CALPAIN INHIBITOR III
Synonym(s):Calpain Inhibitor III;Calpain Inhibitor III - CAS 88191-84-8 - Calbiochem;Carbobenzoxy-valinyl-phenylalaninal, MDL 28170
- CAS NO.:88191-84-8
- Empirical Formula: C22H26N2O4
- Molecular Weight: 382.45
- MDL number: MFCD00798796
- EINECS: 618-124-4
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-05-18 11:31:19
What is CALPAIN INHIBITOR III?
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
The Uses of CALPAIN INHIBITOR III
MDL 28170 acts as a caplain inhibitor reducing hypoxia in ischemic-retinopathy, and various other neuroprotective effects.
The Uses of CALPAIN INHIBITOR III
Inhibits calpain proteolysis
What are the applications of Application
MDL-28170 is a cell permeable, selective inhibitor of μ-calpain (calpain-1) and m-calpain (calpain-2).
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
Properties of CALPAIN INHIBITOR III
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 |
pka | 11.05±0.46(Predicted) |
form | White lyophilized solid |
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 information for CALPAIN INHIBITOR III
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P260:Do not breathe dust/fume/gas/mist/vapours/spray. P280:Wear protective gloves/protective clothing/eye protection/face protection. P301+P312:IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. |
Computed Descriptors for CALPAIN INHIBITOR III
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