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Terfenadine [50679-08-8]

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Référence NB-64-04157-1mL

Conditionnement : 1mLx10mM(inDMSO)

Marque : Neo Biotech

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Terfenadine

(Synonyms: MDL-991, (±)-Terfenadine) Copy Product Info

Synonyms: MDL-991, (±)-Terfenadine

Catalog No. T1266 Copy Product Info

Purity: 99.97%

Terfenadine ((±)-Terfenadine) is a prodrug metabolized by intestinal CYP3A4 into fexofenadine, an active selective histamine H1-receptor antagonist that possesses antihistaminic and non-sedative effects.

Cas No. 50679-08-8

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.97%

Appearance:Solid

Color:White

Product Introduction

Terfenadine AI Summary

Terfenadine exhibits diverse bioactivities across various biological assays, revealing a multifaceted pharmacological profile. Notably, it demonstrates potent inhibition of the K+ channel HERG, with IC50 values ranging from 56.0 nM to 213.8 nM, indicating significant cardiotoxic potential. Additionally, it shows strong antagonism of the human histamine H1 receptor with IC50 values of 94.0 nM and a dissociation constant (Kd) between 31.62 nM and 33.0 nM. In the field of immunology, it inhibits IL-4 and IL-5 production in mice splenocytes with IC50 values of 4950.0 nM and 3960.0 nM, respectively. The compound also exhibits moderate inhibition of cytochrome P450 enzymes, including CYP3A4 and CYP2J2, suggesting potential drug-drug interactions. In terms of pharmacokinetics, Terfenadine possesses a lengthy half-life of 23.0 hours in humans, a high plasma protein binding rate of 98.0%, and a volume of distribution of 2.9 L/kg. Additionally, the compound displays lipophilicity with a LogP value of 5.7 and shows inhibitory activity against various transporters, including P-glycoprotein. Furthermore, it demonstrates moderate antimicrobial activity against multiple strains of Plasmodium falciparum and Staphylococcus aureus. Overall, Terfenadine’s extensive bioactivity spectrum across multiple biological targets and its pharmacokinetic characteristics make it an intriguing subject for further research in various therapeutic areas..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Terfenadine ((±)-Terfenadine) is a prodrug metabolized by intestinal CYP3A4 into fexofenadine, an active selective histamine H1-receptor antagonist that possesses antihistaminic and non-sedative effects.
Targets & IC50	ERG (human):204 nM
Synonyms	MDL-991, (±)-Terfenadine

Chemical Properties

Molecular Weight	471.67
Formula	C₃₂H₄₁NO₂
Cas No.	50679-08-8
Smiles	CC(C)(C)c1ccc(cc1)C(O)CCCN1CCC(CC1)C(O)(c1ccccc1)c1ccccc1
Relative Density.	1.0488 g/cm3 (Estimated)

Storage & Solubility Information

Storage

Keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 47.2 mg/mL (100.07 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.24 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

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1201 mL	10.6006 mL	21.2013 mL	106.0063 mL
5 mM	0.4240 mL	2.1201 mL	4.2403 mL	21.2013 mL
10 mM	0.2120 mL	1.0601 mL	2.1201 mL	10.6006 mL
20 mM	0.1060 mL	0.5300 mL	1.0601 mL	5.3003 mL
50 mM	0.0424 mL	0.2120 mL	0.4240 mL	2.1201 mL
100 mM	0.0212 mL	0.1060 mL	0.2120 mL	1.0601 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 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 DMSO 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 DMSO stock solution to 400 µL PEG300 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 ddH₂O 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.

Dose Conversion

Keywords

TerfenadinePotassiumChannelPotassium ChannelNa+ExchangerNa+/Ca2+ ExchangerNa+ ExchangerMDL991MDL 991mAChRKcsAInhibitorinhibitHTHistamineReceptorHistamine ReceptorhERGCaspaseCa2+ExchangerCa2+ ExchangerApoptosis5HTReceptor5HT Receptor

Related Tags: Terfenadine chemical structure | Terfenadine formula | Terfenadine molecular weight