中文名:雷諾嗪二鹽酸鹽
英文名:Ranolazine 2HCl
英文別名:RS-43285;N-(2,6-dimethylphenyl)-2-(4-(2-hydroxy-3-(2-methoxyphenoxy)propyl)piperazin-1-yl)acetamide dihydrochloride
純度:10mM in DMSO
貨號:R408393
包裝:1ml
Cas號:95635-56-6
存儲溫度:-80℃儲存
產品介紹:
Information
Ranolazine 2HCl Ranolazine 2HCl (RS-43285) is a calcium uptake inhibitor via the sodium/calcium channal , used to treat chronic angina.
In?vitro
Ranolazine\xa0selectively inhibits\xa0late\xa0I(Na), reduces [Na(+)](i)-dependent calcium overload and attenuates the abnormalities of ventricular repolarisation and contractility that are associated with ischaemia/reperfusion and heart failure in myocardial cells. Ranolazine\xa0significantly and reversibly shortens the action potential duration (APD) of\xa0myocytes\xa0stimulated at either 0.5 Hz or 0.25 Hz in a concentration-dependent manner in left ventricular myocytes of dogs.\xa0Ranolazine\xa0at 5 and 10 mM reversibly shortens the duration of twitch\xa0contractions\xa0(TC) and abolished the after\xa0contraction. Ranolazine\xa0is found to bind more tightly to the inactivated state than the resting state of the\xa0sodium\xa0channel underlying I(NaL).
In?vivo
Ranolazine\xa0(10 mM) significantly increases\xa0glucose\xa0oxidation\xa01.5-fold to 3-fold under conditions in which the contribution of\xa0glucoseto overall ATP production is low (low Ca, high FA, with insulin), high (high Ca, low Fa, with pacing), or intermediate in working\xa0hearts. Ranolazine\xa0similarly increases glucose\xa0oxidation in\xa0normoxic\xa0Langendorff\xa0hearts\xa0(high Ca, low FA; 15 mL/min). Ranolazine\xa0also significantly increases it during flow reduction to 7 mL/min, 3 mL/min, and 0.5 mL/min. Ranolazine\xa0significantly improves functional outcome, which is associated with significant increases in\xa0glucoseoxidation, a reversal of the increased FA\xa0oxidation\xa0seen in control reperfusions (versus preischemic), and a smaller but significant increase in glycolysis in\xa0reperfuse dischemic\xa0working\xa0hearts.
Cell?Data
cell?lines:
Concentrations:
Incubation?Time:
Powder?Purity:≥99%
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關鍵字: RS-43285;N-(2,6-dimethylphenyl)-2-(4-(2-hydroxy-3-(2-methoxyphenoxy)propyl)piperazin-1-yl)acetamide dihydrochloride
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