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    Ivabradine HCl (Procoralan)
    Ivabradine HCl (Procoralan)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1142
    CAS #: 148849-67-6 Purity ≥98%

    Description: Ivabradine HCl (Corlentor; Coraxan; Ivabid; Procoralan; Coralan; S16257; S 16257; S-16257; Bradia), the hydrochloride salt of Ivabradine, is a novel and potent cardiac pacemaker current (If) inhibitor with antianginal effects. It inhibits IF with IC50 of 2.9 μM. Ivabradine acts specifically on the pacemaker activity of the sinoatrial node, and is a pure heart rate lowering agent. Ivabradine is a new drug used for the symptomatic management of stable angina pectoris. Ivabradine acts by reducing the heart rate via specific inhibition of the funny channel, a mechanism different from that of beta blockers and calcium channel blockers, two commonly prescribed antianginal drugs. 

    Related CAS #: 155974-00-8 (free base)   1202000-62-1 (sulfate)   148849-67-6 (HCl)   1086026-42-7 (oxalate)    

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    Molecular Weight (MW)505.05 
    FormulaC27H36N2O5.HCl 
    CAS No.148849-67-6 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 101 mg/mL (200 mM)
    Water: 82 mg/mL (162.4 mM)
    Ethanol: 101 mg/mL (200 mM)
    Other info

    Chemical Name: (S)-3-(3-(((3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl)methyl)(methyl)amino)propyl)-7,8-dimethoxy-1,3,4,5-tetrahydro-2H-benzo[d]azepin-2-one hydrochloride

    InChi Key: HLUKNZUABFFNQS-ZMBIFBSDSA-N

    InChi Code: InChI=1S/C27H36N2O5.ClH/c1-28(17-21-11-20-14-25(33-4)26(34-5)16-22(20)21)8-6-9-29-10-7-18-12-23(31-2)24(32-3)13-19(18)15-27(29)30;/h12-14,16,21H,6-11,15,17H2,1-5H3;1H/t21-;/m1./s1

    SMILES Code: O=C1N(CCCN(C[[email protected]@H]2C3=CC(OC)=C(OC)C=C3C2)C)CCC4=CC(OC)=C(OC)C=C4C1.[H]Cl

    SynonymsS 16257-2; S-16257-2; S16257-2; Ivabradine HCl; Corlentor; Coraxan; Ivabid; Procoralan; Coralan; S16257; S 16257; S-16257; S 16257-2; Bradia.


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    In Vitro

    In vitro activity: Ivabradine HCl (also known as S 16257-2), a novel If inhibitor with IC 50 of 2.9 μM which acts specifically on the pacemaker activity of the sinoatrial node, is a pure heart rate lowering agent. Ivabradine is a new drug used for the symptomatic management of stable angina pectoris. Ivabradine acts by reducing the heart rate via specific inhibition of the funny channel, a mechanism different from that of beta blockers and calcium channel blockers, two commonly prescribed antianginal drugs.

    In VivoIvabradine hydrochloride treatment (10 mg/kg/d) induces long-term HRR, and that improves diastolic LV function probably involving attenuated hypoxia, reduced remodeling, and/or preserved nitric oxide bioavailability, resulting from processes triggered early after HRR initiation: angiogenesis and/or preservation of endothelial nitric oxide synthase expression. Ivabradine hydrochloride leads to a sustained 15-20% heart rate reduction, but has no effect on blood pressure. While ivabradine has no effect on endothelial function and vascular reactive oxygen species production in angiotensin II-treated rats, it improves both parameters in ApoE knockout mice. Ivabradine hydrochloride treatment leads to an attenuation of angiotensin II signaling and increased the expression of telomere-stabilizing proteins in ApoE knockout mice, which may explain its beneficial effects on the vasculature. The absence of these protective ivabradine effects in angiotensin II-infused rats may relate to the treatment duration or the presence of arterial hypertension.
    Animal modelRats
    Formulation & DosageN/A
    References

    [1]. Fang, Y., et al. Heart rate reduction induced by the if current inhibitor ivabradine improves diastolic function and attenuates cardiac tissue hypoxia. J Cardiovasc Pharmacol, 2012. 59(3): p. 260-7.

    [2]. Kroller-Schon, S., et al. Differential effects of heart rate reduction with ivabradine in two models of endothelial dysfunction and oxidative stress. Basic Res Cardiol, 2011. 106(6): p. 1147-58.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Ivabradine HClIvabradine administration attenuates post‐MI LV remodeling. J Am Heart Assoc. 2016 Apr; 5(4): e002989.
     
    Ivabradine HCl
    Ivabradine administration reduces the extent of wall thinning after MI. J Am Heart Assoc. 2016 Apr; 5(4): e002989.
     
    Ivabradine HCl
    Ivabradine administration reduces post‐MI LV dyssynchrony. J Am Heart Assoc. 2016 Apr; 5(4): e002989.


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