Benzethonium Chloride

Catalog No.S4162

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

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Benzethonium Chloride Chemical Structure

Benzethonium Chloride Chemical Structure
Molecular Weight: 448.08

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Quality Control & MSDS

Product Information

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Product Description

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]
IC50 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 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]
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]
Features

Protocol(Only for 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.
Formulation PBS
Dosages 5 mg/kg
Administration intraperitoneal injection

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Coates KM, et al. Br J Pharmacol, 2001, 134(4), 871-879.

[2] Zaman Z, et al. Eur J Clin Chem Clin Biochem, 1997, 35(8), 603-607.

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Chemical Information

Download Benzethonium Chloride SDF
Molecular Weight (MW) 448.08
Formula

C27H42NO2.Cl

CAS No. 121-54-0
Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms
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.
Chemical Name Benzenemethanaminium, N,N-dimethyl-N-[2-[2-[4-(1,1,3,3-tetramethylbutyl)phenoxy]ethoxy]ethyl]-, chloride (1:1)

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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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