Benzethonium Chloride

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

Benzethonium Chloride Chemical Structure

Benzethonium Chloride Chemical Structure

CAS: 121-54-0

Selleck's Benzethonium Chloride has been cited by 5 publications

Purity & Quality Control

Batch: S416201 DMSO] 90 mg/mL] false] Water] 90 mg/mL] false] Ethanol] 90 mg/mL] false Purity: 99.18%
99.18

Benzethonium Chloride Related Products

Signaling Pathway

Choose Selective AChR Inhibitors

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
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 ICl(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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models established FaDu tumors in SCID mice.
Dosages 5 mg/kg
Administration intraperitoneal injection

Chemical Information & Solubility

Molecular Weight 448.08 Formula

C27H42NO2.Cl

CAS No. 121-54-0 SDF Download Benzethonium Chloride SDF
Smiles CC(C)(C)CC(C)(C)C1=CC=C(C=C1)OCCOCC[N+](C)(C)CC2=CC=CC=C2.[Cl-]
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 90 mg/mL ( (200.85 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 90 mg/mL

Ethanol : 90 mg/mL


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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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