| Name | JTV-519 |
| Description | JTV-519 is a Ca2+-dependent blocker and prevents abnormal Ca(2+) leak from the sarcoplasmic reticulum in the ischemic heart and skeletal muscle (SkM) by stabilizing the ryanodine receptors. |
| In vitro | In isolated cardiac and SkM SR microsomes, K201 slowed the rate of SR Ca(2+) loading, suggesting potential SERCA block and/or RyR agonism. K201 displayed Ca(2+)-dependent inhibition of SERCA-dependent ATPase activity, which was measured in microsomes incubated with 200, 2, and 0.25 µM Ca(2+) and with the half-maximal K201 inhibitory doses (IC50) estimated at 130, 19, and 9 µM (cardiac muscle) and 104, 13, and 5 µM (SkM SR). K201 (≥5 µM) increased RyR1-mediated Ca(2+) release from SkM microsomes. Maximal K201 doses at 80 µM produced ∼37% of the increase in SkM SR Ca(2+) release observed with the RyR agonist caffeine. K201 (≥5 µM) increased the open probability (Po) of very active ('high-activity') RyR1 of SkM reconstituted into bilayers, but it had no effect on 'low-activity' channels. Likewise, K201 activated cardiac RyR2 under systolic Ca(2+) conditions (∼5 µM; channels at Po ∼0.3) but not under diastolic Ca(2+) conditions (∼100 nM; Po < 0.01)[1]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 25 mg/mL (54.22 mM), Sonication is recommended.
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| Keywords | K201 | JTV519 | CalciumChannel | Calcium Channel | Ca(2+) receptor |
| Inhibitors Related | Quadrol | Tricaine methanesulfonate | Nisoldipine | 2,4,6-Tri-tert-butylphenol | Chlorocresol | L-Ascorbic acid | L-Phenylalanine | L-Ascorbic acid sodium salt | 1-Octanol | 2-Nitrobenzoic acid | Magnesium Chloride Hexahydrate | Magnesium sulfate |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Neuroprotective Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library |
United States
