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88191-84-8,MFCD28137700
Catalog No.:AA003OLZ

88191-84-8 | Calpain Inhibitor III, MDL 28170

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5mg
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10mg
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25mg
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50mg
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500mg
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  • Technical Information
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  • Technical Information
  • Properties
  • Literature
Technical Information
Catalog Number:
AA003OLZ
Chemical Name:
Calpain Inhibitor III, MDL 28170
CAS Number:
88191-84-8
Molecular Formula:
C22H26N2O4
Molecular Weight:
382.4528
MDL Number:
MFCD28137700
SMILES:
O=CC(NC(=O)C(C(C)C)NC(=O)OCc1ccccc1)Cc1ccccc1
Properties
Properties
 
Form:
Solid  
Storage:
2-8℃;Light sensitive;Keep in dry area;  

Computed Properties
 
Complexity:
497  
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
2  
Heavy Atom Count:
28  
Hydrogen Bond Acceptor Count:
4  
Hydrogen Bond Donor Count:
2  
Rotatable Bond Count:
10  
XLogP3:
2.7  

Literature

Title: Calpain and JNK pathways participate in isoflurane - induced nucleus translocation of apoptosis-inducing factor in the brain of neonatal rats.

Journal: Toxicology letters 20180315

Title: Redox-control of the alarmin, Interleukin-1α.

Journal: Redox biology 20130101

Title: Temporal dependence of cysteine protease activation following excitotoxic hippocampal injury.

Journal: Neuroscience 20121011

Title: Low-dose methylmercury-induced oxidative stress, cytotoxicity, and tau-hyperphosphorylation in human neuroblastoma (SH-SY5Y) cells.

Journal: Environmental toxicology 20120901

Title: Activity-dependent cleavage of the K-Cl cotransporter KCC2 mediated by calcium-activated protease calpain.

Journal: The Journal of neuroscience : the official journal of the Society for Neuroscience 20120815

Title: Calpain induces N-terminal truncation of β-catenin in normal murine liver development: diagnostic implications in hepatoblastomas.

Journal: The Journal of biological chemistry 20120629

Title: Calpain inhibitors exhibit matrix metalloproteinase-2 inhibitory activity.

Journal: Biochemical and biophysical research communications 20120622

Title: Neuroprotective effect of undecylenic acid extracted from Ricinus communis L. through inhibition of μ-calpain.

Journal: European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences 20120512

Title: Ablation of junctin or triadin is associated with increased cardiac injury following ischaemia/reperfusion.

Journal: Cardiovascular research 20120501

Title: Calpain inhibitor MDL 28170 protects against the Ca2+ paradox in rat hearts.

Journal: Clinical and experimental pharmacology & physiology 20120401

Title: Short-duration treatment with the calpain inhibitor MDL-28170 does not protect axonal transport in an in vivo model of traumatic axonal injury.

Journal: Journal of neurotrauma 20120120

Title: A pharmacologically-based array to identify targets of cyclosporine A-induced toxicity in cultured renal proximal tubule cells.

Journal: Toxicology and applied pharmacology 20120115

Title: Calpain activation is involved in acute manganese neurotoxicity in the rat striatum in vivo.

Journal: Experimental neurology 20120101

Title: Inhibition of calpain blocks the phagosomal escape of Listeria monocytogenes.

Journal: PloS one 20120101

Title: Activation of mitochondrial μ-calpain increases AIF cleavage in cardiac mitochondria during ischemia-reperfusion.

Journal: Biochemical and biophysical research communications 20111202

Title: Neuroprotective effects of MAPK/ERK1/2 and calpain inhibitors on lactacystin-induced cell damage in primary cortical neurons.

Journal: Neurotoxicology 20111201

Title: Targeted proteolysis of plectin isoform 1a accounts for hemidesmosome dysfunction in mice mimicking the dominant skin blistering disease EBS-Ogna.

Journal: PLoS genetics 20111201

Title: Calpain mediates pulmonary vascular remodeling in rodent models of pulmonary hypertension, and its inhibition attenuates pathologic features of disease.

Journal: The Journal of clinical investigation 20111101

Title: MDL28170, a calpain inhibitor, affects Trypanosoma cruzi metacyclogenesis, ultrastructure and attachment to Rhodnius prolixus midgut.

Journal: PloS one 20110101

Title: Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.

Journal: Bioorganic & medicinal chemistry letters 20101101

Title: Calpain is involved in cisplatin-induced endothelial injury in an in vitro three-dimensional blood vessel model.

Journal: International journal of oncology 20101101

Title: MDL-28170 has no analgesic effect on CCI induced neuropathic pain in mice.

Journal: Molecules (Basel, Switzerland) 20100427

Title: Ischemia-reperfusion-induced changes in sarcolemmal Na+/K+-ATPase are due to the activation of calpain in the heart.

Journal: Canadian journal of physiology and pharmacology 20100301

Title: Calcium-dependent cleavage of the Na(+)/Ca(2+) exchanger by m-calpain in isolated endoplasmic reticulum.

