diazoxide

Modify Date: 2024-01-02 00:49:29

diazoxide Structure
diazoxide structure
Common Name diazoxide
CAS Number 364-98-7 Molecular Weight 230.671
Density 1.6±0.1 g/cm3 Boiling Point 414.8±47.0 °C at 760 mmHg
Molecular Formula C8H7ClN2O2S Melting Point >310°C
MSDS Chinese USA Flash Point 204.6±29.3 °C
Symbol GHS07
GHS07
Signal Word Warning

 Use of diazoxide


Diazoxide is an ATP-sensitive potassium channel activator ; can be used to treat hyperinsulinism.

 Names

Name diazoxide
Synonym More Synonyms

 diazoxide Biological Activity

Description Diazoxide is an ATP-sensitive potassium channel activator ; can be used to treat hyperinsulinism.
Related Catalog
In Vitro Diazoxide has a number of physiological effects, including lowering the blood pressure and rectifying hypoglycemia. Diazoxide has powerful protective properties against cardiac ischemia[1].Diazoxide could protect NSC-34 neurons against the main sources of neurodegenerative damage. Diazoxide increases Nrf2 nuclear translocation in NSC-34 motoneurons and prevents endogenous oxidative damage[2].
In Vivo Diazoxide attenuates postresuscitation brain injury, protects mitochondrial function, inhibits brain cell apoptosis, and activates the PKC pathway by opening mitoKATP channels[3]. Treatment with diazoxide in wild-type mice decreases intraocular pressure (IOP) by 21.5±3.2% with an absolute IOP reduction of 3.9 ± 0.6 mm Hg[4].
Cell Assay Diazoxide is dissolved in DMSO to prepare 50 mM stock solution. NSC-34 cells are allowed to differentiate for 8 weeks under reduced serum conditions and then seeded in 24-well plates. Glutamate is dissolved in culture medium and added to cultures at concentration of 10 μM for 24 h. Cell treatment with 100 µM diazoxide starts 2 h before glutamate exposure. Cell viability is measured by the MTT assay[2].
Animal Admin Rats: Adult male Sprague-Dawley rats with induced cerebral ischemia (n=10 per group) receive an intraperitoneal injection of 0.1% DMSO (1 mL; vehicle group), diazoxide (10 mg/kg; DZ group), or diazoxide (10 mg/kg) plus 5-hydroxydecanoate (5 mg/kg; DZ + 5-HD group) 30 min after CPR. The control group (sham group, n=5) undergoes sham operation, without cardiac arrest. Mitochondrial respiratory control rate (RCR) is determined. Brain cell apoptosis is assessed using TUNEL staining. Expression of Bcl-2, Bax, and protein kinase C epsilon (PKCε) in the cerebral cortex is determined by Western blotting and immunohistochemistry[3]. Mouse: Diazoxide is prepared by diluting a 100 mM stock solution in 10% polyethoxylated castor oil in PBS. In C57BL/6 wild-type and Kir6.2(−/−) mice, a 5 μL drop of 5 mM diazoxide is topically administered to one eye of each mouse while the fellow control eye received vehicle (DMSO and 10% polyethoxylated castor oil in the same proportion as the treated eye). IOP is measured daily at 1 hour, 4 hours, and 23 hours following treatment. Treatment with diazoxide and vehicle is continued daily for 14 consecutive days[4].
References

[1]. Coetzee WA, et al. Multiplicity of effectors of the cardioprotective agent, diazoxide. Pharmacol Ther. 2013 Nov;140(2):167-75.

[2]. Virgili N, et al. K(ATP) channel opener diazoxide prevents neurodegeneration: a new mechanism of action viaantioxidative pathway activation. PLoS One. 2013 Sep 11;8(9):e75189.

[3]. Wu H, et al. Diazoxide Attenuates Postresuscitation Brain Injury in a Rat Model of Asphyxial Cardiac Arrest by Opening Mitochondrial ATP-Sensitive Potassium Channels. Biomed Res Int. 2016;2016:1253842.

[4]. Chowdhury UR, et al. ATP-sensitive potassium (K(ATP)) channel openers diazoxide and nicorandil lower intraocular pressure in vivo. Invest Ophthalmol Vis Sci. 2013 Jul 22;54(7):4892-9.

