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MDL-28170

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Chemical Structure| 88191-84-8 同义名 : Calpain Inhibitor III
CAS号 : 88191-84-8
货号 : A172590
分子式 : C22H26N2O4
纯度 : 98+%
分子量 : 382.45
MDL号 : MFCD28137700
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(78.44 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 MDL-28170 (Calpain Inhibitor III) is a potent, selective and membrane-permeable cysteine protease inhibitor of calpain. The newly-developed calpain inhibitor, MDL 28170 penetrates the blood-brain barrier and inhibits brain cysteine protease activity after systemic administration. The calpain inhibitor, MDL 28170 (50 mg/kg), was initiated at 0.5 and 3 h of recirculation following 5min of global ischemia. The calpain inhibitor, MDL 28170, protects against cortical neuronal damage even if the treatment is delayed until 3 h after reperfusion[3]. The calpain inhibitor, MDL28170, significantly improved the recovery of synaptic responses in hippocampal slices following prolonged, moderate hypoxia without hypoxic depolarization[4]. MDL28170 increased VSC4.1 motor neurons' viability under tunicamycin (an endoplasmic reticulum stress) induced injury. In a traumatic SCI (spinal cord injury) rat model, MDL28170-loaded PCL (polycaprolactone) film reduced the area of lesion cavity, and promoted recovery of locomotor behavior. Moreover, the expression of GAP-43 was upregulated after MDL28170-loaded PCL film treatment[5]. MDL-28170 (30 mg/kg, i.p.) reduces the functional and structural deterioration of corpus callosum following fluid percussion injury[6]. MDL-28170 (10 mg/kg, i.p.) significantly improves nerve function parameters in diabetic rats. MDL-28170 (3 and 10 mg/kg, i.p.) improves nociceptive behavior in diabetic rats[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.61mL

0.52mL

0.26mL

13.07mL

2.61mL

1.31mL

26.15mL

5.23mL

2.61mL
参考文献

[1]Brocard C, Plantier V, et al. Cleavage of Na(+) channels by calpain increases persistent Na(+) current and promotes spasticity after spinal cord injury. Nat Med. 2016 Apr;22(4):404-11.

[2]Chen ZF, Schottler F, Lee KS. Neuronal recovery after moderate hypoxia is improved by the calpain inhibitor MDL28170. Brain Res. 1997 Sep 19;769(1):188-92.

[3]Li PA, Howlett W, He QP, Miyashita H, Siddiqui M, Shuaib A. Postischemic treatment with calpain inhibitor MDL 28170 ameliorates brain damage in a gerbil model of global ischemia. Neurosci Lett. 1998 May 8;247(1):17-20

[4]Chen ZF, Schottler F, Lee KS. Neuronal recovery after moderate hypoxia is improved by the calpain inhibitor MDL28170. Brain Res. 1997 Sep 19;769(1):188-92

[5]Shi D, He T, Tang W, Li H, Wang C, Zheng M, Hu J, Song X, Ding Y, Chen YY, Shen Y, Jin H, Wang LL. Local application of MDL28170-loaded PCL film improves functional recovery by preserving survival of motor neurons after traumatic spinal cord injury. Neurosci Lett. 2019 Feb 16;694:161-167

[6]Ai J, Liu E, Wang J, Chen Y, Yu J, Baker AJ. Calpain inhibitor MDL-28170 reduces the functional and structural deterioration of corpus callosum following fluid percussion injury. J Neurotrauma. 2007 Jun;24(6):960-78

[7]Kharatmal SB, Singh JN, Sharma SS. Calpain inhibitor, MDL 28170 confer electrophysiological, nociceptive and biochemical improvement in diabetic neuropathy. Neuropharmacology. 2015 Oct;97:113-21