Vernakalant Hydrochloride

SKU: orb1706483

Description

Vernakalant Hydrochloride is an antiarrhythmic agent that selectively blocks atrial sodium and potassium channels in a use-dependent manner. It is utilized in cardiovascular research to study atrial fibrillation mechanisms and has been investigated in both in vitro electrophysiology assays and in vivo animal models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 748810-28-8
• MW: 385.93
• Purity: 99.89% (May vary between batches)
• Formula: C₂₀H₃₂ClNO₄
• SMILES: Cl.COc1ccc(CCO[C@@H]2CCCC[C@H]2N2CC[C@@H](O)C2)cc1OC
• Target: Potassium Channel,Sodium Channel
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.18 mM);DMSO:45 mg/mL (116.6 mM);H2O:45 mg/mL (116.6 mM)

Bioactivity

• Target IC50:
  I508F:0.61±0.03 μM|Kv1.5 channel (T479A):1.63±0.09 μM|Kv1.5 channel (WT):13.35±0.93 μM
• In Vitro:
  Block of Kv1.5 by Vernakalant Hydrochloride occurs after channel activation, as Vernakalant induces a rapid block of channel current upon depolarization with minimal resting or “tonic” block. The most significant effect is the reduction in potency at I502A, with an IC50 of 329±19 μM (n=4-10) compared to a control IC50 of 13.4±0.9 μM (n=5-23), reflecting a 25-fold potency decrease. Lesser reductions in potency, between 3- and 4-fold, were noted for V505A, I508A, T480A, and C500A. For wild-type and mutant Kv1.5 channels, IC50 for Vernakalant block are 13.35±0.93 μM, 0.61±0.03 μM, and 1.63±0.09 μM for Kv1.5 channels, Kv1.5 channelI508F, and Kv1.5 channelT479A, respectively .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

I508F, KV1.5 channel, Kv1.5 channel T479A, Kv1.5 channelwt, Vernakalant Hydrochloride, PotassiumChannel, Potassium Channel, Sodium Channel, RSD 1235 Hydrochloride, RSD1235 Hydrochloride, RSD1235 hydrochloride, RSD-1235 Hydrochloride, SodiumChannel

Compound Identifiers

PubChem CID

9930048