 Chemical & Physical Properties

Density 1.6±0.1 g/cm3
Boiling Point 414.8±47.0 °C at 760 mmHg
Melting Point >310°C
Molecular Formula C8H7ClN2O2S
Molecular Weight 230.671
Flash Point 204.6±29.3 °C
Exact Mass 229.991669
PSA 66.91000
LogP 1.08
Vapour Pressure 0.0±1.0 mmHg at 25°C
Index of Refraction 1.692
Storage condition Store at RT
Water Solubility 0.1 M NaOH: soluble

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
DK8185000
CHEMICAL NAME :
2H-1,2,4-Benzothiadiazine, 7-chloro-3-methyl-, 1,1-dioxide
CAS REGISTRY NUMBER :
364-98-7
LAST UPDATED :
199504
DATA ITEMS CITED :
7
MOLECULAR FORMULA :
C8-H7-Cl-N2-O2-S
MOLECULAR WEIGHT :
230.68
WISWESSER LINE NOTATION :
T66 BSWM ENJ D1 IG

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
980 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 143,446,1963
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
510 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 143,446,1963
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
444 mg/kg
TOXIC EFFECTS :
Vascular - BP lowering not characterized in autonomic section
REFERENCE :
JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 136,344,1962
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
326 mg/kg
TOXIC EFFECTS :
Vascular - BP lowering not characterized in autonomic section
REFERENCE :
JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 136,344,1962
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
228 mg/kg
TOXIC EFFECTS :
Vascular - BP lowering not characterized in autonomic section
REFERENCE :
JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 136,344,1962 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
65 mg/kg
SEX/DURATION :
female 110-114 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - other effects to embryo
REFERENCE :
JCNDBK Journal of Clinical Pharmacology and New Drugs. (Stamford, CT) V.11-13, 1971-73. For publisher information, see JCPCBR. Volume(issue)/page/year: 11,206,1971 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X7114 No. of Facilities: 63 (estimated) No. of Industries: 1 No. of Occupations: 3 No. of Employees: 612 (estimated) No. of Female Employees: 395 (estimated)

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302-H315-H319-H335
Precautionary Statements P261-P305 + P351 + P338
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes Xn: Harmful;
Risk Phrases R22;R36/37/38
Safety Phrases S22;S26;S36
RIDADR NONH for all modes of transport
WGK Germany 3
RTECS DK8185000
HS Code 2933990090

 Synthetic Route

~90%

diazoxide Structure

diazoxide

CAS#:364-98-7

Literature: Khelili, Smail; Faury, Gilles; Nicolle, Edwige; Verdetti, Jean; Leclerc, Gerard Medicinal Chemistry Research, 2003 , vol. 12, # 9 p. 457 - 470

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diazoxide Structure

diazoxide

CAS#:364-98-7

Literature: Medicinal Chemistry Research, , vol. 12, # 9 p. 457 - 470

~%

diazoxide Structure

diazoxide

CAS#:364-98-7

Literature: Medicinal Chemistry Research, , vol. 12, # 9 p. 457 - 470

~%

diazoxide Structure

diazoxide

CAS#:364-98-7

Literature: Medicinal Chemistry Research, , vol. 12, # 9 p. 457 - 470

~%

diazoxide Structure

diazoxide

CAS#:364-98-7

Literature: Medicinal Chemistry Research, , vol. 12, # 9 p. 457 - 470

 Customs

HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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 Synonyms

diazoxidum [INN_la]
7-chloro-3-methyl-4H-1λ<sup>6</sup>,2,4-benzothiadiazine 1,1-dioxide
Hypertonalum
Diazoxido
7-chloro-3-methyl-4H-1,2,4-benzothiadiazine 1,1-dioxide
Sodium dodecyl sulphate solution
EINECS 206-668-1
Mutabase
Proglycem
Dizoxide
Diazossido
MFCD00078578
diazoxide
Eudemine
Proglicem
2H-1,2,4-Benzothiadiazine, 7-chloro-3-methyl-, 1,1-dioxide
7-chloro-3-methyl-1,2,4-benzothiadiazine-1,1-dioxide
Hyperstat
7-Chloro-3-methyl-2H-1,2,4-benzothiadiazine 1,1-dioxide
7-chloro-3-méthyl-2H-1,2,4-benzothiadiazine-1,1-dioxyde
3-Methyl-7-chloro-1,2,4-benzothiadiazine 1,1-dioxide
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  • Product Name: Diazoxide
  • Price: $100.0/100mg $200.0/250mg $400.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao



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Price: $66/10mM*1mLinDMSO

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