Powder: -20°C for 3 years | In solvent: -80°C for 1 year
K201 (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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 55.00 | |
5 mg | In stock | $ 112.00 | |
10 mg | In stock | $ 157.00 | |
25 mg | In stock | $ 260.00 | |
50 mg | In stock | $ 385.00 | |
100 mg | In stock | $ 573.00 | |
500 mg | In stock | $ 1,250.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 136.00 |
Description | K201 (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]. |
Synonyms | K-201, JTV 519, JTV-519, K 201 |
Molecular Weight | 461.06 |
Formula | C25H33ClN2O2S |
CAS No. | 1038410-88-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 25 mg/mL (54.22 mM)
You can also refer to dose conversion for different animals. More
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K201 1038410-88-6 Membrane transporter/Ion channel Metabolism Calcium Channel JTV519 K-201 JTV 519 JTV-519 K 201 inhibitor inhibit