PD 151746

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PD 151746

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CAS NO:	179461-52-0
规格:	≥98%

包装与价格：

包装	价格(元)
5mg	询价
10mg	询价
25mg	询价
50mg	询价
100mg	询价
250mg	询价
500mg	询价

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
Formula	C11H8FNO2S
CAS No.	179461-52-0
Storage	-20℃ for 3 years in powder form
Storage	-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 info	Chemical 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
Synonyms	PD 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
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.