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K201

Catalog No. T24239   CAS 1038410-88-6
Synonyms: K-201, JTV 519, JTV-519, K 201

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.

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K201 Chemical Structure
K201, CAS 1038410-88-6
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
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Purity: 99.8%
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 25 mg/mL (54.22 mM)

TargetMolReferences and Literature

1. Darcy YL, Diaz-Sylvester PL, Copello JA. K201 (JTV519) is a Ca2+-Dependent Blocker of SERCA and a Partial Agonist of Ryanodine Receptors in Striated Muscle. Mol Pharmacol. 2016 Aug;90(2):106-15. 2. Toischer K, et al. K201 improves aspects of the contractile performance of human failing myocardium via reduction in Ca2+ leak from the sarcoplasmic reticulum. Basic Res Cardiol. 2010 Mar;105(2):279-87.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Membrane Protein-targeted Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Bioactive Compound Library Metabolism Compound Library Neuronal Signaling Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max Clinical Compound Library

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Keywords

K201 1038410-88-6 Membrane transporter/Ion channel Metabolism Calcium Channel JTV519 K-201 JTV 519 JTV-519 K 201 inhibitor inhibit

 

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