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Edaravone 89-25-8

Product Description

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Edaravone

Molecular Weight: 174.2 Edaravone is a novel potent free radical scavenger that has been clinically used to reduce the neuronal damage following ischemic stroke.


Biological Activity


Edaravone exerts neuroprotective effects by inhibiting endothelial
injury and by ameliorating neuronal damage in brain ischemia. Edaravone
provides the desirable features of NOS: it increases eNOS (beneficial
NOS for rescuing ischemic stroke) and decreases nNOS and iNOS
(detrimental NOS). Edaravone, which inhibits oxidation and enhances NO
production derived from increased eNOS expression, may improve and
conserve cerebral blood flow without peroxynitrite generation during
reperfusion.


Edaravone significantly reduces the infarct volume and improves the
neurological deficit scores at 24 hours after reperfusion in mice brain.
Edaravone markedly suppresses the accumulation of HNE-modified protein
and 8-OHdG at the penumbra area during the early period after
reperfusion and reduces microglial activation, iNOS expression, and
nitrotyrosine formation at the late period. Edaravone attenuates renal
function and pathologic findings significantly in rat kidney.


Edaravone
significantly reduces the generation of free radicals in the tubular
cells indicated by dichlorodihydrofluorescein. Edaravone-treated
animals shows significantly improved neurological outcome.
Edaravone-treatment provides a significant reduction in the number of
TUNEL-positive apoptotic cells, a decrease in Bax immunoreactivity and
an increase in Bcl-2 expression within the peri-infarct area. Edaravone
shows an excellent neuroprotective effect against ischemia/reperfusion
brain injury through a Bax/Bcl-2 dependent anti-apoptotic mechanism.


Protocol(Only for Reference)


Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)


Species Baboon Dog Monkey Rabbit Guinea pig Rat Hamster Mouse
Weight (kg) 12 10 3 1.8 0.4 0.15 0.08 0.02
Body Surface Area (m2) 0.6 0.5 0.24 0.15 0.05 0.025 0.02 0.007
Km factor 20 20 12 12 8 6 5 3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by Animal B Km
Animal A Km



For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) × mouse Km(3) = 11.2 mg/kg
rat Km(6)







Chemical Information








Molecular Weight (MW) 174.2
Formula

C10H10N2O

CAS No. 89-25-8

Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms MCI-186



Solubility (25°C) * In vitro DMSO 35 mg/mL (200.91 mM)
Water <1 mg/mL (
Ethanol 35 mg/mL (200.91 mM)




Chemical Name 3-methyl-1-phenyl-1H-pyrazol-5(4H)-one







Stock Solution (1ml DMSO) 1mM 10mM 20mM 30mM
Mass(mg) 0.1742 1.742 3.484 5.226


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