| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Small conductance calcium-activated potassium (SK) channels. GW354586X is an inhibitor that blocks these channels by interacting with the apamin binding site.
|
|---|---|
| ln Vitro |
ICA, an inhibitor of SK channel, has antiarrhythmic properties. In the isolated right atrium, ICA inhibits electrically induced atrial fibrillation, causes atrial refractoriness postrepolarization, and depolarizes the resting membrane potential. Conduction velocity is slowed by ICA at 1 to 10 μM. Significant suppression of other sodium channel-dependent parameters is observed upon increasing pacing frequency when SK channels are inhibited by ICA (10-30 μM) [2].
GW354586X inhibits SK channels. It has anti-Leishmania activity with an IC50 of 2.1 µM. In isolated right atria, it inhibits electrically induced atrial fibrillation, causes atrial post-repolarization refractoriness, and depolarizes the resting membrane potential. It slows conduction velocity at 1 to 10 µM. |
| ln Vivo |
In isolated right atria, GW354586X inhibits electrically induced atrial fibrillation, causes atrial post-repolarization refractoriness, and depolarizes the resting membrane potential. It slows conduction velocity at 1 to 10 µM. These effects are consistent with its SK channel inhibitory activity and suggest anti-arrhythmic potential.
|
| Enzyme Assay |
The in vitro assay for SK channel inhibition involves measuring the activity of SK channels in the presence of GW354586X. This can be done using patch-clamp electrophysiology in cells expressing SK channels. The compound is applied at various concentrations, and the inhibition of channel current is measured. The IC50 is determined from the dose-response curve.
|
| Cell Assay |
Specific in vitro cell-based assay protocols for GW354586X are not detailed. Its anti-Leishmania activity can be assessed in Leishmania-infected macrophages or in axenic amastigote cultures. Cells are treated with GW354586X, and the reduction in parasite load is measured.
|
| Animal Protocol |
Specific in vivo animal model protocols for GW354586X are not described. Its anti-arrhythmic effects could be evaluated in animal models of atrial fibrillation. Its anti-Leishmania activity could be evaluated in mouse models of Leishmaniasis. However, specific studies are not detailed.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for GW354586X are not reported in the available literature. As a research compound, its absorption, distribution, metabolism, and excretion (ADME) properties have not been extensively characterized.
|
| Toxicity/Toxicokinetics |
Specific toxicological data for GW354586X are not available. As a research compound, its safety profile has not been comprehensively characterized. Toxicity studies would be required to determine its safety margin and potential off-target effects.
|
| References |
[1]. Bhuniya D, et al. Aminothiazoles: Hit to lead development to identify antileishmanial agents. Eur J Med Chem. 2015 Sep 18;102:582-93.
[2]. Skibsbye L, et al. Antiarrhythmic Mechanisms of SK Channel Inhibition in the Rat Atrium. J Cardiovasc Pharmacol. 2015 Aug;66(2):165-76. |
| Additional Infomation |
SK channel inhibitors
GW354586X is a research tool for studying SK channel function and for investigating the role of these channels in various physiological and pathological processes, including cardiac arrhythmias and parasitic infections. It is not an approved therapeutic agent. |
| Molecular Formula |
C13H10N4S
|
|---|---|
| Molecular Weight |
254.31
|
| Exact Mass |
254.062
|
| CAS # |
3374-88-7
|
| PubChem CID |
772885
|
| Appearance |
Light brown to brown solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
466.4±48.0 °C at 760 mmHg
|
| Flash Point |
235.9±29.6 °C
|
| Vapour Pressure |
0.0±1.2 mmHg at 25°C
|
| Index of Refraction |
1.694
|
| LogP |
1.39
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
18
|
| Complexity |
263
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1(NC2=NC(C3=NC=CC=C3)=CS2)=NC=CC=C1
|
| InChi Key |
RYCUBTFYRLAMFA-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C13H10N4S/c1-3-7-14-10(5-1)11-9-18-13(16-11)17-12-6-2-4-8-15-12/h1-9H,(H,15,16,17)
|
| Chemical Name |
N,4-dipyridin-2-yl-1,3-thiazol-2-amine
|
| Synonyms |
GW 354586 X; GW-354586-X; GW354586X
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ≥ 49.5 mg/mL (~194.64 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9322 mL | 19.6610 mL | 39.3221 mL | |
| 5 mM | 0.7864 mL | 3.9322 mL | 7.8644 mL | |
| 10 mM | 0.3932 mL | 1.9661 mL | 3.9322 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
