| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg | |||
| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
Small-conductance calcium-activated potassium (KCa2) channels, specifically KCa2.1 (SK1). As an activator, GW542573X enhances the activity of these channels, which are involved in neuronal excitability and other physiological processes.
|
|---|---|
| ln Vitro |
GW542573X activates KCa2.1 channels with an EC50 of 8.2 µM in HEK293 cells expressing hKCa2.1. It induces a left shift in the Ca2+ response curve of hSK1 from an EC50 (Ca2+) value of 410 nM to 240 nM, indicating that it potentiates the channel's sensitivity to calcium.
|
| ln Vivo |
Specific in vivo activity data for GW542573X are not detailed in the available literature. As a KCa2 channel activator, it could have effects on neuronal excitability and could be relevant for neurological disorders. However, specific animal model studies are not described.
|
| Enzyme Assay |
The in vitro assay for KCa2 channel activation involves measuring the activity of KCa2 channels in the presence of GW542573X. This can be done using patch-clamp electrophysiology in cells expressing KCa2.1. The compound is applied at various concentrations, and the enhancement of channel current is measured. The EC50 is determined from the dose-response curve.
|
| Cell Assay |
Specific in vitro cell-based assay protocols for GW542573X are not detailed. Its activity can be assessed in HEK293 cells expressing hKCa2.1 by measuring the channel current using patch-clamp electrophysiology. This is a direct measure of its modulatory activity.
|
| Animal Protocol |
Specific in vivo animal model protocols for GW542573X are not described. To evaluate its in vivo activity, GW542573X could be administered to animal models of neurological disorders where KCa2 channels play a role. Endpoints would depend on the specific model.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for GW542573X 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 GW542573X 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.
|
| Additional Infomation |
GW542573X is a research tool for studying KCa2 channel function and for investigating the role of these channels in neuronal-related diseases. It is a first-in-class selective KCa2.1 activator and is not an approved therapeutic agent.
|
| Molecular Formula |
C19H28N2O5
|
|---|---|
| Molecular Weight |
364.44
|
| Exact Mass |
364.2
|
| CAS # |
660846-41-3
|
| PubChem CID |
24885053
|
| Appearance |
White to off-white solid powder
|
| LogP |
3.842
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
26
|
| Complexity |
469
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(C)(OC(N1CCC(COC(NC2=CC=CC=C2OC)=O)CC1)=O)C
|
| InChi Key |
SAXGSDIZIYFNKD-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H28N2O5/c1-19(2,3)26-18(23)21-11-9-14(10-12-21)13-25-17(22)20-15-7-5-6-8-16(15)24-4/h5-8,14H,9-13H2,1-4H3,(H,20,22)
|
| Chemical Name |
tert-butyl 4-[(2-methoxyphenyl)carbamoyloxymethyl]piperidine-1-carboxylate
|
| Synonyms |
GW-542573X; GW 542573X; GW542573X
|
| 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 : ~125 mg/mL (~342.99 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 | 2.7439 mL | 13.7197 mL | 27.4394 mL | |
| 5 mM | 0.5488 mL | 2.7439 mL | 5.4879 mL | |
| 10 mM | 0.2744 mL | 1.3720 mL | 2.7439 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
