Product ID L9072 
Molecular formula C8H7ClN2O2S

Activator of ATP-dependent K+ channels; antihypertensive.

Sulphonamide, chemically related to sulphonylureas , synthetic.
Biological activity

<B>Diazoxide</B> increases K<SUP>+</SUP> efflux: like Cromakalim, it opens 86 Rb<SUP>+</SUP>-permeable K<SUP>+</SUP> channels in vascular smooth muscle (aorta and portal vein). In the insulin-secreting cell line RINm5F, in the continued presence of ATP, <B>Diazoxide</B> 200 &mu;M evokes a marked and sustained activation of ATP-inhibited channels. <B>Diazoxide</B> mediates its effects through the activation of ATP-sensitive K<SUP>+</SUP> channels.<BR><br>Used as an antihypertensive agent because of its arterial smooth muscles vasodilator activity. It has vascular effects on embryo and foetus. Perifusion of 10 &mu;M decreases integrated spontaneous contractions of the rat portal vein to 22 %. In the rabbit aorta, inhibited vasoconstrictor responses to Angiotensin II, Noradrenaline and low concentrations (<=30 mM) of KCl, the antivasoconstrictor activities being abolished in vessels depolarized with >= 35 mM K<SUP>+</SUP>. <br><br>Its hyperglycaemic effect is correlated with its ability to induce the opening of the ATP-regulated K<SUP>+</SUP> channels in mouse pancreatic beta-cells. 30 mg/kg caused a more than 2-fold increase in plasma glucose in rats and prevented any return toward base line within 1.5 hour after a glucose load.<br><br>
<B>Diazoxide </B>has the opposite effect to glucose: hyperpolarizing the cell membrane, it abolishes the glucose-induced release of insulin.<BR><br>It is also an antidiuretic agent.

 Packaging and Prices

Packaging Price (€) Quantité Buy Now
20 mg 230.00

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100 mg 920.00

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 Product Technical Documents
Safety Data Sheet Available on request, please Contact us
Ref. SDS_L9072 : unit price : free of charge
 Chemical and Physical Properties
Product code L9072  Molecular weight 230,67 g/mol (Anhyd.)
Product name DIAZOXIDE  Physical form white solid
CAS No. 364-98-7 Melting point 330-331 °C
RTECS DK8185000 Solubility In methanol
Slightly in dilute aqueous base
Insoluble in water.
UNIPROT Optical Activity
PubChem SID    
PubChem CID 3019    
Purity min. 99%.
TLC [Fluorescent silica gel, ethylacetate:methanol:ammonium hydroxide (68:16:12) or chloroform:methanol (90:10), detection under UV light].
Toxicity(LD50) rat (p.o.): 980 mg/kg; mice (p.o.): 444 mg/kg
mice (i.v.): 228 mg/kg
rat (i.p.): 510 mg/kg; mice (i.p.): 326 mg/kg
Chemical Name 7-chloro-3-methyl-2H-1,2,4-benzothiadiazine-1,1-dioxide    
Storage & Reconstitution

Store at room temperature

Savety Recommandations

For research Use only — Not intended for Food , Diagnostic or therapeutic use

 Bibliographic References
Product code L9072 
Product name DIAZOXIDE 

- Quast et al., "In vitro and in vivo comparison of two K+ channels openers, Diazoxide and Cromakalim, and their inhibition by Glibenclamide." J. Pharmacol. Exp. Ther. (1989). 250(1):261-271
- Trube et al., "Opposite effects of Tolbutamide and Diazoxide on the ATP-dependent K+ channel in mouse pancreatic beta-cells." Pflugers Arch. (1986) 407:493-499
- Dunne, "Protein phosphorylation is required for Diazoxide to open ATP-sensitive potassium channels in Insulin (RINm5F) secreting cells." FEBS Lett. (1989). 250(2):262-266
- Lebrun et al., "Similarities between the effects of Pinacidil and Diazoxide on ionic and secretory events in rat pancreatic islets." J. Pharmacol. Exp. Ther. (1989). 250:1011
- Ashford et al., J. Physiol. (1989). 409:53P
- VIDAL Dictionary, Ed. du Vidal, Paris, (1994). 705
Product code L9072 
Product name DIAZOXIDE 
External Links PubMed
Biomedical Citations From PubMed
Toxicology Citations From PubMed
PubChem CID
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