Journal: Journal of biochemistry 20100201

Title: Calpain inhibition reduces axolemmal leakage in traumatic axonal injury.

Journal: Molecules (Basel, Switzerland) 20091209

Title: Interactions between apoptotic signal transduction and capacitation in human spermatozoa.

Journal: Human reproduction (Oxford, England) 20090901

Title: Mitochondrial micro-calpain is not involved in the processing of apoptosis-inducing factor.

Journal: Experimental neurology 20090801

Title: Over-expression of calpastatin inhibits calpain activation and attenuates myocardial dysfunction during endotoxaemia.

Journal: Cardiovascular research 20090701

Title: Role of GRP78/BiP degradation and ER stress in deoxynivalenol-induced interleukin-6 upregulation in the macrophage.

Journal: Toxicological sciences : an official journal of the Society of Toxicology 20090601

Title: Calpain-mediated degradation of G-substrate plays a critical role in retinal excitotoxicity for amacrine cells.

Journal: Journal of neuroscience research 20090501

Title: Calpain-mediated truncation of GSK-3 in post-mortem brain samples.

Journal: Journal of neuroscience research 20090401

Title: Arrested growth of Trypanosoma cruzi by the calpain inhibitor MDL28170 and detection of calpain homologues in epimastigote forms.

Journal: Parasitology 20090401

Title: Participation of mu-calpain in status epilepticus-induced hippocampal injury.

Journal: Brain research bulletin 20090316

Title: mu-Calpain mediated cleavage of the Na+/Ca2+ exchanger in isolated mitochondria under A23187 induced Ca2+ stimulation.

Journal: Archives of biochemistry and biophysics 20090201

Title: Protein Never in Mitosis Gene A Interacting-1 (PIN1) regulates degradation of inducible nitric oxide synthase in endothelial cells.

Journal: American journal of physiology. Cell physiology 20080901

Title: Contribution of NMDA and non-NMDA receptors to in vivo glutamate-induced calpain activation in the rat striatum. Relation to neuronal damage.

Journal: Neurochemical research 20080801

Title: Intraspinal MDL28170 microinjection improves functional and pathological outcome following spinal cord injury.

Journal: Journal of neurotrauma 20080701

Title: Mu-calpain mediates hippocampal neuron death in rats after lithium-pilocarpine-induced status epilepticus.

Journal: Brain research bulletin 20080515

Title: Calpain activation is involved in early caspase-independent neurodegeneration in the hippocampus following status epilepticus.

Journal: Journal of neurochemistry 20080501

Title: Contribution of calpain activation to early stages of hippocampal damage during oxygen-glucose deprivation.

Journal: Brain research 20080227

Title: Intracellular GSH levels rather than ROS levels are tightly related to AMA-induced HeLa cell death.

Journal: Chemico-biological interactions 20080110

Title: Sustained calpain inhibition improves locomotor function and tissue sparing following contusive spinal cord injury.

Journal: Neurochemical research 20071201

Title: A key role for calpains in retinal ganglion cell death.

Journal: Investigative ophthalmology & visual science 20071201

Title: Coherent anti-Stokes Raman scattering imaging of myelin degradation reveals a calcium-dependent pathway in lyso-PtdCho-induced demyelination.

Journal: Journal of neuroscience research 20071001

Title: Specific blockage of ligand-induced degradation of the Ah receptor by proteasome but not calpain inhibitors in cell culture lines from different species.

Journal: Biochemical pharmacology 20070630

Title: Calpain inhibitor MDL-28170 reduces the functional and structural deterioration of corpus callosum following fluid percussion injury.

Journal: Journal of neurotrauma 20070601

Title: Ischemia promotes calpain-mediated degradation of p120-catenin in SH-SY5Y cells.

Journal: Biochemical and biophysical research communications 20070216

Title: A role for the intracellular protease calpain in the activation of store-operated calcium entry in human platelets.

Journal: Cell calcium 20070201

Title: Calpain inhibition stimulates caspase-dependent apoptosis induced by taxol in NIH3T3 cells.

Journal: Experimental cell research 20070115

Title: Microtubule disruption, not calpain-dependent loss of MAP2, contributes to enduring NMDA-induced dendritic dysfunction in acute hippocampal slices.

Journal: Experimental neurology 20061201

Title: Calpain mediates the dioxin-induced activation and down-regulation of the aryl hydrocarbon receptor.

Journal: Molecular pharmacology 20061101

Title: Glutamate-induced protease-mediated loss of plasma membrane Ca2+ pump activity in rat hippocampal neurons.

Journal: Journal of neurochemistry 20060901

Title: Antileishmanial activity of MDL 28170, a potent calpain inhibitor.

Journal: International journal of antimicrobial agents 20060801

Title: Tributyltin-induced cell death is mediated by calpain in PC12 cells.

Journal: Neurotoxicology 20060701

Title: Ischemic preconditioning prevents calpain-mediated impairment of Na+/K+-ATPase activity during early reperfusion.

