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DIAZOXIDE

DIAZOXIDE
DIAZOXIDE structure
CAS No.
364-98-7
Chemical Name:
DIAZOXIDE
Synonyms
Eudemine;Sch-6783;mutabase;srg95213;dizoxide;hyperstat;NSC-64198;proglicem;DIAZOXIDE;Diazoxided
CBNumber:
CB8426893
Molecular Formula:
C8H7ClN2O2S
Formula Weight:
230.67
MOL File:
364-98-7.mol

DIAZOXIDE Properties

Melting point:
>310°C
Density 
1.3767 (rough estimate)
refractive index 
1.6300 (estimate)
storage temp. 
Store at RT
solubility 
0.1 M NaOH: soluble
pka
pKa 8.5 (Uncertain)
form 
neat
Water Solubility 
Soluble in 0.1M NaOH. Insoluble in water or in methanol.
λmax
268nm(MeOH)(lit.)
Merck 
14,3004
SAFETY
  • Risk and Safety Statements
  • Hazard and Precautionary Statements (GHS)
Hazard Codes  Xn
Risk Statements  22-36/37/38
Safety Statements  22-26-36
WGK Germany  3
RTECS  DK8185000
HS Code  2934990002
Symbol(GHS):
Signal word: Warning
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H302 Harmful if swallowed Acute toxicity,oral Category 4 Warning P264, P270, P301+P312, P330, P501
H315 Causes skin irritation Skin corrosion/irritation Category 2 Warning P264, P280, P302+P352, P321,P332+P313, P362
H319 Causes serious eye irritation Serious eye damage/eye irritation Category 2A Warning P264, P280, P305+P351+P338,P337+P313P
H335 May cause respiratory irritation Specific target organ toxicity, single exposure;Respiratory tract irritation Category 3 Warning
Precautionary statements:
P261 Avoid breathing dust/fume/gas/mist/vapours/spray.
P304+P340 IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338 IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P405 Store locked up.

DIAZOXIDE price More Price(11)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich D9035 Diazoxide 364-98-7 1g $263 2018-11-13 Buy
Sigma-Aldrich 1186000 Diazoxide United States Pharmacopeia (USP) Reference Standard 364-98-7 200mg $348 2018-11-13 Buy
TCI Chemical D5402 Diazoxide >98.0%(HPLC)(T) 364-98-7 250mg $60 2018-11-22 Buy
TCI Chemical D5402 Diazoxide >98.0%(HPLC)(T) 364-98-7 1g $176 2018-11-22 Buy
Alfa Aesar J66010 Diazoxide, 98% 364-98-7 1g $316 2018-11-13 Buy

DIAZOXIDE Chemical Properties,Uses,Production

Chemical Properties

White Solid

Uses

wound healing agent

Uses

Diazoxide reduces status epilepticus neuron damage in diabetes.

Definition

ChEBI: A benzothiadiazine that is the S,S-dioxide of 2H-1,2,4-benzothiadiazine which is substituted at position 3 by a methyl group and at position 7 by chlorine. A peripheral vasodilator, it increases the oncentration of glucose in the plasma and inhibits the secretion of insulin by the beta- cells of the pancreas. It is used orally in the management of intractable hypoglycaemia and intravenously in the management of hypertensive emergencies.

brand name

Hyperstat (Schering); Proglycem (Baker Norton).

Biological Functions

Diazoxide (Hyperstat) is chemically similar to the thiazide diuretics. It is devoid of diuretic activity and causes Na+ and water retention. Diazoxide is a very potent vasodilator and is available only for intravenous use in the treatment of hypertensive emergencies. The mechanism by which diazoxide relaxes vascular smooth muscle is related to its ability to activate potassium channels and produce a hyperpolarization of the cell membrane.

General Description

Diazoxide is 7-chloro-3-methyl-4H-benzo[e][1,2,4]thiadiazine-1,1-dioxide , and is currentlyavailable in the United States only as a 50-mg/mLoral suspension (Proglycem); discontinued formulations includedcapsules for oral administration, and injectable formsthat typically found use for indications other than hypoglycemicconditions. Diazoxide is a cyclic benzenesulfonamide,although the free acid in solution can exist in threetautomeric forms, and the 4H tautomer most likely predominatesto a very high proportion. Partly because of theadditional nitrogen in the quinazoline ring structure, themolecule is somewhat more acidic (pKa~8.4, 8.6)than benzenesulfonamide (pKa~10).

General Description

Diazoxide is used as the sodium salt of7-chloro-3-methyl-2H-1,2,4-benzothiadiazine 1,1-dioxide(Hyperstat IV). Diazoxide lowers peripheral vascular resistance,increases cardiac output, and does not compromiserenal blood flow.
This is a des-sulfamoyl analog of the benzothiazine diureticsand has a close structural similarity to chlorothiazide. Itwas developed intentionally to increase the antihypertensiveaction of the thiazides and to minimize the diuretic effect.

