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Ivabradine HCl(Procoralan)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ivabradine HCl(Procoralan)图片
CAS NO:148849-67-6
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
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[C@@H]2C3=CC(OC)=C(OC)C=C3C2)C)CCC4=CC(OC)=C(OC)C=C4C1.[H]Cl

SynonymsS 16257-2; Corlanor; S-16257-2; Coraxan; Ivabid; S16257-2; Ivabradine HCl; Corlentor; Procoralan; Coralan; Bradia.
实验参考方法
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.