Nifuroxazide 965-52-6

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Molecular Weight:

275.22 Nifuroxazide is a cell-permeable and orally available nitrofuran-based antidiarrheal agent that effectively suppresses the activation of cellular STAT1/3/5 transcription activity with IC50 of 3 μM against IL-6-induced STAT3 activation in U3A cells


Biological Activity


Nifuroxazide is a nitrofuran compound inhibitor of STAT transcription
factor signaling. Nifuroxazide is described to block constitutive
phosphorylation of STAT3 by reducing Jak kinase autophosphorylation,
decreasing the viability of myeloma cells depending on constitutive
STAT3 activity for survival while not affecting normal peripheral blood
mononuclear cells. Nifuroxazide produces decreases in tyrosine
phosphorylation of Jak2 and Tyk2, and showed no effects on EGF receptor
tyrosine kinase or Src kinase, indicating a relative specificity of
Nifuroxazide for Jak2 and Tyk2. Nifuroxazide shows no inhibition of Akt
or MAPK phosphorylation. Nifuroxazide inhibits the constitutive
phosphorylation of STAT3 in MM cells by reducing Jak kinase
autophosphorylation, and leads to down-regulation of the STAT3 target
gene Mcl-1.


Nifuroxazide causes a decrease in viability of primary
myeloma cells and myeloma cell lines containing STAT3 activation, but
not normal peripheral blood mononuclear cells. Although bone marrow
stromal cells provide survival signals to myeloma cells, nifuroxazide
can overcome this survival advantage. Reflecting the interaction of
STAT3 with other cellular pathways, nifuroxazide shows enhanced
cytotoxicity when combined with either the histone deacetylase inhibitor
depsipeptide or the MEK Inhibitor UO126.


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)	275.22
Formula	C12H9N3O5
CAS No.	965-52-6

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

Solubility (25°C) *	In vitro	DMSO	55 mg/mL (199.84 mM)
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	Benzoic acid, 4-hydroxy-, 2-[(5-nitro-2-furanyl)methylene]hydrazide

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Product Categories : JAK/STAT > STAT inhibitor