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Merck
CN

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.

别名:

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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关于此项目

经验公式（希尔记法）:
C20H25N3O2
分子量:
339.43
UNSPSC Code:
12352200

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assay

≥98% (HPLC)

form

oil

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

clear colorless

solubility

DMSO: 50 mg/mL

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

存储类别

10 - Combustible liquids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

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