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MDL 28170
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。
MDL 28170图片
CAS NO:88191-84-8
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
25mg电议

产品介绍

化学性质

Physical AppearanceA solid
StorageStore at -20°C
M.Wt382.45
Cas No.88191-84-8
FormulaC22H26N2O4
Solubilityinsoluble in H2O; ≥16.75 mg/mL in DMSO; ≥25.05 mg/mL in EtOH with ultrasonic
Chemical Namebenzyl N-[(2S)-3-methyl-1-oxo-1-[(1-oxo-3-phenylpropan-2-yl)amino]butan-2-yl]carbamate
Canonical SMILESCC(C)C(C(=O)NC(CC1=CC=CC=C1)C=O)NC(=O)OCC2=CC=CC=C2
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

资料参考

MDL 28170是一种选择性的抑制剂,抑制calpain和cathepsin B,Ki值分别为10和25 nM,而不抑制胰蛋白酶样丝氨酸蛋白酶。MDL 28170可以快速通过血脑屏障,在全身给药后可抑制脑内半胱氨酸蛋白酶的活性[1,2]。

Calpain可通过直接限制肌节的蛋白水解,从而影响再灌注功能。再灌注期间,MDL-28170的功能改善得到实验的支持。MDL-28170通过阻断calpains的催化位点而起作用。实验也表明,皮肤肌纤维减少了对Ca2+的敏感性,而在缺血之前或再灌注的早期给予MDL-28170治疗可恢复敏感性[1]。

小鼠腹腔巨噬细胞用trypomastigotes预感染3小时,MDL28170能够显著减少血流中trypomastigotes的生存能力,IC50/24 h值为20.4 mM。在感染巨噬细胞之前,寄生虫用6.25-50 mM的MDL28170预处理呈现明显的剂量依赖性抑制,相应的抑制从20%增加到50%。此外,实验感染T. Cruzi的巨噬细胞用MDL 28170处理减少了感染的百分比,即使在6.25 mM的最低浓度时[3]。

在离体大鼠心脏中,一旦Ca2+饱食,心脏立即恶化,揭示了心脏功能的显著抑制和心肌损伤区域的扩大,并伴随乳酸脱氢酶、线粒体释放细胞色素c、凋亡指数及降解肌钙蛋白(TnI)的显著增加。MDL 28170显著抑制这些变化,除了肌钙蛋白的降解[4]。

参考文献:
1. Urthaler F, Wolkowicz PE, Digerness SB, et al. MDL-28170, a membrane-permeantcalpain inhibitor, attenuates stunning and PKC epsilon proteolysis in reperfused ferret hearts. Cardiovasc Res, 1997, 35 (1): 60-7.
2. Li P, Wendy H, He Q, et al. Postischemic treatment withcalpain inhibitor MDL 28170ameliorates brain damage in a gerbil model of global ischemia, Neuroscience Letters, 1998, 247 :17–20.
3. V?´tor EV, Rubem F, Andre´ L, Effects of the calpain inhibitor MDL28170 on the clinically relevant forms of Trypanosomacruzi in vitro. J AntimicrobChemother , 2010, 65: 1395–1398.
4. Bi S H, Jin Z X, Zhang J Y, et al. Calpaininhibi tor MDL 28170 protectsagainst the Ca2+paradox in rat hearts.Clinical and Experimental Pharmacology and Physiology , 2012, 39:385–392 .

试验操作

Cell experiment:[1]

Cell lines

Schwann cells

Reaction Conditions

50 nM, 500 nM, 5 μM, or 50 μM MDL 28170 for 4 h incubation

Applications

MDL 28170 significantly enhanced Schwann cell survivalin vitroin response to oxidative stress induced by application of H2O2, without reducing lactate dehydrogenase release.

Animal experiment:[2]

Animal models

A gerbil model of global ischemia

Dosage form

50 mg/kg

Injected at 0.5 and 3 h of recirculation following 5 min of global ischemia

Applications

The calpain inhibitor, MDL 28170, protected against cortical neuronal damage even if the treatment was delayed until 3 h after reperfusion. However, the neuroprotective effect of this agent was less pronounced in the hippocampal CA1 sector.

Note

The technical data provided above is for reference only.

References:

1. Hill CE, Guller Y, Raffa SJ, et al. A calpain inhibitor enhances the survival of Schwann cells in vitro and after transplantation into the injured spinal cord. Journal of Neurotrauma, 2010, 27(9): 1685-1695.

2. Li PA, Howlett W, He QP, et al. Postischemic treatment with calpain inhibitor MDL 28170 ameliorates brain damage in a gerbil model of global ischemia. Neuroscience Letters, 1998, 247(1): 17-20.

生物活性

MDL 28170是一种有效的和选择性的calpain和cathepsin B抑制剂,Ki值分别为10和25 nM,而不抑制胰蛋白酶样丝氨酸蛋白酶。
靶点calpaincathepsin B    
IC5010nM25nM