Terfenadine

Catalog No.S4353 Batch:S435302

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Technical Data

Formula

C32H41NO2
Molecular Weight 471.67 CAS No. 50679-08-8
Solubility (25°C)* In vitro DMSO 31 mg/mL (65.72 mM)
Ethanol 11 mg/mL (23.32 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.35mg/ml Taking the 1 mL working solution as an example, add 50 μL of 7 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.55mg/ml Taking the 1 mL working solution as an example, add 50 μL of 31 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
Targets
Caspase-4 [6] Caspase-2 [6] Caspase-9 [6] Ca2+ homeostasis [6] H1 histamine receptor [6] View More
In vitro

Terfenadine is equipotent to quinidine as a blocker of the delayed rectifier potassium current in isolated feline myocytes. [1] Terfenadine inhibits the human ether-a-go-go related gene (HERG) encoded channels expressed in Xenopus oocytes at nanomolar concentrations in a use- and voltage-dependent fashion. [2] Terfenadine (2 μM) blocks the steady-state maximum current at 0 mV by 65% in Xenopus oocytes. Terfenadine block is dose dependent and equally potent on the maximal steady-state and tail currents, its Kd values are 350 nM and 390 nM, respectively. Terfenadine blocks Kv1.5 (a member of the Kv1 subfamily of voltage-dependent K+ channels) in human atrial myocytes and in the human embryonic kidney cell expression system. Terfenadine (10 μM) produces a dose-dependent block with a 60% reduction of steady-state current in Xenopus oocytes. [3] Terfenadine is oxidated into oxidative N-dealkylation to 4-(hydroxydiphenylmethyl)-piperidine and oxidation of a tert-butyl methyl group to a primary alcohol, which is subsequently oxidized to a carboxylic acid, which is markedly inhibited by gestodene, a selective mechanism-based inactivator of P-450 3A enzymes but not by any of several other P-450 inhibitors. [4] Terfenadine significantly increases action potential duration of guinea pig myocytes. Terfenadine potently blocks the rapidly activating component of the delayed rectifier, IKr, with IC50 values of 1.5 nM and 50 nM, respectively. Terfenadine (10 μM) blocks the slowly activating component of the delayed rectifier, IKs (58.4%), and the inward rectifier, IK1 (20.5%). [5]
In vivo

Terfenadine (1.0 to 3.0 mg/kg, i.v.) significantly prolongs the QTc interval and ventricular effective refractory period in chloralose-anesthetized dogs. [5]

Protocol (from reference)

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.