Cat. No.: HY-B0303A

Diphenhydramine hydrochloride

9 Cited Publications

Customer Review

Based on 9 publication(s) in Google Scholar

Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB).

For research use only. We do not sell to patients.

Purity: 99.93%
CAS No.: 147-24-0
Formula: C₁₇H₂₂ClNO
Molecular Weight:291.82

Storage:

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Diphenhydramine hydrochloride Chemical Structure

CAS No.: 147-24-0

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (9)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB)^[1]^[2].

IC₅₀ & Target

H₁ Receptor

All Histamine Receptor Isoforms :

All Endogenous Metabolite Isoforms :

In Vitro

Diphenhydramine hydrochloride inhibits Cisplatin (HY-17394)-induced cell death in kidney proximal tubular cells (HK-2 and LLC-PK1 cells)^[3].
Diphenhydramine (0.2-1 mM, 24 h) hydrochloride inhibits cell viability in CCRF-CEM and Jurkat cells^[4].
Diphenhydramine (0.5 and 1 mM, 24 h) hydrochloride induces apoptosis in CCRF-CEM and Jurkat cells^[4].
Diphenhydramine (0-10 μg/mL, 24 or 48 h) hydrochloride increases the expression of Bad and Bax, and decreases BCL-2 level in PANC-1 cells^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[5]

Cell Line:

PANC-1 cells
Concentration:

0-10 μg/mL
Incubation Time:

24 or 48 h
Result:

Increased the expression of Bad and Bax, and decreased Bcl2 level.
Decreased the expression of p-AKT (Thr308), p-AKT (Ser 473), p-mTOR (Ser 2448), p-FoxO1 (Ser 256), p-MDM2 (Ser 166), p-NF-ĸB p65 (Ser 536), and p-GSK-3 (Ser 9).

In Vivo

Diphenhydramine (20 mg/kg) hydrochloride inhibits Cisplatin (HY-17394)-induced kidney toxicity in mice^[3].
Diphenhydramine (3-30 mg/kg, i.m., 5 minutes prior to a s.c. of 25 mg/kg Dichlorvos) hydrochloride reduces mortality in rats with acute, severe dichlorvos exposure^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 147-24-0
Appearance Solid
Molecular Weight 291.82
Formula C₁₇H₂₂ClNO
Color White to off-white
SMILES

CN(C)CCOC(C1=CC=CC=C1)C2=CC=CC=C2.Cl
Structure Classification
- Alkaloids
- Other Alkaloids
Initial Source
- Endogenous metabolite
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Publications (9)

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Journal Impact Factor

Acta Pharmacol Sin

Desloratadine ameliorates paclitaxel-induced peripheral neuropathy and hypersensitivity reactions in mice. [Abstract]

2024 Oct;45(10):2061-2076. PMID: 38789495
Cell Rep

Curative islet and hematopoietic cell transplantation in diabetic mice without toxic bone marrow conditioning. [Abstract]

2022 Nov 8;41(6):111615. PMID: 36351397
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
Am J Physiol Cell Physiol

Redox-sensitive GPCR signaling drives Gq-dependent Ca²⁺ mobilization and cytokine production in human bronchial epithelial cells. [Abstract]

2026 Jun 18. PMID: 42314770
Pharm Res

Profiling Interactions Between Bicyclol and SLC/ABC Transporters: Advancing Clinical Safety and Efficacy in Combination Therapy. [Abstract]

2025 Oct 27. PMID: 41145746
Pharmacol Res Perspect

Effects of membrane transport activity and cell metabolism on the unbound drug concentrations in the skeletal muscle and liver of drugs: A microdialysis study in rats. [Abstract]

2021 Oct;9(5):e00879. PMID: 34628723
Res Sq

2026 Mar 10.
bioRxiv

Curing autoimmune diabetes with islet and hematopoietic cell transplantation after CD117 antibody-based conditioning. [Abstract]

2025 Sep 10:2025.09.05.673576. PMID: 40964321
Chemosphere

Mass-balance-model-based evaluation of sewage treatment plant contribution to residual pharmaceuticals in environmental waters. [Abstract]

2019 Jun:225:378-387. PMID: 30884299

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (342.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 100 mg/mL (342.68 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.4268 mL

17.1338 mL

34.2677 mL

5 mM

0.6854 mL

3.4268 mL

6.8535 mL

10 mM

0.3427 mL

1.7134 mL

3.4268 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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Volume _(start) Volume _(start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (8.57 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (8.57 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.57 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS

Solubility: 130 mg/mL (445.48 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Simons FE. H1-receptor antagonists. Comparative tolerability and safety. Drug Saf. 1994;10(5):350-380. [Content Brief]

[2]. Sadiq MW, et al. Diphenhydramine active uptake at the blood-brain barrier and its interaction with oxycodone in vitro and in vivo. J Pharm Sci. 2011;100(9):3912-3923. [Content Brief]

[3]. Hamano H, et al. Diphenhydramine may be a preventive medicine against cisplatin-induced kidney toxicity. Kidney Int. 2021 Apr;99(4):885-899. [Content Brief]

[4]. Jangi SM, et al. Apoptosis of human T-cell acute lymphoblastic leukemia cells by diphenhydramine, an H1 histamine receptor antagonist. Oncol Res. 2004;14(7-8):363-72. [Content Brief]

[5]. Zhang R, Chen M, Yu L, et al. Anticancer activity of diphenhydramine against pancreatic cancer by stimulating cell cycle arrest, apoptosis, and modulation of PI3K/Akt/mTOR pathway[J]. Cell proliferation, 2021, 69: 5.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / H₂O	1 mM	3.4268 mL	17.1338 mL	34.2677 mL	85.6692 mL
	5 mM	0.6854 mL	3.4268 mL	6.8535 mL	17.1338 mL
	10 mM	0.3427 mL	1.7134 mL	3.4268 mL	8.5669 mL
	15 mM	0.2285 mL	1.1423 mL	2.2845 mL	5.7113 mL
	20 mM	0.1713 mL	0.8567 mL	1.7134 mL	4.2835 mL
	25 mM	0.1371 mL	0.6854 mL	1.3707 mL	3.4268 mL
	30 mM	0.1142 mL	0.5711 mL	1.1423 mL	2.8556 mL
	40 mM	0.0857 mL	0.4283 mL	0.8567 mL	2.1417 mL
	50 mM	0.0685 mL	0.3427 mL	0.6854 mL	1.7134 mL
	60 mM	0.0571 mL	0.2856 mL	0.5711 mL	1.4278 mL
	80 mM	0.0428 mL	0.2142 mL	0.4283 mL	1.0709 mL
	100 mM	0.0343 mL	0.1713 mL	0.3427 mL	0.8567 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Diphenhydramine hydrochloride

9 Cited Publications

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Diphenhydramine hydrochloride

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Publications Citing Use of MedChemExpress (MCE) Diphenhydramine hydrochloride

All Histamine Receptor Isoforms

All Endogenous Metabolite Isoforms

Biological Activity

Chemical Information

Publications (9)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Diphenhydramine hydrochloride Related Classifications

HY-B0303A Related Classifications