Ranolazine(CVT303,RS43285-003 Ranexa)

Molecular Weight (MW)	427.54
Formula	C24H33N3O4
CAS No.	95635-55-5
Storage	-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 86 mg/mL (201.2 mM)
Water: <1 mg/mL
Ethanol: 20 mg/mL (46.8 mM)
SMILES	O=C(NC1=C(C)C=CC=C1C)CN2CCN(CC(O)COC3=CC=CC=C3OC)CC2
Synonyms	Ranolazine Dihydrochloride; CVT 303, RS 43285-003; Ranolazine; S 43285; RS-43285; RS43285; CVT-303; CVT303; Ranexa; Latixa; Ranolazine HCl; Ranolazine Hydrochloride.

Molecular Weight (MW)

427.54

Formula

C24H33N3O4

CAS No.

95635-55-5

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility (In vitro)

DMSO: 86 mg/mL (201.2 mM)

Water: <1 mg/mL

Ethanol: 20 mg/mL (46.8 mM)

SMILES

O=C(NC1=C(C)C=CC=C1C)CN2CCN(CC(O)COC3=CC=CC=C3OC)CC2

Synonyms

Ranolazine Dihydrochloride; CVT 303, RS 43285-003; Ranolazine; S 43285; RS-43285; RS43285; CVT-303; CVT303; Ranexa; Latixa; Ranolazine HCl; Ranolazine Hydrochloride.

In Vitro	In vitro activity: Ranolazine selectively inhibits late I(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 significantly and reversibly shortens the action potential duration (APD) of myocytes stimulated at either 0.5 Hz or 0.25 Hz in a concentration-dependent manner in left ventricular myocytes of dogs. Ranolazine at 5 and 10 mM reversibly shortens the duration of twitch contractions (TC) and abolished the after contraction. Ranolazine is found to bind more tightly to the inactivated state than the resting state of the sodium channel underlying I(NaL).
In Vivo	Ranolazine (10 mM) significantly increases glucose oxidation 1.5-fold to 3-fold under conditions in which the contribution of glucoseto overall ATP production is low (low Ca, high FA, with insulin), high (high Ca, low Fa, with pacing), or intermediate in working hearts. Ranolazine similarly increases glucose oxidation in normoxic Langendorff hearts (high Ca, low FA; 15 mL/min). Ranolazine also significantly increases it during flow reduction to 7 mL/min, 3 mL/min, and 0.5 mL/min. Ranolazine significantly improves functional outcome, which is associated with significant increases in glucoseoxidation, a reversal of the increased FA oxidation seen in control reperfusions (versus preischemic), and a smaller but significant increase in glycolysis in reperfuse dischemic working hearts.
Animal model	Rats: Ranolazine (Bolus injection 10 mg/kg and infusion 9.6 mg/kg/h; bolus injection; for 145 minutes; male Wistar rats) treatment significantly reduces infarct size and cardiac troponin T release in rats subjected to left anterior descending coronary artery occlusion-reperfusion
Formulation & Dosage	Bolus injection 10 mg/kg and infusion 9.6 mg/kg/h; bolus injection
References	Heart. 2006 Jul;92 Suppl 4:iv6-iv14; Circulation. 1996 Jan 1;93(1):135-42.

In Vitro

In vitro activity: Ranolazine selectively inhibits late I(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 significantly and reversibly shortens the action potential duration (APD) of myocytes stimulated at either 0.5 Hz or 0.25 Hz in a concentration-dependent manner in left ventricular myocytes of dogs. Ranolazine at 5 and 10 mM reversibly shortens the duration of twitch contractions (TC) and abolished the after contraction. Ranolazine is found to bind more tightly to the inactivated state than the resting state of the sodium channel underlying I(NaL).

In Vivo

Ranolazine (10 mM) significantly increases glucose oxidation 1.5-fold to 3-fold under conditions in which the contribution of glucoseto overall ATP production is low (low Ca, high FA, with insulin), high (high Ca, low Fa, with pacing), or intermediate in working hearts. Ranolazine similarly increases glucose oxidation in normoxic Langendorff hearts (high Ca, low FA; 15 mL/min). Ranolazine also significantly increases it during flow reduction to 7 mL/min, 3 mL/min, and 0.5 mL/min. Ranolazine significantly improves functional outcome, which is associated with significant increases in glucoseoxidation, a reversal of the increased FA oxidation seen in control reperfusions (versus preischemic), and a smaller but significant increase in glycolysis in reperfuse dischemic working hearts.

Animal model

Rats: Ranolazine (Bolus injection 10 mg/kg and infusion 9.6 mg/kg/h; bolus injection; for 145 minutes; male Wistar rats) treatment significantly reduces infarct size and cardiac troponin T release in rats subjected to left anterior descending coronary artery occlusion-reperfusion

Formulation & Dosage

Bolus injection 10 mg/kg and infusion 9.6 mg/kg/h; bolus injection

References

Heart. 2006 Jul;92 Suppl 4:iv6-iv14; Circulation. 1996 Jan 1;93(1):135-42.

CAS NO:	95635-55-5
规格:	≥98%

包装	价格(元)
500mg	电议
1g	电议
2g	电议