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

Vernakalant Hydrochloride (Synonyms: RSD1235 hydrochloride)

製品番号: HY-14183 純度: 99.33%
取扱説明書

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.

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Vernakalant Hydrochloride 構造式

Vernakalant Hydrochloride 構造式

CAS 番号 : 748810-28-8

容量 価格(税別) 在庫状況 数量
10 mM * 1  mL in DMSO USD 234 在庫あり
Estimated Time of Arrival: December 31
2 mg USD 180 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 276 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 436 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 1122 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 1800 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 2 publication(s) in Google Scholar

Other Forms of Vernakalant Hydrochloride:

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製品説明

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]

体外実験

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].

臨床実験
分子量

385.93

分子式

C₂₀H₃₂ClNO₄

CAS 番号

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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.
体内:
  • 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.
参考文献

純度: 99.33%

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Keywords:

VernakalantRSD1235RSD 1235RSD-1235Potassium ChannelKcsAInhibitorinhibitorinhibit

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製品名:
Vernakalant Hydrochloride
製品番号:
HY-14183
数量:
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