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Ivabradine hydrochloride

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Catalog No. T2535Cas No. 148849-67-6
Alias 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.

Ivabradine hydrochloride

Ivabradine hydrochloride

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Purity: 99.73%
Catalog No. T2535Alias S 16257-2, Ivabradine HClCas No. 148849-67-6
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.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
10 mg$33In StockIn Stock
25 mg$50In StockIn Stock
50 mg$68In StockIn Stock
100 mg$98In StockIn Stock
200 mg$148In StockIn Stock
500 mg$263-In Stock
1 mL x 10 mM (in DMSO)$39In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.73%
Color:White
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Product Introduction

Bioactivity
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].
SynonymsS 16257-2, Ivabradine HCl
Chemical Properties
Molecular Weight505.05
FormulaC27H37ClN2O5
Cas No.148849-67-6
SmilesN1(C(=O)Cc2c(CC1)cc(c(c2)OC)OC)CCCN(C)C[C@@H]1c2c(cc(c(c2)OC)OC)C1.Cl
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 250 mg/mL (495 mM), Sonication is recommended.
Ethanol: 93 mg/mL (184.14 mM), Sonication is recommended.
H2O: 75 mg/mL (148.5 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.53 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
H2O/Ethanol/DMSO
1mg5mg10mg50mg
1 mM1.9800 mL9.9000 mL19.8000 mL99.0001 mL
5 mM0.3960 mL1.9800 mL3.9600 mL19.8000 mL
10 mM0.1980 mL0.9900 mL1.9800 mL9.9000 mL
20 mM0.0990 mL0.4950 mL0.9900 mL4.9500 mL
50 mM0.0396 mL0.1980 mL0.3960 mL1.9800 mL
100 mM0.0198 mL0.0990 mL0.1980 mL0.9900 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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%
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