| Bioactivity | MDL-28170 (Calpain Inhibitor III) is a potent, selective and membrane-permeable cysteine protease inhibitor of calpain that rapidly penetrates the blood-brain barrier following systemic administration[1][2]. MDL-28170 also block γ-secretase[4]. | |||||||||
| Target | Calpain. | |||||||||
| Invitro | MDL-28170 significantly and time-dependently improves the recovery of synaptic responses in hippocampal slices following prolonged, moderate hypoxia without hypoxic depolarization[1].MDL-28170 dose-dependently inhibits brain cysteine proteinase activity (in vitro Ki= 0.01 μM)[2]. | |||||||||
| In Vivo | Treatment with MDL-28170 (50 mg/kg, i.p.) completely prevents the striatal damage in four animals in each of the two treatment groups. The numbers of necrotic neurons are reduced by 85% and 68% in animals in which MDL-28170 injections are initiated at 0.5 and 3 h of recirculation, respectively[2].MDL-28170 (30 mg/kg, i.p.) reduces the functional and structural deterioration of corpus callosum following fluid percussion injury[3].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[5]. | |||||||||
| Name | MDL-28170 | |||||||||
| CAS | 88191-84-8 | |||||||||
| Formula | C22H26N2O4 | |||||||||
| Molar Mass | 382.45 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Chen ZF, et al. Neuronal recovery after moderate hypoxia is improved by the calpain inhibitor MDL28170. Brain Res. 1997 Sep 19;769(1):188-92. [2]. Li PA, et al. 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. [3]. Ai J, et al. 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. [4]. De Strooper B, et al. A presenilin-1-dependent gamma-secretase-like protease mediates release of Notch intracellular domain. Nature. 1999 Apr 8;398(6727):518-22. [5]. Kharatmal SB, et al. Calpain inhibitor, MDL 28170 confer electrophysiological, nociceptive and biochemical improvement in diabetic neuropathy. Neuropharmacology. 2015 Oct;97:113-21. |
MDL-28170
CAS: 88191-84-8 F: C22H26N2O4 W: 382.45
MDL-28170 (Calpain Inhibitor III) is a potent, selective and membrane-permeable cysteine protease inhibitor of calpain t
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