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| 10mg |
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| Targets |
KCNQ1 activator-1 targets the KCNQ1 potassium channel (also known as Kv7.1), which plays a crucial role in regulating cardiac repolarization and other physiological processes. The KCNQ1 channel is essential for the proper functioning of the heart and is involved in conditions such as Long QT syndrome. By activating this channel, the compound enhances potassium ion flow and helps maintain normal cardiac rhythm.
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| ln Vitro |
In vitro, KCNQ1 activator-1 activates the Kv7.1 channel expressed in CHO cells, leading to depolarization-induced thallium influx within 3 minutes, as determined by patch clamp assay. The compound demonstrates a wide range of bioactivities across various assays and is known to modulate splicing and enhance SMN2 splice variant expression. It is a potent activator with potential for research on Long QT syndrome.
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| ln Vivo |
In vivo, KCNQ1 activator-1 has the potential for the research of Long QT syndrome (LQTS). The compound may be used in animal models to study cardiac rhythm disorders and the effects of KCNQ1 channel activation on heart function. Detailed in vivo data regarding dosage, administration routes, and specific efficacy endpoints are limited in the available literature.
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| Enzyme Assay |
KCNQ1 activator-1's receptor-binding activity has been characterized using patch clamp assays in CHO cells expressing the Kv7.1 channel. The compound activates the channel, leading to thallium influx, which is measured as an indicator of channel activity. Binding affinity and activation kinetics can be determined using standard electrophysiological techniques.
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| Cell Assay |
In vitro cell experiments with KCNQ1 activator-1 typically use CHO cells expressing the Kv7.1 channel. Cells are treated with the compound at various concentrations, and channel activity is measured using patch clamp electrophysiology or thallium influx assays. The compound's effects on channel activation, ion flow, and cellular excitability are assessed.
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| Animal Protocol |
In vivo animal studies with KCNQ1 activator-1 have been conducted using rodent models of Long QT syndrome. The compound is typically administered via oral gavage or intravenous injection. Detailed protocols regarding dosage, treatment duration, and specific animal models are not extensively reported in the available literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic data specific to KCNQ1 activator-1 are limited in the available literature. As a small molecule with a molecular weight of 457.6 g/mol and an XLogP3 of 3.9, the compound is expected to have reasonable oral bioavailability and tissue penetration. Further pharmacokinetic studies are needed to fully characterize its absorption, distribution, metabolism, and excretion properties.
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| Toxicity/Toxicokinetics |
KCNQ1 activator-1 is considered safe for research use at typical concentrations. As a research compound, it is intended for laboratory use only and not for human consumption. The compound should be handled under standard laboratory safety practices with appropriate precautions.
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| Additional Infomation |
KCNQ1 activator-1 (compound 3) is a potent activator of the KCNQ1 channel with potential for the research of Long QT syndrome (LQTS). The compound has a molecular formula of C22H23N3O4S2, a molecular weight of 457.6 g/mol, and a PubChem CID of 4880560. It is stored under recommended conditions and is primarily used in cardiovascular research.
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| Molecular Formula |
C22H23N3O4S2
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|---|---|
| Molecular Weight |
457.57
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| Exact Mass |
457.112
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| CAS # |
1008671-38-2
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| PubChem CID |
4880560
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| Appearance |
Typically exists as solid at room temperature
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| Flash Point |
312.4±37.0 °C(Predicted)
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| LogP |
3.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
31
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| Complexity |
700
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1(S(C2=CC=CC=C2)(=O)=O)CCCCC1C(NC1=NC(C2=CC=C(OC)C=C2)=CS1)=O
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| InChi Key |
UUTYPVHYRISWDI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H23N3O4S2/c1-29-17-12-10-16(11-13-17)19-15-30-22(23-19)24-21(26)20-9-5-6-14-25(20)31(27,28)18-7-3-2-4-8-18/h2-4,7-8,10-13,15,20H,5-6,9,14H2,1H3,(H,23,24,26)
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| Chemical Name |
1-(benzenesulfonyl)-N-[4-(4-methoxyphenyl)-1,3-thiazol-2-yl]piperidine-2-carboxamide
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~546.36 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.55 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 | 2.1855 mL | 10.9273 mL | 21.8546 mL | |
| 5 mM | 0.4371 mL | 2.1855 mL | 4.3709 mL | |
| 10 mM | 0.2185 mL | 1.0927 mL | 2.1855 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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