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A2793

Cat. No. M20746
A2793 Structure
Synonym:

Ethyl [(5-Chloroquinolin-8-yl)oxy]acetate

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Biological Activity

A2793 (Ethyl [(5-Chloroquinolin-8-yl)oxy]acetate) is an efficient inhibitor of TWIK-related spinal cord potassium channel (TRESK, K2P18, KCNK18) and TASK-1 (KCNK3) with IC50 of 6.8 μM for mouse TRESK.

Chemical Information
Molecular Weight 265.69
Formula C13H12ClNO3
CAS Number 88349-90-0
Solubility (25°C) DMSO 53 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] Mikls Lengyel, et al. Mol Pharmacol. Chemically Modified Derivatives of the Activator Compound Cloxyquin Exert Inhibitory Effect on TRESK (K2P18.1) Background Potassium Channel

[2] Willem-Maarten P F Bosman, et al. Ned Tijdschr Geneeskd. [A woman with a painful ankle]

[3] Maren Oehlmann, et al. J Cell Biol. The role of Cdc6 in ensuring complete genome licensing and S phase checkpoint activation

[4] T A Prokhorova, et al. J Biol Chem. Sequential MCM/P1 subcomplex assembly is required to form a heterohexamer with replication licensing activity

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Keywords: A2793, Ethyl [(5-Chloroquinolin-8-yl)oxy]acetate supplier, Potassium Channel, inhibitors, activators


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