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YM758

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Catalog No. T13374Cas No. 312752-85-5

YM758 is an inhibitor of If current channel.

YM758

YM758

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Purity: 99.65%
Catalog No. T13374Cas No. 312752-85-5
YM758 is an inhibitor of If current channel.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$46In StockIn Stock
5 mg$137In StockIn Stock
10 mg$223In StockIn Stock
25 mg$369In StockIn Stock
50 mg$521In StockIn Stock
100 mg$702In StockIn Stock
200 mg$947-In Stock
1 mL x 10 mM (in DMSO)$143In 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:99.65%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
YM758 is an inhibitor of If current channel.
In vitro
YM758 inhibits rOct1- (IC50 = 23.8 μM) and hOCT1- (IC50 = 40.5 μM) mediated [3H]MPP uptake in a concentration-dependent manner. YM758 inhibits OATP1B1-mediated [3H]E217βG uptake in a concentration-dependent manner(IC50 = 13.0 μM). YM758 shows no inhibitory effect on OATP1B3-mediated [3H]E217βG uptake[1].
In vivo
In tachycardia-induced dogs, YM758 (0.03, 0.1, and 0.3 mg/kg; i.v.) plasma concentrations rapidly decrease with t1/2s of 1.62, 4.93, and 1.63 h, respectively. The CLtot values are1.71, 1.69, and 1.48 L/h/kg, and Vdss values amount to 3.19, 5.78, and 2.94 L/kg accordingly[2]. The radioactivity in the rat eyeballs after dosing 14C-YM758 is extracted. The radioactivity recovery is 97.1% at 4 h and 67.1% at 24 h. In the eyeball at 4 h after administration, YM758 (the unchanged drug) is the main compound detected (66.7%)[3].
Chemical Properties
Molecular Weight469.55
FormulaC26H32FN3O4
Cas No.312752-85-5
SmilesCOc1cc2CCN(Cc2cc1OC)C(=O)[C@@H]1CCCN(CCNC(=O)c2ccc(F)cc2)C1
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: 90 mg/mL (191.67 mM), Sonication and heating to 60℃ are recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1297 mL10.6485 mL21.2970 mL106.4849 mL
5 mM0.4259 mL2.1297 mL4.2594 mL21.2970 mL
10 mM0.2130 mL1.0648 mL2.1297 mL10.6485 mL
20 mM0.1065 mL0.5324 mL1.0648 mL5.3242 mL
50 mM0.0426 mL0.2130 mL0.4259 mL2.1297 mL
100 mM0.0213 mL0.1065 mL0.2130 mL1.0648 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:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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