Biological Activity

Antihypertensive, activates ATP-dependent K + channels. Induces activation of PKC ε , an intermediate in the opening of mitoK ATP channels, results in cardioprotection against hypoxia-induced death. Blocks desensitization of AMPA receptors.

Pharmacology

The hemodynamic effects of diazoxide are similar to those of hydralazine and minoxidil. It produces direct relaxation of arteriolar smooth muscle with little effect on capacitance beds. Since it does not impair cardiovascular reflexes, orthostasis is not a problem. Its administration is, however, associated with a reflex increase in cardiac output that partially counters its antihypertensive effects. Propranolol and other -blockers potentiate the vasodilating properties of the drug. Diazoxide has no direct action on the heart. Although renal blood flow and glomerular filtration may fall transiently, they generally return to predrug levels within an hour.

Clinical Use

Diazoxide is used by intravenous injection as a rapidly acting antihypertensiveagent for emergency reduction of blood pressurein hospitalized patients with accelerated or malignanthypertension. More than 90% is bound to serum protein, andcaution is needed when it is used in conjunction with otherprotein-bound drugs that may be displaced by diazoxide.The injection is given rapidly by the intravenous route toensure maximal effect. The initial dose is usually 1 mg/kg ofbody weight, with a second dose given if the first injectiondoes not lower blood pressure satisfactorily within 30 minutes.Further doses may be given at 4- to 24-hour intervalsif needed. Oral antihypertensive therapy is begun as soon aspossible.

Clinical Use

In contrast to the acute clinical uses of glucagon, diazoxidefinds use in chronic hypoglycemic conditions: inoperableislet cell adenoma or carcinomas, extrapancreatic malignanciesof insulin-secreting cells, or islet cell hyperplasias. Inchildren, additional indications include congenital hyperinsulinemia124and leucine sensitivity. Experimentally, diazoxideis among an array of ATP-sensitive potassium channel openersbeing studied for intermittently bringing aboutβ-cell rest.

Side effects

Since diazoxide is not often used for long-term treatment, toxicities associated with chronic use are rare.The chief concern is the side effects associated with the increased workload on the heart, which may precipitate myocardial ischemia and Na+ and water retention. These undesirable effects can be controlled by concurrent therapy with a β-blocker and a diuretic.
Diazoxide may cause hyperglycemia, especially in diabetics, so if the drug is used for several days, blood glucose levels should be measured. When used in the treatment of toxemia, diazoxide may stop labor, because it relaxes uterine smooth muscle.

Veterinary Drugs and Treatments

Oral diazoxide is used in canine and ferret medicine for the treatment of hypoglycemia secondary to hyperinsulin secretion (e.g., insulinoma). Insulinomas are apparently very rare in the cat; there is little experience with this drug in that species.
In human medicine, intravenous diazoxide is sometimes used for treating severe hypertension.

Metabolism

Diazoxide lowers blood pressure within 3 to 5 minutes after rapid intravenous injection, and its duration of action may be 4 to 12 hours. Interestingly, if diazoxide is either injected slowly or infused its hypotensive action is quite modest.This is believed to be due to a rapid and extensive binding of the drug to plasma proteins. Both the liver and kidney contribute to its metabolism and excretion.The plasma half-life is therefore prolonged in patients with chronic renal failure.

DIAZOXIDE Preparation Products And Raw materials

Raw materials

Preparation Products


DIAZOXIDE Suppliers

Global( 111)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21759 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20672 55
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 27142 58
hdzhl biotechnology co., ltd
86-13032617415
sales@luchibiology.com CHINA 914 58
Hebei Aicrowe Biotech Co., Ltd
0311-66855331
aicrowe@kf-chem.com CHINA 315 58
BOC Sciences
1-631-619-7922
1-631-614-7828 inquiry@bocsci.com United States 20116 58
Shanghai Synmedia Chemical Co., Ltd. +86 (21) 3868-1880
+86 (21) 3390-8196 sales@synmedia-chem.com China 158 58
Shanghai Elestone Pharmaceutical Technology Co., Ltd. 021-36680027/QQ:1762825045
sales@elestone.com.cn; sales2@elestone.com.cn China 296 58
hebei aicrowe co.,ltd 0311-66855331 15533616561
0311-66855331 parr-kf@hotmail.com China 12 58
Shanghai VastPro Technology Development Co., Ltd. 021-20608178
021-20608174 sales@vastprotech.com China 20 58

View Lastest Price from DIAZOXIDE manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2019-05-23 Diazoxide API
364-98-7
US $0.00 / g/Bag 10g 99% 80kg hdzhl biotechnology co., ltd
2019-07-09 DIAZOXIDE
364-98-7
US $1.00 / ASSAYS 1ASSAYS 98% 1kg,2kg,100kg career henan chemical co
2019-05-15 Diazoxided
364-98-7
US $1.00 / KG 1g 99% 500 Hebei Aicrowe Biotech Co., Ltd

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