Diazoxide (Synonyms: NSC 64198, NSC 76130, SRG 95213) |
| Catalog No.GC11598 |
positive allosteric modulator of the AMPA and kainate receptors
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Cas No.: 364-98-7
Sample solution is provided at 25 µL, 10mM.
3-Methyl-7-chloro-1,2,4-benzothiadiazine 1,1-dioxide (Sch-6783) is an ATP-sensitive potassium channel activator, can be used to treat hyperinsulinism.
3-Methyl-7-chloro-1,2,4-benzothiadiazine 1,1-dioxide (Sch-6783) has a number of physiological effects, including lowering the blood pressure and rectifying hypoglycemia. Diazoxide has powerful protective properties against cardiac ischemia[1].
3-Methyl-7-chloro-1,2,4-benzothiadiazine 1,1-dioxide (Sch-6783) 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].
3-Methyl-7-chloro-1,2,4-benzothiadiazine 1,1-dioxide (Sch-6783) attenuates postresuscitation brain injury, protects mitochondrial function, inhibits brain cell apoptosis, and activates the PKC pathway by opening mitoKATP channels[3]. Treatment with 3-Methyl-7-chloro-1,2,4-benzothiadiazine 1,1-dioxide (Sch-6783) 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].
Reference:
[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.
Cell experiment: | 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 experiment: | 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. | |
| Cas No. | 364-98-7 | SDF | |
| Synonyms | NSC 64198, NSC 76130, SRG 95213 | ||
| Chemical Name | 7-chloro-3-methyl-4H-benzo[e][1,2,4]thiadiazine 1,1-dioxide | ||
| Canonical SMILES | ClC1=CC=C2NC(C)=NS(=O)(C2=C1)=O | ||
| Formula | C8H7ClN2O2S | M.Wt | 230.67 |
| Solubility | ≥ 10.4mg/mL in DMSO | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.3352 mL | 21.676 mL | 43.352 mL |
| 5 mM | 0.867 mL | 4.3352 mL | 8.6704 mL |
| 10 mM | 0.4335 mL | 2.1676 mL | 4.3352 mL |
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- Purity: >99.50%
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