MDL-28170 (88191-84-8) is a potent and selective cell permeable calpain inhibitor. Inhibits oxidative damage-induced apoptosis in PC12 cells and capsaicin-induced apoptosis in dorsal root ganglion neurons.1 It penetrates the blood-brain barrier and inhibits brain cysteine protease activity after systemic administration, ameliorating brain damage in a gerbil model of global ischemia.2 Displays neuroprotective effects in neurotrauma rodent models.3 Calpain I Ki = 8 nM; Cathepsin B Ki = 24 nM in isolated enzyme assays. IC50 = 0.3 µM in intact cell assay.4 Calpain抑制剂mdl -28170(88191-84-8)是一种高效的选择性细胞透性Calpain抑制剂。 抑制氧化损伤诱导的PC12细胞凋亡和辣椒素诱导的背根神经节神经元凋亡 在全身给药后,它能穿透血脑屏障,抑制脑半胱氨酸蛋白酶活性,改善全脑缺血沙鼠模型的脑损伤 在神经创伤鼠类模型中显示神经保护作用 Calpain I Ki = 8 nM; 分离酶测定中组织蛋白酶bki = 24 nM。 完整细胞实验中IC50 = 0.3 μ M。
References/Citations:
1) Chard et al. (1995), Capsaicin-induced neurotoxicity in cultured dorsal root ganglion neurons: involvement of calcium-activated proteases; Neuroscience, 65 1099 2) Li et al. (1998), Postischemic treatment with calpain inhibitor MDL28170 ameliorates brain damage in a gerbil model of global ischemia; Neurosci. Lett., 247 17 3) Thompson et al. (2010), A pharmacological analysis of the neuroprotective efficacy of the brain- and cell-permeable calpain inhibitor MDL-28170 in the mouse controlled cortical impact traumatic brain injury model; J. Neurotrauma, 27 2233 4) Chatterjee et al. (1998), D-amino acid containing, high-affinity inhibitors of recombinant human calpain I; J. Med. Chem., 41 2663
CAS:
88191-84-8
Catalog Number:
10-3005
Activity:
Calpain inhibitor
Chemical Name:
N-Benzyloxycarbonylvalylphenylalaninal
Alternate Name:
Z-Val-Phe-CHO; Calpain Inhibitor III
Molecular Weight:
382.45
Molecular Formula:
C22H26N2O4 Solubility:
Soluble in DMSO (up to 75 mg/ml).
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT
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