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PD 145305
本产品不向个人销售,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 145305图片
CAS NO:90536-15-5
规格:98%
分子量:182.2
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
selective inhibitor of calpains
CAS:90536-15-5
分子式:C9H10O2S
分子量:182.2
纯度:98%
存储:Store at -20°C

Background:

PD 145305 is an inactive analog of PD 150606, a potent and selective calpains inhibitor [1].


Calpain is a class of cytosolic cysteine protease that is activated by elevated intracellular calcium. Overactivation of calpain has been implicated in the pathophysiology of several degenerative conditions, including stroke, myocardial ischemia, neuromuscular degeneration, and cataract formation [1].


PD 145305 is an inactive analog of PD 150606, a potent and selective calpains inhibitor. PD 150606, an alpha-mercaptoacrylate derivative, inhibited μ-calpain and m-calpain with Ki values of 0.21 and 0.37 μM, respectively. PD 145305 was inactive at concentrations up to 500 μM. In human leukemic Molt-4 cells, PD150606 inhibited a-spectrin proteolysis in a dose-dependent way and virtually eliminated the formation of the 145-kDa fragment at 10 μM, whereas PD145305 did not attenuate a-spectrin breakdown product formation. In fetal rat cerebrocortical cultures subjected to a combination of hypoxia and hypoglycemia, PD150606 significantly inhibited the release of lactate dehydrogenase, whereas PD145305 was ineffective. PD150606, but not PD145305, was found to make cerebral glutamatergic neurons more resistant to hypoxic/hypoglycemic challenge [1].


Reference:
[1].  Wang KK, Nath R, Posner A, et al. An alpha-mercaptoacrylic acid derivative is a selective nonpeptide cell-permeable calpain inhibitor and is neuroprotective. Proc Natl Acad Sci U S A. 1996 Jun 25;93(13):6687-92.