)-1-(4-phenylbutanoyl)-pyrrolidine-2-carbonyl)pyrrolidine-2-carbonitrile, 4-phenylbutanoyl-Lprolyl-2(S)-cyanopyrrolidine, PREP inhibitor III, KYP-2047
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About This Item
Empirical Formula (Hill Notation):
C20H25N3O2
Molecular Weight:
339.43
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
oil
Storage condition:
OK to freeze, protect from light
assay
≥98% (HPLC)
form
oil
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
clear colorless
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
General description
A cell-permeable, potent, fast-acting, and selective inhibitor of prolyl oligopeptidase (PREP) (Ki = 23 pM). Reported to cross the blood-brain barrier. Inhibits about 85% PREP activity within 10 minutes of administration and exhibits a half-life of about 4.8 hours. Exhibits higher lipophilicity that increases its penetration across biological membranes in vivo. Maximum plasma and brain levels are achieved within 10 minutes following its i.p. administration. Shown to block oxidative-stress induced α-synuclein aggregation and clearance in cellular and animal models of Parkinson′s disease. Also shown to improve cognitive performance in young rats (1-5 mg/kg) in a dose-dependent manner.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Jarho, E., et al. 2004. J. Med. Chem.47, 5605.
Venalainen, J., et al. 2011. Biochem. Pharmacol.71, 683.
Jalkanen, A., et al. 2006. Basic & Clin. Pharmac. & Tox.100, 132.
Jalkanen, A., et al. 2011. Basic & Clin. Pharmac. & Tox.109, 443.
Klimaviciusa, L., et al. 2012. Journ. Neuros. Methods.204, 104.
Myohanen, T., et al. 2012. Brit. J. Pharm.166, 1097.
Venalainen, J., et al. 2011. Biochem. Pharmacol.71, 683.
Jalkanen, A., et al. 2006. Basic & Clin. Pharmac. & Tox.100, 132.
Jalkanen, A., et al. 2011. Basic & Clin. Pharmac. & Tox.109, 443.
Klimaviciusa, L., et al. 2012. Journ. Neuros. Methods.204, 104.
Myohanen, T., et al. 2012. Brit. J. Pharm.166, 1097.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
10 - Combustible liquids
wgk
WGK 2
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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