| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg | |||
| 250mg | |||
| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
AUT1 targets voltage-gated potassium channels of the Kv3 family, specifically Kv3.1b and Kv3.2a. It is a positive allosteric modulator that enhances channel activity. AUT1 increases whole currents mediated by human Kv3.1b and Kv3.2a channels, with a concomitant leftward shift in the voltage-dependence of activation. It has a less potent effect on hKv3.3 currents. The EC₅₀ values are 4.7 and 4.9 µM for Kv3.1b and Kv3.2a, respectively.
|
|---|---|
| ln Vitro |
In human recombinants, AUT1 (1.5, 12.5, and 25 μM) modifies Kv3.1b and Kv3.2a channels with pEC50 values of 5.33 and 5.31 μM, respectively [1]. In a concentration-dependent manner, AUT1 increases total current mediated by human Kv3.1b and Kv3.2a channels [1]. Human Kv3.1b and Kv3.2a channel voltage dependency of activation and inactivation is changed by AUT1 (10 and 30 μM) [1]. EGFP-positive cortical interneurons fire rapidly, and AUT1 prevents this from happening at 1 and 10 μM [1].
In vitro, AUT1 increases the current mediated by human recombinant Kv3.1b and Kv3.2a channels. It has pEC₅₀ values of 5.33 and 5.31 µM for Kv3.1b and Kv3.2a channels, respectively. In a concentration-dependent manner, AUT1 increases total current mediated by human Kv3.1b and Kv3.2a channels. Human Kv3.1b and Kv3.2a channel voltage dependency of activation and inactivation is changed by AUT1 (10 and 30 µM). EGFP-positive cortical interneurons fire rapidly, and AUT1 prevents this from happening at 1 and 10 µM. |
| ln Vivo |
Specific in vivo data for AUT1 are not extensively detailed in the available literature. However, AUT1 increases tetraethylammonium-induced decreases in the firing frequency and amplitude of action potentials in mouse somatosensory cortex slices when used at concentrations of 1 and 10 µM. By enhancing Kv3 channel activity, it promotes rapid neuronal repolarization and thereby regulates neuronal firing and synaptic transmission.
|
| Enzyme Assay |
The activity of AUT1 can be assessed using electrophysiological techniques, specifically patch-clamp electrophysiology. Cells expressing human Kv3.1b or Kv3.2a channels are treated with varying concentrations of AUT1. The whole-cell currents are recorded, and the voltage-dependence of activation and inactivation is analyzed. The EC₅₀ for modulation of channel activity is determined from dose-response curves.
|
| Cell Assay |
To evaluate the cellular effects of AUT1, neurons or cells expressing Kv3 channels are treated with the compound. The effects on action potential firing frequency and amplitude are measured using electrophysiological recordings. The modulation of channel activity and neuronal excitability is assessed. The compound's effects on synaptic transmission can also be evaluated in brain slice preparations.
|
| Animal Protocol |
In vivo studies with AUT1 would typically involve administration to animal models via oral or parenteral routes. The compound's effects on neuronal excitability, seizure susceptibility, or other neurological functions could be assessed. However, detailed in vivo protocols for AUT1 are not extensively documented in the available literature.
|
| ADME/Pharmacokinetics |
AUT1 has a molecular formula of C₁₈H₁₉N₃O₄ and a molecular weight of 341.36 g/mol. Its CAS number is 1311136-84-1. It appears as a white to off-white solid powder with a logP of 2.8. The purity is ≥98%. The powder should be stored at -20°C for 3 years or at 4°C for 2 years; in solvent at -80°C for 6 months or at -20°C for 1 month.
|
| Toxicity/Toxicokinetics |
Specific toxicology data for AUT1 are not extensively detailed in the available literature. As with all research compounds, standard safety precautions should be taken when handling AUT1. It is intended for research use only and is not for human consumption.
|
| References | |
| Additional Infomation |
AUT1 is a positive modulator of Kv3.1 and Kv3.2 potassium channels. It increases whole currents mediated by these channels and shifts the voltage-dependence of activation. AUT1 is used as a research tool to study the role of Kv3 channels in neuronal excitability, rapid repolarization, and synaptic transmission. It is not a clinically approved drug.
|
| Molecular Formula |
C18H19N3O4
|
|---|---|
| Molecular Weight |
341.361164331436
|
| Exact Mass |
341.137
|
| Elemental Analysis |
C, 63.33; H, 5.61; N, 12.31; O, 18.75
|
| CAS # |
1311136-84-1
|
| Related CAS # |
1311136-84-1
|
| PubChem CID |
53230344
|
| Appearance |
White to off-white solid powder
|
| LogP |
2.8
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
25
|
| Complexity |
501
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CC[C@@H]1C(=O)N(C(=O)N1)C2=CN=C(C=C2)OC3=CC(=C(C=C3)C)OC
|
| InChi Key |
AMAOXEGBJHLCSF-CQSZACIVSA-N
|
| InChi Code |
InChI=1S/C18H19N3O4/c1-4-14-17(22)21(18(23)20-14)12-6-8-16(19-10-12)25-13-7-5-11(2)15(9-13)24-3/h5-10,14H,4H2,1-3H3,(H,20,23)/t14-/m1/s1
|
| Chemical Name |
(5R)-5-Ethyl-3-(6-{[4-methyl-3-(methyloxy)phenyl]oxy}-3-pyridinyl)-2,4-imidazolidinedione
|
| Synonyms |
AUT-1 AUT 1 AUT1
|
| 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 : ≥ 250 mg/mL (~732.36 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.09 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9295 mL | 14.6473 mL | 29.2946 mL | |
| 5 mM | 0.5859 mL | 2.9295 mL | 5.8589 mL | |
| 10 mM | 0.2929 mL | 1.4647 mL | 2.9295 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
COA