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| CALPAIN INHIBITOR III Basic information |
| Product Name: | CALPAIN INHIBITOR III | | Synonyms: | Calpain Inhibitor III - CAS 88191-84-8 - Calbiochem;CS-1705;CALPAIN INHIBITOR III;CARBOBEZOXY-VALINYL-PHENYLALANINALZ-VAL-PHE-CHO;CARBOBENZOXY-VALINYL-PHENYLALANINAL;MDL 28170;Z-VAL-PHE-ALDEHYDE;Z-VAL-PHE-CHO | | CAS: | 88191-84-8 | | MF: | C22H26N2O4 | | MW: | 382.45 | | EINECS: | 618-124-4 | | Product Categories: | inhibitor | | Mol File: | 88191-84-8.mol |
| CALPAIN INHIBITOR III Chemical Properties |
| Boiling point | 595.6±50.0 °C(Predicted) | | density | 1.153±0.06 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: 26 mg/mL | | form | White lyophilized solid | | pka | 11.05±0.46(Predicted) | | color | White | | 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. |
| Safety Statements | 22-24/25 | | WGK Germany | 3 | | HS Code | 2924297099 |
| CALPAIN INHIBITOR III Usage And Synthesis |
| Description | 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 | | Uses | MDL 28170 acts as a caplain inhibitor reducing hypoxia in ischemic-retinopathy, and various other neuroprotective effects. | | Uses | Inhibits calpain proteolysis | | Definition | ChEBI: A dipeptide resulting from the formal condensation of the carboxy group of N-benzyloxycarbonyl-L-valine with the amino group of L-phenylalanine aldehyde. It is a potent cell-permeable inhibitor of calpai
I and II, and is also a gamma-secretase inhibitor. | | General Description | A potent, cell-permeable inhibitor of calpain I and II (Ki = 8 nM) that also reduces capsaicin-mediated cell death in cultured dorsal root ganglion. Reported to block A23187-induced suppression of neurite outgrowth in isolated hippocampal pyramidal neurons. Exhibits neuroprotective effects against glutamate-induced toxicity. | | Biological Activity | Potent, selective inhibitor of calpain and cathepsin B (K i values are 10 and 25 nM respectively) that does not inhibit trypsin-like serine proteases. Rapidly penetrates the blood-brain barrier following systemic administration and displays neuroprotective effects in vivo . | | Biochem/physiol Actions | Cell permeable: yes | | References | 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 |
| CALPAIN INHIBITOR III Preparation Products And Raw materials |
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