Ranolazine 2HCl(RS-43285 CVT-303) - �뵺�羺�ٷ��ַ

Molecular Weight (MW)	500.46
Formula	C24H33N3O4.2HCl
CAS No.	95635-56-6
Storage	-20�� for 3 years in powder form
-80�� for 2 years in solvent
Solubility(In vitro)	DMSO: 100 mg/mL (199.8 mM)
Water: 100 mg/mL (199.8 mM)
Ethanol: <1 mg/mL
Solubility(In vivo)	Chemical Name: N-(2,6-dimethylphenyl)-2-[4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl]acetamide dihydrochloride InChi Key: RJNSNFZXAZXOFX-UHFFFAOYSA-N InChi Code: InChI=1S/C24H33N3O4.2ClH/c1-18-7-6-8-19(2)24(18)25-23(29)16-27-13-11-26(12-14-27)15-20(28)17-31-22-10-5-4-9-21(22)30-3;;/h4-10,20,28H,11-17H2,1-3H3,(H,25,29);2*1H SMILES Code: O=C(NC1=C(C)C=CC=C1C)CN2CCN(CC(O)COC3=CC=CC=C3OC)CC2.[H]Cl.[H]Cl
Synonyms	RS-43285; RS43285; RS 43285; CVT 303; CVT303; CVT-303; Ranolazine; Ranexa; Latixa; Ranolazine Dihydrochloride; Ranolazine Hydrochloride; Ranolazine HCl; .

Molecular Weight (MW)

500.46

Formula

C24H33N3O4.2HCl

CAS No.

95635-56-6

Storage

-20�� for 3 years in powder form

-80�� for 2 years in solvent

Solubility(In vitro)

DMSO: 100 mg/mL (199.8 mM)

Water: 100 mg/mL (199.8 mM)

Ethanol: <1 mg/mL

Solubility(In vivo)

Chemical Name: N-(2,6-dimethylphenyl)-2-[4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl]acetamide dihydrochloride

InChi Key: RJNSNFZXAZXOFX-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H33N3O4.2ClH/c1-18-7-6-8-19(2)24(18)25-23(29)16-27-13-11-26(12-14-27)15-20(28)17-31-22-10-5-4-9-21(22)30-3;;/h4-10,20,28H,11-17H2,1-3H3,(H,25,29);2*1H

SMILES Code: O=C(NC1=C(C)C=CC=C1C)CN2CCN(CC(O)COC3=CC=CC=C3OC)CC2.[H]Cl.[H]Cl

Synonyms

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

In Vitro	In vitroactivity: 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
Formulation & Dosage
References	Heart. 2006 Jul;92 Suppl 4:iv6-iv14; Circulation. 1996 Jan 1;93(1):135-42.

In Vitro

In vitroactivity: 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

Formulation & Dosage

References

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

CAS NO:	95635-56-6
��:	��98%

��װ	�۸�(Ԫ)
1g	��
2g	��
5g	��