Vernakalant-Hydrochloride-RSD1235-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEVernakalant HydrochlorideCat. No.: HY-14183CAS No.: 748810-28-8Synonyms: RSD1235 hydrochloride分式: CHClNO分量: 385.93作靶點: Potassium Channel作通路: Membrane Transporter/Ion Channel儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 mon

2、ths-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 50 mg/mL (129.56 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.5911 mL 12.9557 mL 25.9114 mL5 mM 0.5182 mL 2.5911 mL 5.1823 mL10 mM 0.2591 mL 1.2956 mL 2.5911 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍福渲魄罢埾扰渲瞥吻宓?/p>

3、儲備液，再依次添加助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.48 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.48 mM); Clear solution3. 請依序添加每種

4、溶劑： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (6.48 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Vernakalant hydrochloride種混合電壓和頻率依賴性的 Na+ 和 K+ 通道阻斷劑。Vernakalant 抑制 Kv1.5channelwt，Kv1.5 channelI508F，Kv1.5 channelT479A，IC50 分別為 13.350.93 M。IC50 & Target

5、IC50: 13.350.93 M (Kv1.5 channelwt), 0.610.03 M (I508F), 1.630.09 M (Kv1.5 channel T479A) 1體外研究 Block of Kv1.5 by Vernakalant Hydrochloride is mediated after channel activation, because Vernakalantcauses a relatively rapid onset of block of channel current upon depolarization but little evidence of

6、resting or“tonic” block of the channel. In the presence of 10 M Vernakalant, rapid block is apparent after channelopening, and a steady-state current level is rapidly reached. The most important effect is the reduction inpotency for Vernakalant centered at I502A, which had an IC50 of 32919 M (n=4-10

7、), compared with acontrol IC50 of 13.40.9 M (n=5-23), which is a 25-fold decrease in potency. V505A, I508A, T480A, andC500A showed lesser reductions in potency on Kv1.5, of between 3- and 4-fold. I508Y in our experimentsincreased the IC50 for Vernakalant on Kv1.5 to 24.7 M, again similar to the repo

8、rted value for hERG 1.戶使本產(chǎn)品發(fā)表的科研獻 Clin Pharmacol Ther. 2019 May;105(5):1175-1186. J Pharmacol Sci. 2016 Mar;130(3):170-6.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Eldstrom J, et al. The molecular basis of high-affinity binding of the antiarrhythmic compound Vernakalant (R

9、SD1235) to Kv1.5 channels.Mol Pharmacol. 2007 Dec;72(6):1522-34.2. Chiba T, et al. Influences of rapid pacing-induced electrical remodeling on pharmacological manipulation of the atrial refractoriness inrabbits. J Pharmacol Sci. 2016 Mar;130(3):170-6.McePdfHeightCaution: Product has not been fully validated for medical