| Size | Price | Stock | Qty |
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Purity: ≥98%
Diazoxide (also known as Proglycem) is a potassium channel activator used to treat hyperinsulinism. It causes local relaxation in smooth muscle by increasing membrane permeability to potassium ions. This switches off voltage-gated calcium ion channels, preventing calcium flux across the sarcolemma and activation of the contractile apparatus. This agent also inhibits insulin release by interacting with ATP-sensitive potassium channels of pancreatic islet beta-cells.
| ln Vitro |
Among its many physiological effects is the reduction of hypertension and hypotension caused by dialezoxide (Sch-6783). Strong antioxidant protection qualities are exhibited by dialzoxide [1]. Diazoxide (Sch-6783) shields NSC-34 neurons, which are a primary cause of neurological damage in the cardiovascular system. In NSC-34 motor neurons, dialzoxide promotes Nrf2 nuclear translocation and guards against endogenous oxidative damage [2].
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| ln Vivo |
Diazoxide (Sch-6783) can reduce brain damage following resuscitation, protect mitochondrial function, block brain cell shutdown, and activate PKC blue by activating mitoKATP channels [3]. Diazoxide (Sch-6783) therapy lowered intraocular pressure (ocular pressure) by 21.5 ± 3.2% in wild-type mice, with an absolute IOP reduction of 3.9 ± 0.6 mm Hg [4].
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| 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 |
| Molecular Formula |
C8H7CLN2O2S
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|---|---|
| Molecular Weight |
230.6714
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| CAS # |
364-98-7
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| Related CAS # |
Diazoxide-d3;1432063-51-8
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| SMILES |
CC1=NS(=O)(=O)C2=C(N1)C=CC(=C2)Cl
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| InChi Key |
GDLBFKVLRPITMI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H7ClN2O2S/c1-5-10-7-3-2-6(9)4-8(7)14(12,13)11-5/h2-4H,1H3,(H,10,11)
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| Chemical Name |
7-chloro-3-methyl-4H-1$l^{6},2,4-benzothiadiazine 1,1-dioxide
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| Synonyms |
Sch-6783; SRG-95213; Sch6783; SRG95213; Sch 6783; SRG 95213; Eudemine; Hyperstat; Proglycem; Hypertonalum; Proglicem
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 35 mg/mL (~151.73 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (9.02 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (9.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3352 mL | 21.6760 mL | 43.3520 mL | |
| 5 mM | 0.8670 mL | 4.3352 mL | 8.6704 mL | |
| 10 mM | 0.4335 mL | 2.1676 mL | 4.3352 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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