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AUT1

Cat. No. M10516
AUT1 Structure
Synonym:

AUT-1

Size Price Availability Quantity
5mg USD 440  USD440 In stock
10mg USD 730  USD730 In stock
50mg USD 2180  USD2180 In stock
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Quality Control & Documentation
Biological Activity

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. AUT1 has pEC50 values of 5.33 and 5.31 for human recombinant Kv3.1b and Kv3.2a, respectively, exhibits 10-fold lower potency at human recombinant Kv3.3 channel (pEC50, 4.5).

Chemical Information
Molecular Weight 341.36
Formula C18H19N3O4
CAS Number 1311136-84-1
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Timothy Olsen, et al. Neuropharmacology. Kv3 K+ currents contribute to spike-timing in dorsal cochlear nucleus principal cells

[2] Puja K Parekh, et al. Neuropsychopharmacology. Antimanic Efficacy of a Novel Kv3 Potassium Channel Modulator

[3] Maile R Brown, et al. J Neurophysiol. Physiological modulators of Kv3.1 channels adjust firing patterns of auditory brain stem neurons

[4] Marcelo D Rosato-Siri, et al. J Pharmacol Exp Ther. A Novel Modulator of Kv3 Potassium Channels Regulates the Firing of Parvalbumin-Positive Cortical Interneurons

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Keywords: AUT1, AUT-1 supplier, Potassium Channel, inhibitors, activators


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