Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C22H26N2O4 |
| Molecular Weight | 382.4528 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)[C@H](NC(=O)OCC1=CC=CC=C1)C(=O)N[C@@H](CC2=CC=CC=C2)C=O
InChI
InChIKey=NGBKFLTYGSREKK-PMACEKPBSA-N
InChI=1S/C22H26N2O4/c1-16(2)20(24-22(27)28-15-18-11-7-4-8-12-18)21(26)23-19(14-25)13-17-9-5-3-6-10-17/h3-12,14,16,19-20H,13,15H2,1-2H3,(H,23,26)(H,24,27)/t19-,20-/m0/s1
| Molecular Formula | C22H26N2O4 |
| Molecular Weight | 382.4528 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/20874056 | https://www.ncbi.nlm.nih.gov/pubmed/15013018 | https://www.ncbi.nlm.nih.gov/pubmed/11012026 | https://www.ncbi.nlm.nih.gov/pubmed/28663009
Curator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/20874056 | https://www.ncbi.nlm.nih.gov/pubmed/15013018 | https://www.ncbi.nlm.nih.gov/pubmed/11012026 | https://www.ncbi.nlm.nih.gov/pubmed/28663009
MDL-28170 is a potent, selective inhibitor of calpain and cathepsin B that does not inhibit trypsin-like serine proteases. In vitro MDL-28170 reduces capsaicin-mediated cell death in cultured dorsal root ganglion, block Ca2+-induced suppression of neurite outgrowth in isolated hippocampal pyramidal neurons. MDL28170 was able to significantly reduce the viability of bloodstream trypomastigotes in mouse macrophages pre-infected with trypomastigotes. In vivo MDL-28170 rapidly penetrates the blood-brain barrier following systemic administration and displays neuroprotective effects in vivo.
CNS Activity
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Redox-control of the alarmin, Interleukin-1α. | 2013 |
|
| A pharmacologically-based array to identify targets of cyclosporine A-induced toxicity in cultured renal proximal tubule cells. | 2012-01-15 |
|
| Calpain activation is involved in acute manganese neurotoxicity in the rat striatum in vivo. | 2012-01 |
|
| Neuroprotective effects of MAPK/ERK1/2 and calpain inhibitors on lactacystin-induced cell damage in primary cortical neurons. | 2011-12 |
|
| Calpain is involved in cisplatin-induced endothelial injury in an in vitro three-dimensional blood vessel model. | 2010-11 |
|
| Role of GRP78/BiP degradation and ER stress in deoxynivalenol-induced interleukin-6 upregulation in the macrophage. | 2009-06 |
|
| Calpain mediates the dioxin-induced activation and down-regulation of the aryl hydrocarbon receptor. | 2006-11 |
|
| The calpain inhibitor MDL 28170 prevents inflammation-induced neurofilament light chain breakdown in the spinal cord and reduces thermal hyperalgesia. | 2004-07 |
|
| Protective effect of MDL28170 against thioacetamide-induced acute liver failure in mice. | 2004-01-20 |
|
| Inhibition of severe acute respiratory syndrome-associated coronavirus (SARSCoV) by calpain inhibitors and beta-D-N4-hydroxycytidine. | 2004-01 |
|
| Calpain released from dying hepatocytes mediates progression of acute liver injury induced by model hepatotoxicants. | 2003-09-15 |
|
| In vitro isolation and identification of human immunodeficiency virus (HIV) variants with reduced sensitivity to C-2 symmetrical inhibitors of HIV type 1 protease. | 1993-08-15 |
|
| Peptide aldehydes as inhibitors of HIV protease. | 1993-03-22 |
Patents
Sample Use Guides
A single tail vein bolus injection of 30 mg/kg MDL-28170 (courtesy of Aventis Pharmaceuticals) dissolved in 1 mL of the vehicle (PEG300/EtOH, 9:1) was administered to Wistar rats.
Route of Administration:
Intravenous
Peritoneal macrophages from female BALB/c mice were incubated in the absence or presence of MDL28170 at 30 μM (from a stock solut ion at 5 mM) and dimethylsulfoxide (DMSO, inhibitor diluent ) in triplicate for 72 h. The effect of MDL28170 on the viability of murine peritoneal macrophages was assessed by lack of Trypan blue vital dye staining.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:27:08 GMT 2025
by
admin
on
Mon Mar 31 18:27:08 GMT 2025
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| Record UNII |
WCJ9LQ197S
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| Record Status |
Validated (UNII)
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| Record Version |
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