AUT1 is a Kv3 potassium channel modulator which increases whole currents mediated by human Kv3.1b and Kv3.2a channels, with a concomitant leftward shift in the voltage-dependence of activation, while having a less potent effect on hKv3.3 currents.
Physicochemical Properties
| 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) |
Biological Activity
| 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]. |
| References |
[1]. A Novel Modulator of Kv3 Potassium Channels Regulates the Firing of Parvalbumin-Positive Cortical Interneurons. J Pharmacol Exp Ther. 2015 Sep;354(3):251-60. |
Solubility Data
| 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. 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. 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 | 2.9295 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 |