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Dichlorphenamide

CAS# 120-97-8

Dichlorphenamide

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Dichlorphenamide

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Chemical Properties of Dichlorphenamide

Cas No. 120-97-8 SDF Download SDF
PubChem ID 3038 Appearance Powder
Formula C6H6Cl2N2O4S2 M.Wt 305.16
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Diclofenamide
Solubility DMSO : 100 mg/mL (327.70 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name 4,5-dichlorobenzene-1,3-disulfonamide
SMILES C1=C(C=C(C(=C1S(=O)(=O)N)Cl)Cl)S(=O)(=O)N
Standard InChIKey GJQPMPFPNINLKP-UHFFFAOYSA-N
Standard InChI InChI=1S/C6H6Cl2N2O4S2/c7-4-1-3(15(9,11)12)2-5(6(4)8)16(10,13)14/h1-2H,(H2,9,11,12)(H2,10,13,14)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Dichlorphenamide

DescriptionDichlorphenamide(Diclofenamide) is a carbonic anhydrase inhibitor that is used in the treatment of glaucoma. Target: Carbonic Anhydrase Dichlorphenamide is a sulfonamide and a carbonic anhydrase inhibitor of the meta-Disulfamoylbenzene class. This drug has the same side-effects as acetazolamide, for which it is a useful substitute, except for a lesser tendency to cause dermatitis, renal calculi and metabolic acidosis. It may induce a more pronounced renal loss of potassium [1]. An average daily dose of 33 mg of diclofenamide, a carbonic-anhydrase inhibitor, was added to the anti-epileptic medication already employed in 105 cases of severe epilepsy which had shown insufficient clinical improvement. A favourable action on seizures, often accompanied by an improvement in the EEG tracing, was observed in 83 cases. The effect was of long duration in 47 cases in that it lasted for more than a year. It persisted for one to twelve months in a further 17 cases, while in 19 patients, who had reacted favourably to the treatment, medication had to be suspended because of intolerance [2].

References:
[1]. Kanski, J.J., Carbonic anhydrase inhibitors and osmotic agents in glaucoma. Carbonic anhydrase inhibitors. Br J Ophthalmol, 1968. 52(8): p. 642-3. [2]. Rucquoy, M. and L. Sorel, Diclofenamide in the treatment of therapy-resistant epilepsy. Acta Neurol Belg, 1978. 78(3): p. 174-82.

Dichlorphenamide Dilution Calculator

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Dichlorphenamide Molarity Calculator

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Preparing Stock Solutions of Dichlorphenamide

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.277 mL 16.3848 mL 32.7697 mL 65.5394 mL 81.9242 mL
5 mM 0.6554 mL 3.277 mL 6.5539 mL 13.1079 mL 16.3848 mL
10 mM 0.3277 mL 1.6385 mL 3.277 mL 6.5539 mL 8.1924 mL
50 mM 0.0655 mL 0.3277 mL 0.6554 mL 1.3108 mL 1.6385 mL
100 mM 0.0328 mL 0.1638 mL 0.3277 mL 0.6554 mL 0.8192 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Dichlorphenamide

Dichlorphenamide is a carbonic anhydrase inhibitor. Carbonic anhydrase is a protein in your body.

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References on Dichlorphenamide

Dichlorphenamide: A Review in Primary Periodic Paralyses.[Pubmed:26941026]

Drugs. 2016 Mar;76(4):501-7.

Oral Dichlorphenamide (Keveyis) is a carbonic anhydrase inhibitor that is approved in the USA for the treatment of primary hyperkalaemic and hypokalaemic periodic paralyses and related variants. The efficacy and safety of Dichlorphenamide in patients with primary periodic paralyses have been evaluated in four 9-week, randomized, double-blind, placebo-controlled, phase III trials [two parallel-group trials (HOP and HYP) and two crossover trials]. In two trials in patients with hypokalaemic periodic paralysis, Dichlorphenamide was associated with a significantly (eightfold) lower paralytic attack rate and fewer patients with acute intolerable worsening compared with placebo. In two trials in patients with hyperkalaemic periodic paralysis, the attack rate was lower with Dichlorphenamide than placebo, with this comparison reaching statistical significance in one trial (crossover) but not the other (HYP), although the attack rate was approximately fivefold lower with Dichlorphenamide than placebo in the HYP trial. In 52-week, open-label extensions of the HOP and HYP trials, Dichlorphenamide provided sustained efficacy in patients with hypokalaemic or hyperkalaemic periodic paralysis. Dichlorphenamide was generally well tolerated in all four phase III trials and during the extension trials; the most common adverse events were paraesthesia, cognitive disorders and dysgeusia. As the first agent to be approved in the USA for this indication, Dichlorphenamide is a valuable treatment option for patients with primary hyperkalaemic or hypokalaemic periodic paralysis.

Randomized, placebo-controlled trials of dichlorphenamide in periodic paralysis.[Pubmed:26865514]

Neurology. 2016 Apr 12;86(15):1408-1416.

OBJECTIVE: To determine the short-term and long-term effects of Dichlorphenamide (DCP) on attack frequency and quality of life in hyperkalemic (HYP) and hypokalemic (HOP) periodic paralysis. METHODS: Two multicenter randomized, double-blind, placebo-controlled trials lasted 9 weeks (Class I evidence), followed by a 1-year extension phase in which all participants received DCP. Forty-four HOP and 21 HYP participants participated. The primary outcome variable was the average number of attacks per week over the final 8 weeks of the double-blind phase. RESULTS: The median attack rate was lower in HOP participants on DCP than in participants on placebo (0.3 vs 2.4, p = 0.02). The 9-week mean change in the Physical Component Summary score of the Short Form-36 was also better in HOP participants receiving DCP (treatment effect = 7.29 points, 95% confidence interval 2.26 to 12.32, p = 0.006). The median attack rate was also lower in HYP participants on DCP (0.9 vs 4.8) than in participants on placebo, but the difference in median attack rate was not significant (p = 0.10). There were no significant effects of DCP on muscle strength or muscle mass in either trial. The most common adverse events in both trials were paresthesia (47% DCP vs 14% placebo, both trials combined) and confusion (19% DCP vs 7% placebo, both trials combined). CONCLUSIONS: DCP is effective in reducing the attack frequency, is safe, and improves quality of life in HOP periodic paralysis. CLASSIFICATION OF EVIDENCE: These studies provide Class I evidence that DCP significantly reduces attack frequency in HOP but lacked the precision to support either efficacy or lack of efficacy of DCP in HYP.

Description

Dichlorphenamide(Diclofenamide) is a carbonic anhydrase inhibitor that is used in the treatment of glaucoma.

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