Deferiprone 30652-11-0

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Molecular Weight: 139.15 Deferiprone is a chelating agent with an affinity for ferric ion (iron III),binds with ferric ions to form neutral 3:1 (deferiprone:iron) complexes that are stable over a wide range of pH values.


Biological Activity


Deferiprone (100 μM) is able to protect myocytes from
doxorubicin-induced lactate dehydrogenase release. Deferiprone (300 μM)
quickly and efficiently removes iron(III) from its complex with
doxorubicin. Deferiprone (300 μM) rapidly enters myocytes and displaces
iron from a fluorescence-quenched trapped intracellular iron-calcein
complex, suggesting that in the myocyte, deferiprone should also be able
to displace iron from its complex with doxorubicin. Deferiprone (3 mM)
also greatly reduces hydroxyl radical production by the
iron(III)-doxorubicin complex in the xanthine oxidase/xanthine
superoxide generating system. .


Deferiprone (0.5 mM) increases removal of RBC membrane free iron in a time and dose dependent manner.
Deferiprone (0.3 mM) is effective in inhibiting radioactive iron
mobilization from iron-loaded heart cells and protecting or restoring
mitochondrial respiratory enzyme activity. Deferiprone (1 mM) results in
a sharp decrease in complex I-III activity in iron-loaded heart cells.


Deferiprone shows cytotoxic effect of human tumor cell lines HSC-2,
HSC-3 and HL-60 with IC50 of 13.5 μg/mL, 9.9 μg/mL and 10.6 μg/mL, the
cytotoxic activity of HK1 against HL-60 and HSC-2 cells is reduced in
the presence of FeCl3. Deferiprone (100 μg/mL) induces internucleosomal DNA fragmentation in HL-60 cells, but the addition of FeCl3 inhibits the DNA fragmentation. Deferiprone (100 μg/mL) activates the caspase 3, 8 and 9 in HSC-2 cells.


Deferiprone (100 mg/kg) reduces the mean basilar artery cross-sectional
areas by 24% in rabbits. Deferiprone (100 mg/kg) combined with
subarachnoid hemorrhage(SAH) shows a variable amount of corrugation of
the internal elastic lamina in rabbits.


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)	139.15
Formula	C7H9NO2
CAS No.	30652-11-0

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

Solubility (25°C) *	In vitro	DMSO	<1 mg/mL (
		Water	1 mg/mL (7.18 mM)
		Ethanol	<1 mg/mL (

Chemical Name	4(1H)-Pyridinone, 3-hydroxy-1,2-dimethyl-

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