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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Calcium Channel -JTV-519 fumarate
JTV-519 fumarate

Chemical Structure : JTV-519 fumarate

CAS No.: 1883549-36-7

JTV-519 fumarate (K201;JTV519)

货号: PC-63283Not For Human Use, Lab Use Only.

JTV-519 (K201) is a Ca2+-dependent blocker of SERCA and a partial agonist of ryanodine receptors (RyRs).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

JTV-519 (K201) is a Ca2+-dependent blocker of SERCA and a partial agonist of ryanodine receptors (RyRs); displays Ca(2+)-dependent inhibition of SERCA-dependent ATPase activity with IC50 of 9 uM at 0.25 Ca2+ in cardiac muscle; may prevent abnormal Ca(2+) leak from the sarcoplasmic reticulum (SR) in the ischemic heart and skeletal muscle (SkM) by stabilizing the ryanodine receptors (RyRs; RyR1 and RyR2, respectively).

Heart Arrhythmia

Phase 2 Discontinued

物理化学性质&存储条件

分子量 540.675
分子式 C29H36N2O6S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-(2,3-Dihydro-7-methoxy-1,4-benzothiazepin-4(5H)-yl)-3-[4-(phenylmethyl)-1-piperidinyl]-1-propanone fumarate

参考文献

1. Darcy YL, et al. Mol Pharmacol. 2016 Aug;90(2):106-15.

2. Inagaki K, et al. Circulation. 2000 Feb 22;101(7):797-804.

3. Ito K, et al. Br J Pharmacol. 2000 Jun;130(4):767-76.

4. Nakaya H, et al. Br J Pharmacol. 2000 Dec;131(7):1363-72.

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