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AVE-0118 

Cat. No. M30182
AVE-0118  Structure
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Quality Control & Documentation
Biological Activity

AVE-0118 is a nonselective Kv1.5 blocker with an IC50 of 1.1 μM. AVE-0118 is a multichannel inhibitor with weak, micromolar activity against Kv1.5 and other ion channels. It is inactive against IKs, IKATP, and L-type Ca+ channels.

Chemical Information
Molecular Weight 479.57
Formula C30H29N3O3
CAS Number 498577-53-0
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Attila Kun, et al. Basic Clin Pharmacol Toxicol. Neurogenic contraction induced by the antiarrhythmic compound, AVE 0118, in rat small mesenteric arteries

[2] David Hillman. Sleep. A new pharmacological treatment to treat obstructive sleep apnea?

[3] Mark T Bilodeau, et al. Curr Top Med Chem. Kv1.5 blockers for the treatment of atrial fibrillation: approaches to optimization of potency and selectivity and translation to in vivo pharmacology

[4] Barry London. J Cardiovasc Electrophysiol. Amiodarone and atrial fibrillation

[5] Gerald V Naccarelli, et al. Expert Rev Cardiovasc Ther. New antiarrhythmic treatment of atrial fibrillation

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  Catalog
Abmole Inhibitor Catalog




Keywords: AVE-0118  supplier, Potassium Channel, inhibitors, activators


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