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)
存储类别
10 - Combustible liquids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable