Benzethonium Chloride

Catalog No.S4162 Batch:S416201

Technical Data

Formula	C₂₇H₄₂NO₂.Cl
Molecular Weight	448.08	CAS No.	121-54-0
Solubility (25°C)*	In vitro	DMSO	90 mg/mL (200.85 mM)
		Water	90 mg/mL (200.85 mM)
		Ethanol	90 mg/mL (200.85 mM)
* <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.)

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Biological Activity

Description

Benzethonium chloride is a potent inhibitor of nAChRs, it inhibits α4β2 nAChRs and α7 nAChRs with IC50 of 49 nM and 122 nM, respectively.

Targets

α4β2 nAChRs ^[1]	α7 nAChRs ^[1]
49 nM	122 nM

In vitro

Benzethonium chloride inhibits acetylcholine responses in the α7 nAChRs in a mixed competitive and non-competitive manner but there is no voltage- or use-dependence of the response in either subtype. ^[1] Benzethonium chloride produces mixed-type inhibition of choline esterase and acetylcholine esterase-affecting both Fmax and Km, Choline esterase is about 10-fold more sensitive to benzethonium chloride than acetylcholine esterase. ^[2] Benzethonium chloride inhibits I_Cl(Ca) in response to 0.1 μM acetyl-beta-methylcholine in oocytes expressing m1 muscarinic receptors with IC50 of 0.88 μM. Benzethonium chloride combined with racemic S(+)/R(-) ketamine inhibits muscarinic signaling with a calculated IC50 of 15 μM and a Hill coefficient of 0.6. ^[3] Benzethonium (5 μM) significantly increases cytosolic Ca(2+)-concentration, decreases forward scatter and triggered annexin V-binding affecting some 30% of the erythrocytes. Benzethonium (5 μM) further significantly enhances the effect of glucose depletion on cytosolic Ca(2+)-concentration and annexin V-binding, but significantly blunts the effect of glucose depletion on forward scatter. Benzethonium (5 μM) significantly enhances lactic acid formation but not ceramide abundance. ^[4] Benzethonium chloride reduces cell viability with IC50 of 3.8 μM in FaDu, 42.2 μM in NIH 3T3, 5.3 μM in C666-1, and 17.0 μM in GM05757. Benzethonium chloride (9 μM) induces apoptosis and activates caspases after 12 hours in FaDu cells. ^[5]

In vivo

Benzethonium chloride (5 mg/kg) ablates the tumor-forming ability of FaDu cells, delays the growth of xenograft tumors, and combined additively with local tumor radiation therapy in established FaDu tumors in SCID mice. ^[5]

Protocol (from reference)

Cell Assay:^{^[5]}	Cell lines FaDu, C666-1, NIH 3T3 and GM05757 cell lines Concentrations 42.2 μM Incubation Time 48 hours Method Cells are seeded in 96-well plates at 5,000 per well in 100 μL of growth medium and allowed to incubate for 24 hours. Benzethonium chloride is then added, as indicated, in a total volume of 5 μL. After 48 hours, MTS assay is done according to the specifications of the manufacturer, with DMSO (0.1%)–treated cells as negative control and cisplatin (166.6 μM)–treated cells as positive control.
Animal Study:^{^[5]}	Animal Models established FaDu tumors in SCID mice. Dosages 5 mg/kg Administration intraperitoneal injection

Cell Assay:^{^[5]}

Cell lines
FaDu, C666-1, NIH 3T3 and GM05757 cell lines
Concentrations
42.2 μM
Incubation Time
48 hours
Method
Cells are seeded in 96-well plates at 5,000 per well in 100 μL of growth medium and allowed to incubate for 24 hours. Benzethonium chloride is then added, as indicated, in a total volume of 5 μL. After 48 hours, MTS assay is done according to the specifications of the manufacturer, with DMSO (0.1%)–treated cells as negative control and cisplatin (166.6 μM)–treated cells as positive control.

Animal Study:^{^[5]}

Animal Models
established FaDu tumors in SCID mice.
Dosages
5 mg/kg
Administration
intraperitoneal injection

References

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Selleck's Benzethonium Chloride has been cited by 6 publications

The liver microenvironment orchestrates FGL1-mediated immune escape and progression of metastatic colorectal cancer [ Nat Commun, 2023, 10.1038/s41467-023-42332-0]	PubMed: 37872170
The liver microenvironment orchestrates FGL1-mediated immune escape and progression of metastatic colorectal cancer [ Nat Commun, 2023, 14(1):6690]	PubMed: 37872170
Targeting CD36 determines nicotine derivative NNK-induced lung adenocarcinoma carcinogenesis [ iScience, 2023, 26(8):107477]	PubMed: 37599821
Utilizing an Endogenous Progesterone Receptor Reporter Gene for Drug Screening and Mechanistic Study in Endometrial Cancer [ Cancers (Basel), 2022, 14(19)4883]	PubMed: 36230806
Eryptosis and Malaria: New Experimental Guidelines and Re-Evaluation of the Antimalarial Potential of Eryptosis Inducers [ Front Cell Infect Microbiol, 2021, 11:630812]	PubMed: 33777843
Benzethonium chloride suppresses lung cancer tumorigenesis through inducing p38-mediated cyclin D1 degradation. [ Am J Cancer Res, 2019, 9(11):2397-2412]	PubMed: 31815042

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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.

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