1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. Vernakalant Hydrochloride

Vernakalant Hydrochloride (Synonyms: RSD1235 hydrochloride)

Cat. No.: HY-14183 Purity: 99.33%
Handling Instructions

Vernakalant hydrochloride is a mixed voltage- and frequency-dependent Na+ and atria-preferred K+ channel blocker. IC50 for block by Vernakalant of wild-type and mutant Kv1.5 channels Fractional block is 13.35±0.93 μM, 0.61±0.03 μM, and 1.63±0.09 μM for Kv1.5 channelwt, Kv1.5 channelI508F, Kv1.5 channelT479A, respectively.

For research use only. We do not sell to patients.

Vernakalant Hydrochloride Chemical Structure

Vernakalant Hydrochloride Chemical Structure

CAS No. : 748810-28-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 234 In-stock
Estimated Time of Arrival: December 31
2 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 276 In-stock
Estimated Time of Arrival: December 31
10 mg USD 436 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1122 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

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Description

Vernakalant hydrochloride is a mixed voltage- and frequency-dependent Na+ and atria-preferred K+ channel blocker. IC50 for block by Vernakalant of wild-type and mutant Kv1.5 channels Fractional block is 13.35±0.93 μM, 0.61±0.03 μM, and 1.63±0.09 μM for Kv1.5 channelwt, Kv1.5 channelI508F, Kv1.5 channelT479A, respectively.

IC50 & Target

IC50: 13.35±0.93 μM (Kv1.5 channelwt), 0.61±0.03 μM (I508F), 1.63±0.09 μM (Kv1.5 channel T479A)[1]

In Vitro

Block of Kv1.5 by Vernakalant Hydrochloride is mediated after channel activation, because Vernakalant causes a relatively rapid onset of block of channel current upon depolarization but little evidence of resting or “tonic” block of the channel. In the presence of 10 μM Vernakalant, rapid block is apparent after channel opening, and a steady-state current level is rapidly reached. The most important effect is the reduction in potency for Vernakalant centered at I502A, which had an IC50 of 329±19 μM (n=4-10), compared with a control IC50 of 13.4±0.9 μM (n=5-23), which is a 25-fold decrease in potency. V505A, I508A, T480A, and C500A showed lesser reductions in potency on Kv1.5, of between 3- and 4-fold. I508Y in our experiments increased the IC50 for Vernakalant on Kv1.5 to 24.7 μM, again similar to the reported value for hERG[1].

Clinical Trial
Molecular Weight

385.93

Formula

C₂₀H₃₂ClNO₄

CAS No.

748810-28-8

SMILES

COC1=C(OC)C=C(CCO[[email protected]]2[[email protected]](N3CC[[email protected]@H](O)C3)CCCC2)C=C1.Cl

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (129.56 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5911 mL 12.9557 mL 25.9114 mL
5 mM 0.5182 mL 2.5911 mL 5.1823 mL
10 mM 0.2591 mL 1.2956 mL 2.5911 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.48 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.48 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.48 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.33%

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Vernakalant Hydrochloride
Cat. No.:
HY-14183
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