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JTV 519 fumarate

Cat. No. 4564 Submit a Review Datasheet / COA / SDS
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Cat.No. 4564 - JTV 519 fumarate | C25H32N2O2.C4H4O4
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)
Datasheet
Citations
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Biological Activity Technical Data Solubility Calculators Datasheets References

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 C25H32N2O2.C4H4O4
Storage Store at +4°C
Purity ≥98% (HPLC)
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.

All Tocris products are intended for laboratory research use only.

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 solvent 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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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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