Journal: Cardiovascular research 20060501

Title: The calpain inhibitor MDL-28170 and the AMPA/KA receptor antagonist CNQX inhibit neurofilament degradation and enhance neuronal survival in kainic acid-treated hippocampal slice cultures.

Journal: The European journal of neuroscience 20060501

Title: Developmental changes in NMDA neurotoxicity reflect developmental changes in subunit composition of NMDA receptors.

Journal: The Journal of neuroscience : the official journal of the Society for Neuroscience 20060315

Title: Endoplasmic reticulum Ca2+ depletion induces endothelial cell apoptosis independently of caspase-12.

Journal: Cardiovascular research 20060301

Title: Calpain inhibitor MDL28170 modulates Abeta formation by inhibiting the formation of intermediate Abeta46 and protecting Abeta from degradation.

Journal: FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20060201

Title: Calpain inhibitor MDL 28170 protects hypoxic-ischemic brain injury in neonatal rats by inhibition of both apoptosis and necrosis.

Journal: Brain research 20050310

Title: Calpain inhibitor inhibits p35-p25-Cdk5 activation, decreases tau hyperphosphorylation, and improves neurological function after spinal cord hemisection in rats.

Journal: Journal of neuropathology and experimental neurology 20050101

Title: Ischemic preconditioning attenuates calpain-mediated degradation of structural proteins through a protein kinase A-dependent mechanism.

Journal: Cardiovascular research 20041001

Title: Epimerization study of the L,L- and L,D-diastereoisomers of the calpain inhibitor MDL 28170 by capillary electrophoresis.

Journal: Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 20040925

Title: Both N-methyl-D-aspartate (NMDA) and non-NMDA receptors mediate glutamate-induced cleavage of the cyclin-dependent kinase 5 (cdk5) activator p35 in cultured rat hippocampal neurons.

Journal: Neuroscience letters 20040923

Title: The calpain inhibitor MDL 28170 prevents inflammation-induced neurofilament light chain breakdown in the spinal cord and reduces thermal hyperalgesia.

Journal: Pain 20040701

Title: Inhibition of severe acute respiratory syndrome-associated coronavirus (SARSCoV) by calpain inhibitors and beta-D-N4-hydroxycytidine.

Journal: Antiviral chemistry & chemotherapy 20040101

Title: Effects of fimbria-fornix transection on calpain and choline acetyl transferase activities in the septohippocampal pathway.

Journal: Neuroscience 20040101

Title: Protective effect of MDL28170 against thioacetamide-induced acute liver failure in mice.

Journal: Journal of biomedical science 20040101

Title: Calpain released from dying hepatocytes mediates progression of acute liver injury induced by model hepatotoxicants.

Journal: Toxicology and applied pharmacology 20030915

Title: Inhibition of calpains prevents neuronal and behavioral deficits in an MPTP mouse model of Parkinson's disease.

Journal: The Journal of neuroscience : the official journal of the Society for Neuroscience 20030515

Title: A 48-hour exposure of pancreatic islets to calpain inhibitors impairs mitochondrial fuel metabolism and the exocytosis of insulin.

Journal: Metabolism: clinical and experimental 20030501

Title: Preinjury administration of the calpain inhibitor MDL-28170 attenuates traumatically induced axonal injury.

Journal: Journal of neurotrauma 20030301

Title: Lysophosphatidylcholine inhibits endothelial cell migration by increasing intracellular calcium and activating calpain.

Journal: Arteriosclerosis, thrombosis, and vascular biology 20030201

Title: beta-Amyloid (1-40)-induced apoptosis of cultured cortical neurones involves calpain-mediated cleavage of poly-ADP-ribose polymerase.

Journal: Neurobiology of aging 20030101

Title: Evaluation of conditions for calpain inhibition in the rat spinal cord: effective postinjury inhibition with intraspinal MDL28170 microinjection.

Journal: Journal of neurotrauma 20030101

Title: Cleavage of the cyclin-dependent kinase 5 activator p35 to p25 does not induce tau hyperphosphorylation.

Journal: Biochemical and biophysical research communications 20021115

Title: Selective release of calpain produced alphalI-spectrin (alpha-fodrin) breakdown products by acute neuronal cell death.

Journal: Biological chemistry 20020501

Title: Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.

Journal: The Journal of biological chemistry 20020419

Title: In vitro isolation and identification of human immunodeficiency virus (HIV) variants with reduced sensitivity to C-2 symmetrical inhibitors of HIV type 1 protease.

Journal: Proceedings of the National Academy of Sciences of the United States of America 19930815

Title: Peptide aldehydes as inhibitors of HIV protease.

Journal: FEBS letters 19930322

Title: 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.

Title: 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.

Title: 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.

Title: 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.

Title: Kharatmal SB, et al. Calpain inhibitor, MDL 28170 confer electrophysiological, nociceptive and biochemical improvement in diabetic neuropathy. Neuropharmacology. 2015 Oct;97:113-21.

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