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Diphenhydramine

Name: Diphenhydramine
Brand: TargetMol
SKU: T21419
Price: 34 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T21419Cas No. 58-73-1

Alias Syntedril, PM-255, PM255, PM 255, Debendrin, Dabylen

Diphenhydramine (Syntedril), a first-generation antihistamine possessing antiemetic, antitussive, anticholinergic, and sedative properties, is mainly used in the treatment of allergies. Diphenhydramine is also used in the management of drug-induced parkinsonism and other extrapyramidal symptoms.

Diphenhydramine

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Purity: 98.07%

Catalog No. T21419Alias Syntedril, PM-255, PM255, PM 255, Debendrin, DabylenCas No. 58-73-1

Pack Size	Price	USA Warehouse	Global Warehouse
200 mg	$34	In Stock	In Stock
500 mg	$55	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$39	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Batch Information

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Purity:98.07%

Appearance:Liquid

Color:Transparent

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COA HNMR GC LCMS

Product Introduction

Diphenhydramine AI Summary

Diphenhydramine exhibits a broad spectrum of pharmacological and bioactivity properties. It has a distribution volume of 4.5 L.kg-1 and demonstrates high plasma protein binding with a low unbound fraction (Fu = 0.22). The compound is highly ionized at a physiological pH of 7.4, with a pKa of 9.1. It shows notable lipophilicity with an eLog D value of 1.38. Pharmacokinetically, Diphenhydramine has a half-life of 31.05 hours in humans, with an apparent volume of distribution of 3.3 L.kg-1 and a high oral bioavailability of 79.0%. It exhibits a high unbound drug partitioning coefficient in the brain (Kp = 3.02), indicating substantial central nervous system penetration. Bioactivity-wise, Diphenhydramine shows potent antihistaminic activity, inhibiting histamine H1 receptor with an IC50 value of 1.0 nM in guinea pig ileum. It also exhibits significant anti-inflammatory and anti-allergic properties, reducing foot edema in rats and demonstrating protection in guinea pig anaphylaxis assays. The compound shows broad inhibitory activity against various enzymes and receptors, including histamine N-methyl-transferase (activity of 10.0 nM) and UGT1A4 enzyme. It also inhibits the binding of Batrachotoxinin [3H]BTX-B to voltage-dependent sodium channels with an IC50 of 6000.0 nM and exhibits 59.8% inhibition at 10 µM in the same assay. Diphenhydramine also demonstrates antiviral activity against SARS-CoV-2 with an IC50 value greater than 20000.0 nM for inhibiting virus-induced cytotoxicity in Vero-6 cells, and a 11.32% inhibition of SARS-CoV-2 3CL-Pro protease at 20µM. It shows potential as an anti-nociceptive agent, reducing scratching behaviors in mice models induced by histamine. Furthermore, Diphenhydramine inhibits various ion channels, including the human ERG potassium channel (IC50 = 26915.35 nM), and shows inhibitory effects on sodium and calcium currents in cardiac cells. It also demonstrates activity against a range of histamine, serotonin, and muscarinic receptors, indicating its diverse pharmacological profile. Despite its broad-spectrum activity, Diphenhydramine exhibits moderate liver toxicity and high metabolic stability in rat liver microsomes, with a half-life of 0.1133 hours and intrinsic clearance values indicative of rapid metabolism. These features make Diphenhydramine a compound of significant interest for potential therapeutic applications across various pathways and target sites..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Diphenhydramine (Syntedril), a first-generation antihistamine possessing antiemetic, antitussive, anticholinergic, and sedative properties, is mainly used in the treatment of allergies. Diphenhydramine is also used in the management of drug-induced parkinsonism and other extrapyramidal symptoms.
Targets&IC50	NMDAR:24.6 μM
Synonyms	Syntedril, PM-255, PM255, PM 255, Debendrin, Dabylen

Chemical Properties

Molecular Weight	255.35
Formula	C₁₇H₂₁NO
Cas No.	58-73-1
Smiles	C(OCCN(C)C)(C1=CC=CC=C1)C2=CC=CC=C2
Relative Density.	1.024 g/cm3

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: Insoluble

DMSO: 242.5 mg/mL (949.68 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.9162 mL	19.5810 mL	39.1619 mL	195.8097 mL
5 mM	0.7832 mL	3.9162 mL	7.8324 mL	39.1619 mL
10 mM	0.3916 mL	1.9581 mL	3.9162 mL	19.5810 mL
20 mM	0.1958 mL	0.9790 mL	1.9581 mL	9.7905 mL
50 mM	0.0783 mL	0.3916 mL	0.7832 mL	3.9162 mL
100 mM	0.0392 mL	0.1958 mL	0.3916 mL	1.9581 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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent 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 TargetMol | 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.

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