Edaravone 89-25-8

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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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