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Talinolol

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Catalog No. T21640Cas No. 57460-41-0

(±)-Talinolol is a selective β1 adrenoceptor antagonist well known for its cardioprotective and antihypertensive activity.

Talinolol

Talinolol

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Purity: 98.8%
Catalog No. T21640Cas No. 57460-41-0
(±)-Talinolol is a selective β1 adrenoceptor antagonist well known for its cardioprotective and antihypertensive activity.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$30In StockIn Stock
5 mg$44In StockIn Stock
10 mg$84In StockIn Stock
25 mg$189In StockIn Stock
50 mg$328In StockIn Stock
100 mg$579In StockIn Stock
1 mL x 10 mM (in DMSO)$48In 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:98.8%
Appearance:Solid
Color:White
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Product Introduction

Talinolol AI Summary
Talinolol exhibits diverse pharmacokinetic and bioactivity profiles across multiple experimental studies. It demonstrates toxicity in mice with LD50 values ranging from 25.0 to 1048.5 mg/kg through both intravenous and oral administration. In humans, it shows a total body clearance of 4.9 mL/min/kg and a renal clearance of 2.6 mL/min/kg, indicating renal filtration as a major elimination pathway. The hepatic clearance (CL) is recorded at 2.3 mL/min/kg, with a volume of distribution at steady state (Vdss) of 3.3 L/kg. Oral bioavailability (F_fraction) is 0.55, and the fraction absorbed (Fa) is 0.65. Talinolol exhibits notable beta-blocking activity with an activity level of 8.96 and is involved in inhibiting various targets, including the malarial parasite plastid, Glutaminase (GLS), and human tyrosyl-DNA phosphodiesterase 1 (TDP1). It inhibits the β1 and β2 adrenergic receptors with Ki values of 240.0 nM and 900.0 nM, respectively, and shows significant activity against the SARS-CoV-2 virus by inhibiting cytotoxicity in both Caco-2 and VERO-6 cells. Additionally, the compound has a high efflux ratio in human Caco2 cells, indicating active efflux transport mechanisms, and displays moderate permeability from the basolateral to apical side, with an efflux ratio indicating significant interactions with transporters. The compound shows an unbound fraction in human plasma of 0.39 and demonstrates binding affinity to various targets, including β1 adrenergic receptors and soluble epoxide hydrolase. Overall, these bioactivities and pharmacokinetic properties suggest that Talinolol has potential for further pharmacological exploration, especially in the context of its beta-blocking capabilities and antiviral activity..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
(±)-Talinolol is a selective β1 adrenoceptor antagonist well known for its cardioprotective and antihypertensive activity.
Chemical Properties
Molecular Weight363.49
FormulaC20H33N3O3
Cas No.57460-41-0
SmilesCC(C)(C)NCC(O)COC1=CC=C(NC(=O)NC2CCCCC2)C=C1
Relative Density.1.11 g/cm3 (Predicted)
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: 100 mg/mL (275.11 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.7511 mL13.7555 mL27.5111 mL137.5554 mL
5 mM0.5502 mL2.7511 mL5.5022 mL27.5111 mL
10 mM0.2751 mL1.3756 mL2.7511 mL13.7555 mL
20 mM0.1376 mL0.6878 mL1.3756 mL6.8778 mL
50 mM0.0550 mL0.2751 mL0.5502 mL2.7511 mL
100 mM0.0275 mL0.1376 mL0.2751 mL1.3756 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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