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Ivabradine hydrochloride

Catalog No. T2535   CAS 148849-67-6
Synonyms: S 16257-2, Ivabradine HCl

Ivabradine hydrochloride (S 16257-2) is a new If inhibitor (IC50: 2.9 μM). Ivabradine Hydrochloride is the hydrochloride salt form of ivabradine, an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker, with negative chronotropic activity. Upon administration, ivabradine selectively binds to the intracellular portion of the HCN channel pore and blocks HCN channels in the pacemaker cells within the sinoatrial (SA) node. This inhibits the If (funny) pacemaker ion current, prevents the inward flow and intracellular accumulation of positively charged ions, reduces pacemaker activity and slows diastolic depolarization.

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Ivabradine hydrochloride Chemical Structure
Ivabradine hydrochloride, CAS 148849-67-6
Pack Size Availability Price/USD Quantity
10 mg In stock $ 33.00
25 mg In stock $ 50.00
50 mg In stock $ 68.00
100 mg In stock $ 98.00
200 mg In stock $ 148.00
500 mg In stock $ 263.00
1 mL * 10 mM (in DMSO) In stock $ 39.00
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Purity: 99.73%
Purity: 99%
Purity: 98.6%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Ivabradine hydrochloride (S 16257-2) is a new If inhibitor (IC50: 2.9 μM). Ivabradine Hydrochloride is the hydrochloride salt form of ivabradine, an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker, with negative chronotropic activity. Upon administration, ivabradine selectively binds to the intracellular portion of the HCN channel pore and blocks HCN channels in the pacemaker cells within the sinoatrial (SA) node. This inhibits the If (funny) pacemaker ion current, prevents the inward flow and intracellular accumulation of positively charged ions, reduces pacemaker activity and slows diastolic depolarization.
Targets&IC50 If:2.9 μM
In vivo Ivabradine 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[1]. Ivabradine causes 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 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[2].
Synonyms S 16257-2, Ivabradine HCl
Molecular Weight 505.05
Formula C27H37ClN2O5
CAS No. 148849-67-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 93 mg/mL (184.1 mM)

Ethanol: 93 mg/mL (184.1 mM)

H2O: 75 mg/mL (148.5 mM)

TargetMolReferences and Literature

1. Thollon C, et al. Br J Pharmacol, 1994,112(1):37-42.

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library Anti-Cancer Drug Library GPCR Compound Library Anti-Neurodegenerative Disease Compound Library EMA Approved Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Inhibitor Library FDA-Approved Drug Library Target-Focused Phenotypic Screening Library

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Keywords

Ivabradine hydrochloride 148849-67-6 GPCR/G Protein Neuroscience Adrenergic Receptor heart rate orally active anticonvulsant Inhibitor Ivabradine Ivabradine Hydrochloride anti-ischaemic anti-anginal inhibit Hyperpolarization activated cyclic nucleotide gated channels S 16257-2 HCN Channel Ivabradine HCl inhibitor

 

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