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PD 151746
本半岛bd体育手机客户端 不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
PD 151746图片
CAS NO:179461-52-0
规格:≥98%
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

半岛bd体育手机客户端 介绍
PD 151746 (PD-151746) is a novel, potent, selective, and cell-permeable calpain inhibitor with important biological activity. It inhibits calpain with a Ki of 0.26 μM for μ-Calpain, and has about 20-fold higher selectivity for u-calpain (Ki = 0.26 ± 0.03 μM) over m-calpain (Ki = 5.33 ± 0.77 μM). 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. The μ-calpain inhibitor PD 151746 decreases oxLDL-induced cytotoxicity.
理化性质和储存条件
Molecular Weight (MW)237.25
FormulaC11H8FNO2S
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)
Other infoChemical Name: 3-(5-Fluoro-3-indolyl)-2-mercapto-2-propenoic Acid
InChi Key: HWMQHECFXSVZGN-KMKOMSMNSA-N
InChi Code: InChI=1S/C11H8FNO2S/c12-7-1-2-9-8(4-7)6(5-13-9)3-10(16)11(14)15/h1-5,13,16H,(H,14,15)/b10-3-
SMILES Code: O=C(O)/C(S)=C/C1=CNC2=C1C=C(F)C=C2
SynonymsPD 151746; PD151746; PD-151746;
实验参考方法
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: PD151746 is a calpain inhibitor, shows a 20-fold selectivity for u-calpain (Ki = 0.26 ± 0.03 μM) over m-calpain (Ki = 5.33 ± 0.77 μM).

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).

In Vivo
Animal model
Formulation & Dosage
ReferencesProc 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.
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