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Submit ReviewJTV 519 fumarate
Description: Ryanodine receptor (RyR) inhibitor
Alternative Names: K 201
Chemical Name: 1-(2,3-Dihydro-7-methoxy-1,4-benzothiazepin-4(5H)-yl)-3-[4-(phenylmethyl)-1-piperidinyl]-1-propanone fumarate
Purity: ≥98% (HPLC)
Biological Activity
Ryanodine receptor (RyR) inhibitor; stabilizes RyR2 in a closed conformation. Exhibits antiarrhythmic and cardioprotective properties in vivo.
Technical Data
| M. Wt | 540.67 |
| Formula | C25H32N2O2S.C4H4O4 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1883549-36-7 |
| PubChem ID | 91826075 |
| InChI Key | ISLOBKLDZGDFTB-WLHGVMLRSA-N |
| Smiles | O=C(CCN3CCC(CC4=CC=CC=C4)CC3)N2CCSC1=CC=C(OC)C=C1C2.O=C(/C=C/C(O)=O)O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 54.07 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 540.67. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.85 mL | 9.25 mL | 18.5 mL |
| 5 mM | 0.37 mL | 1.85 mL | 3.7 mL |
| 10 mM | 0.18 mL | 0.92 mL | 1.85 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.37 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Hunt et al (2007) K201 (JTV519) suppresses spontaneous Ca2+ release and [3H]ryanodine binding to RyR2 irrespective of FKBP12.6 association. Biochem.J. 404 431 PMID: 17313373
Chen et al (2008) Effect of K201, a novel antiarrhythmic drug on calcium handling and arrhythmogenic activity of pulmonary vein cardiomyocytes. Br.J.Pharmacol. 153 915 PMID: 17994112
Ye et al (2012) Designing calcium release channel inhibitors with enhanced electron donor properties: stabilizing the closed state of ryanodine receptor type 1. Mol.Pharmacol. 81 53 PMID: 21989257
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