1. Membrane Transporter/Ion Channel
  2. Na+/Ca2+ Exchanger
  3. SAR296968

SAR296968 is a Na+/Ca2+ exchanger (NCX) subtype inhibitor with an IC50 value of 74 nM against hNCX1. SAR296968 inhibits both forward and reverse modes of NCX current. SAR296968 enhances cardiac contractility and stroke volume. SAR296968 exerts antiarrhythmic effects. SAR296968 is applicable to research related to heart failure.

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SAR296968

SAR296968 Chemical Structure

CAS No. : 1426899-28-6

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Description

SAR296968 is a Na+/Ca2+ exchanger (NCX) subtype inhibitor with an IC50 value of 74 nM against hNCX1. SAR296968 inhibits both forward and reverse modes of NCX current. SAR296968 enhances cardiac contractility and stroke volume. SAR296968 exerts antiarrhythmic effects. SAR296968 is applicable to research related to heart failure[1].

In Vitro

SAR296968 potently inhibits hNCX1 in CHO cell lines, with an IC50 value of 74 nM[1].
SAR296968 potently inhibits both forward and reverse modes of endogenous NCX currents in guinea pig cardiomyocytes, with corresponding IC50 values of 34.9 nM and 38.9 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

SAR296968 (1.5 mg/kg; i.v.; over 20 minutes) (administered as SAR340835, its prodrug) increases left ventricular contractility by 49% and reduces electrically induced atrial arrhythmias by 74% in anesthetized pigs[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: unspecified strain (pentobarbital-anesthetized)[1]
Dosage: 1.5 mg/kg
Administration: i.v.; over 20 minutes
Result: Increased left ventricular contractility by 49% (dP/dtmax rose from 1423 ± 144 mm Hg/s at baseline to 2115 ± 189 mm Hg/s post-infusion).
Reduced the incidence of atrial arrhythmias by 74% (6.56 ± 1.99 events post-treatment vs.
25.50 ± 1.75 events at baseline, n=8, P<0.001).
Showed no changes in left or right atrial effective refractory period regardless of basic cycle length.
Molecular Weight

410.49

Formula

C22H22N2O4S

CAS No.
SMILES

CC(C=CC=C1)=C1[C@H]2OC3=CC=C(C=C3CC2)OC4=NC=C(C(NCCO)=O)S4

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SAR296968
Cat. No.:
HY-182252
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