product name PD 151746
Description: PD 151746 is a potent and selective, and cell-permeable calpain inhibitor with Ki of 0.26 μM for μ-Calpain, it has about 20-fold selectivity over m-calpain. PD151746 significantly inhibited NMDA-induced α-spectrin breakdown product (SBDP) of 145 kDa and completely inhibited the fragmentation of calmodulin-dependent protein kinase II-α (CaMPK-IIα) and nitric oxide synthase (nNOS), which were cleaved by calpain.
References: Proc Natl Acad Sci U S A. 1996 Jun 25;93(13):6687-92; Biochem J. 2003 Sep 1;374(Pt 2):403-11.
237.25
Formula
C11H8FNO2S
CAS No.
179461-52-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 47 mg/mL (198.1 mM)
Water: <1 mg/mL
Ethanol: 47 mg/mL (198.1 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19409791
| In Vitro |
In vitro activity: In SY5Y cells, PD151746 effectively attenuates the SLLVY-AMC hydrolysis induced by maitotoxin. In HMEC-1 cells, PD 151746 decreases cytotoxicity induced by oxidized low-density lipoprotein (oxLDL). Kinase Assay: Cell Assay: In cerebellar granule cells, PD151746 inhibited serum/potassium (S/K) withdrawal induced apoptosis by 29% through inhibition of calpain. Also, PD151746 inhibited the increase of MEF2 phosphorylation and cdk5/p25 formation and inhibited caspase-3 activity. In human hepatoma G2 cells, PD151746 significantly reduced insulin-stimulated glycogen synthesis and increased the amount of protein tyrosine phosphatase-ε (PTPε), which suggested that calpain played an important role in regulation of insulin-stimulated glycogen synthesis. In HEK-293 cells expressing human formyl peptide receptor (hFPR) or hFPR-like 1 (hFPRL1), PD151746 increased cytoplasmic free Ca2+ ([Ca2+]I). |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Proc Natl Acad Sci U S A. 1996 Jun 25;93(13):6687-92; Br J Pharmacol. 2005 Aug;145(8):1103-11; Biochem J. 2003 Sep 1;374(Pt 2):403-11. |
