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Retigabine dihydrochloride

Catalog No.GC12599

An Analytical Reference Standard

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Retigabine dihydrochloride Chemical Structure

Cas No.: 150812-13-8

Size Price Stock Qty
10mM (in 1mL DMSO)
$55.00
In stock
5mg
$37.00
In stock
10mg
$56.00
In stock
50mg
$148.00
In stock
100mg
$235.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

Chinese hamster ovary (CHO-K1) cells transfected with the KCNQ2/Q3 tandem construct (CHO-KCNQ2/Q3)

Preparation method

This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

0.1 ~ 10 μM

Applications

Retigabine Dihydrochloride (0.1 ~ 10 μM) induced a potassium current and hyperpolarized CHO-KCNQ2/Q3 cells but not in wild-type cells.

Animal experiment [2]:

Animal models

Mouse 6-Hz psychomotor seizure models

Dosage form

26 or 33 mg/kg; i.p.

Applications

In the 6-Hz psychomotor seizure model, Retigabine Dihydrochloride dose-dependently blocked seizures induced by either 32 or 44 mA current stimulation.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Wickenden AD, Yu W, Zou A, Jegla T, Wagoner PK. Retigabine, a novel anti-convulsant, enhances activation of KCNQ2/Q3 potassium channels. Mol Pharmacol. 2000 Sep;58(3):591-600.

[2]. Large CH, Sokal DM, Nehlig A, Gunthorpe MJ, Sankar R, Crean CS, Vanlandingham KE, White HS. The spectrum of anticonvulsant efficacy of retigabine (ezogabine) in animal models: implications for clinical use. Epilepsia. 2012 Mar;53(3):425-36.

Background

IC50: N/A

Retigabine is a first-in-class K+ channel (KCNQ) opener. KCNQ channels are reported to be expressed predominantly in neurons and are critical determinants of cellular excitability, as shown by the occurrence of human genetic mutations in KCNQ channels which underlie inheritable disorders including the syndrome of benign familial neonatal convulsions.

In vitro: Retigabine was found to combine a novel mode of actions, which were namely potassium channel opening (KCNQ2, KCNQ3 as well as KCNQ4 channels). Retigabine also showed activities with some potentiation of gamma amino butyric acid (GABA)-evoked currents at its higher concentrations [1].

In vivo: Animal models of epileptic seizures showed that retigabine treatment was effective at an oral dose as low as 0.01 mg/kg. Studies performed in mice also indicated that combining retigabine with another anticonvulsant agent leads to an additive effect [1].

Clinical trial: A clinical interaction study showed that there was no pharmacokinetic interaction between phenobarbitone and retigabine in healthy subjects. Thus, no dosage adjustment is likely to be necessary when phenobarbitone and retigabine are coadministered to patients [1].

Reference:
[1] Ferron GM,Patat A,Parks V,Rolan P,Troy SM.  Lack of pharmacokinetic interaction between retigabine and phenobarbitone at steady-state in healthy subjects. Br J Clin Pharmacol.2003 Jul;56(1):39-45.

Chemical Properties

Cas No. 150812-13-8 SDF
Chemical Name ethyl N-[2-amino-4-[(4-fluorophenyl)methylamino]phenyl]carbamate;dihydrochloride
Canonical SMILES CCOC(=O)NC1=C(C=C(C=C1)NCC2=CC=C(C=C2)F)N.Cl.Cl
Formula C16H20Cl2FN3O2 M.Wt 376.25
Solubility ≥ 18.8 mg/mL in DMSO, ≥ 8.71 mg/mL in EtOH with ultrasonic and warming, ≥ 52.4 mg/mL in Water with gentle warming Storage Store at -20°C
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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.6578 mL 13.289 mL 26.5781 mL
5 mM 0.5316 mL 2.6578 mL 5.3156 mL
10 mM 0.2658 mL 1.3289 mL 2.6578 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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