Promethazine

SKU:BHB21902684
Research Validated
Overview
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Promethazine (CAS 60-87-7) is an antagonist supplied as a solid. Relevant to GPCR/G Protein and Neuronal Signaling research. Molecular formula C17H20N2S, molecular weight 284.42 g/mol.
Purity 99.67%
CAS Number 60-87-7
Molecular Weight 284.42 g/mol
Form Solid
Storage Powder -20°C; in solvent -80°C
Options selector
Catalog no. Size
HY-B1296-5MG 5 mg
HY-B1296-10MG 10 mg
HY-B1296-25MG 25 mg
HY-B1296-50MG 50 mg
HY-B1296-100MG 100 mg
HY-B1296-200MG 200 mg
HY-B1296-500MG 500 mg
HY-B1296-1MLX10MM 1 mL x 10 mM (in DMSO)
Available Options

Select the variant that best fits your experiment. Availability and lead time may vary by option.

  • Options: Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 mL x 10 mM (in DMSO)
  • Lead time: varies by selected option.
  • Storage: Powder: -20°C, 3 years. In solvent: -80°C, 6 months; -20°C, 1 month.
  • Shipping: Room temperature in continental US; may vary elsewhere.
  • Upon receipt: transfer to -20°C as soon as possible.
Field Specification
Alternative names (±)-Promethazine
CAS no. 60-87-7
Applications
  • Functional Assay (In Vitro)
Molecular weight 284.42
Molecular formula C17H20N2S
Purity 99.67%
SMILES CC(N(C)C)CN1C2=C(C=CC=C2)SC3=CC=CC=C31
Form Solid
Storage Powder: -20°C, 3 years. In solvent: -80°C, 6 months; -20°C, 1 month.
Shipping Room temperature in continental US; may vary elsewhere.
Catalog no. (Mfr.) HY-B1296
Main SKU BHB21902684
Antagonists

Compound Overview

Promethazine, also known as (±)-Promethazine, is an orally active histamine receptor antagonist[1]. It is a first-generation antihistamine of the phenothiazine family that shows strong sedative and weak antipsychotic effects[1][2][3][4]. It is supplied as a white to off-white solid (C17H20N2S, MW 284.42) at 99.67% purity.

Physical & Chemical Properties

CAS Number 60-87-7
Molecular Formula C17H20N2S
Molecular Weight 284.42 g/mol
Purity 99.67%
Appearance Solid
Color White to off-white
SMILES CC(N(C)C)CN1C2=C(C=CC=C2)SC3=CC=CC=C31
Signaling Pathway GPCR/G Protein; Neuronal Signaling; Immunology/Inflammation
Solubility In Vitro: DMSO: 100 mg/mL (351.59 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Storage Powder: -20°C, 3 years. In solvent: -80°C, 6 months; -20°C, 1 month.
Shipping Room temperature in continental US; may vary elsewhere.

Literature Cited

Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.

[1]. Burt DR, et al. Antischizophrenic drugs: chronic treatment elevates dopamine receptor binding in brain. Science. 1977 Apr 15;196(4287):326-8.

[2]. Strenkoski-Nix LC, et al. Pharmacokinetics of promethazine hydrochloride after administration of rectal suppositories and oral syrup to healthy subjects. Am J Health Syst Pharm. 2000 Aug 15;57(16):1499-505.

[3]. Fiorella D, et al. The role of the 5-HT2A and 5-HT2C receptors in the stimulus effects of hallucinogenic drugs. I: Antagonist correlation analysis. Psychopharmacology (Berl). 1995 Oct;121(3):347-56.

[4]. Seeman P, et al. Dopamine D2 receptor binding sites for agonists. A tetrahedral model. Mol Pharmacol. 1985 Nov;28(5):391-9.

[5]. Xinyue Tan, et al. Promethazine inhibits proliferation and promotes apoptosis in colorectal cancer cells by suppressing the PI3K/AKT pathway. Biomed Pharmacother. 2021 Nov;143:112174.

[6]. Niloofar Amidi, et al. A Behavioral Study of Promethazine Interaction with Analgesic Effect of Diclofenac: Pain Combination Therapy. J Pharmacopuncture. 2020 Mar 31;23(1):18-24.

Safety

For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.

In Vitro

SolventSolubilityNotes
DMSO100 mg/mL (351.59 mM)requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility)

Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.

In Vivo

Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.

Protocol 1

Composition10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline
Result≥ 2.5 mg/mL (8.79 mM); clear solution
How to prepareGives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL.

Protocol 2

Composition10% DMSO + 90% Corn Oil
Result≥ 2.5 mg/mL (8.79 mM); clear solution
How to prepareGives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil.

Data provided by the manufacturer.

In Vitro

In SW480, HCT116, HT29, and Caco2 CRC cells, Promethazine (0-100 μM, 24 h) suppresses proliferation in a concentration-dependent manner[5].

Cell Viability Assay[5]

Cell LineSW480, HCT116, HT29, and Caco2 CRC cells
Concentration0-100 μM
Incubation Time24 hours
ResultExhibited IC50 values of 40.96, 74.79, 27.34 and 33.00 μM in Caco2, HCT116, HT29 and SW480 cells, respectively.

In Vivo

A single intraperitoneal injection of Promethazine (2 mg/kg, 4 mg/kg, or 6 mg/kg) effectively lowers the writhing response[6].

Animal ModelMale NMRI mice (20-30 g) injected with acetic acid (0.7%)[6]
Dosage2 mg/kg, 4 mg/kg, 6 mg/kg
AdministrationIntraperitoneal injection; 2 mg/kg, 4 mg/kg, 6 mg/kg; once
ResultInhibited writhing response by 43.2%, 53.9% and 62.3% at 2, 4, 6 mg/kg.

Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.

Q.Why is there no price on some sizes?
A.Availability and lead time for those sizes are confirmed on inquiry. Send us the size you need and we will come back with price and lead time.
Q.Can this be used in humans or for diagnostics?
A.No. This product is supplied For Research Use Only. It is not for diagnostic or therapeutic procedures and not for human or veterinary use.

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Identification of anti-flaviviral drugs with mosquitocidal and anti-Zika virus activity in Aedes aegypti. PLoS Negl Trop Dis 2019 Aug 20;13(8):e0007681.

PMID: 31430351

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