| Identification | Back Directory | [Name]
JTV 519 | [CAS]
1038410-88-6 | [Synonyms]
JTV-519 hydrochloride
JTV-519 hydrochloride
(K201
3-(4-benzylpiperidin-1-yl)-1-(7-methoxy-3,5-dihydro-2H-1,4-benzothiazepin-4-yl)propan-1-one:hydrochloride | [Molecular Formula]
C25H33ClN2O2S | [MDL Number]
MFCD00935784 | [MOL File]
1038410-88-6.mol | [Molecular Weight]
461.06 |
| Hazard Information | Back Directory | [Uses]
JTV-519 (K201) is a Ca2+-dependent blocker of sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties[1][2]. | [in vivo]
JTV-519 (0.5mg/kg/h, i.v., 2 h before the surgery) improves cardiac function in CLP mice, where the fractional shortening (FS) and ejection fraction (EF) are significantly increased as compared with CLP mice without JTV-519 treatment[3]. | Animal Model: | Wild type male C57BL/6 mice weighing 18-22g with polymicrobial sepsis produced by cecal ligation and puncture (CLP) [3] | | Dosage: | 0.5 mg/kg/h | | Administration: | Applied intraperitoneally 2 h before the surgery | | Result: | Improved cardiac function, where the EF and FS were significantly increased. |
| [References]
[1] Darcy YL, et al. 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. DOI:10.1124/mol.115.102277
[2] Kaneko N, et al. Inhibition of annexin V-dependent Ca2+ movement in large unilamellar vesicles by K201, a new 1,4-benzothiazepine derivative. Biochim Biophys Acta. 1997 Nov 13;1330(1):1-7. DOI:10.1016/s0005-2736(97)00132-6
[3] Yang J, et al. Toll-like receptor 4-induced ryanodine receptor 2 oxidation and sarcoplasmic reticulum Ca2+ leakage promote cardiac contractile dysfunction in sepsis. J Biol Chem. 2018 Jan 19;293(3):794-807. DOI:10.1074/jbc.M117.812289 |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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