1. Others Neuronal Signaling
  2. Insecticide Cholinesterase (ChE)
  3. Phosalone

Phosalone is an orally active, blood-brain barrier penetrant Insecticide and acaricide. Phosalone inhibits the activity of Acetylcholinesterase. Phosalone acts as a substrate for detoxifying esterases. Phosalone induces symptoms of cholinergic hyperactivity, toxic reactions, mortality, oxidative stress, and changes in pro-inflammatory protein levels, and exerts toxic effects on colonic tissues and cells. Phosalone controls pistachio psyllids. Phosalone can be used in studies related to colitis.

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Phosalone

Phosalone Chemical Structure

CAS No. : 2310-17-0

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Based on 1 publication(s) in Google Scholar

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Description

Phosalone is an orally active, blood-brain barrier penetrant Insecticide and acaricide. Phosalone inhibits the activity of Acetylcholinesterase. Phosalone acts as a substrate for detoxifying esterases. Phosalone induces symptoms of cholinergic hyperactivity, toxic reactions, mortality, oxidative stress, and changes in pro-inflammatory protein levels, and exerts toxic effects on colonic tissues and cells. Phosalone controls pistachio psyllids. Phosalone can be used in studies related to colitis[1][2][3].

IC50 & Target[1]

Mite

 

AChE

 

In Vitro

Phosalone (Five or six distinct concentrations; 24 h) exhibits variable toxicity to 5th instar nymphs of nine Agonoscena pistaciae populations, with the Rafsanjan (RF) population showing the highest resistance (11.3-fold) and the Bam (BA) population being the most susceptible (LC50 = 55 mg/L)[3].
Phosalone (Various concentrations; 8 h) is 15.65-fold more toxic to susceptible (BA) adult Agonoscena pistaciae (LC50 = 1.14 mg/L) than to resistant (RF) adults, with TPP (synergist ratio 3.14) and DEM (synergist ratio 1.41) enhancing phosalone toxicity in RF adults, while PBO acts antagonistically (synergist ratio 0.45)[3].

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

In Vivo

Phosalone (4-130 mg/kg; p.o.; single dose) has an acute oral LD50 of 120 mg/kg in combined male and female CD (COBS) rats, with minimal lethal doses ranging from 67 to 100 mg/kg depending on sex[1].
Phosalone (4-36 mg/kg; p.o.; single dose) inhibits erythrocyte, plasma, and brain cholinesterase in female CD (COBS) rats after single oral administration, with peak erythrocyte cholinesterase inhibition (ID50 = 10.5 mg/kg) occurring 5 hours post-dose[1].
Phosalone (6-40 mg/kg; gavage; daily; 30 days) induces dose-dependent colon inflammation and oxidative stress in male Wistar rats, with the highest tested dose (40 mg/kg, 1/3 LD50) causing the most severe reductions in AChE activity, total thiols, and antioxidant power, plus the greatest elevations in inflammatory markers, myeloperoxidase activity, and lipid peroxidation[2].

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

Animal Model: Wistar (male, 180-200 g)[2]
Dosage: 6-40 mg/kg
Administration: gavage; daily; 30 days
Result: Caused severe degeneration of mucosal muscle cells and muscle layers, plus significant infiltration of mononuclear inflammatory cells between mucosal glands at 40 mg/kg.
Caused relatively severe muscle layer degeneration and mononuclear cell infiltration at 20 mg/kg.
Caused significant muscle layer degeneration and mild mononuclear cell infiltration at 12 mg/kg.
Caused mild muscle layer degeneration and mild mucosal inflammation at 6 mg/kg.
Reduced AChE activity to 25% (40 mg/kg), 29% (20 mg/kg), 33% (12 mg/kg), and 50% (6 mg/kg) of normal levels, with significant decreases for 40 mg/kg and 20 mg/kg groups compared to normal or ellagic acid-only groups (p < 0.01 to p < 0.05).
Increased MPO activity to 0.387 U/mg protein (40 mg/kg), 0.292 U/mg protein (20 mg/kg), 0.214 U/mg protein (12 mg/kg), and 0.194 U/mg protein (6 mg/kg), with significant elevations for 40 mg/kg and 20 mg/kg groups compared to normal or ellagic acid-only groups (p < 0.01 to p < 0.001).
Increased TBARS levels to 447.46 μg (40 mg/kg), 422.88 μg (20 mg/kg), 390.03 μg (12 mg/kg), and 351.88 μg (6 mg/kg), with significant elevations for all doses compared to normal groups (p < 0.01 to p < 0.001).
Reduced TTM levels to 0.249 mmol/L (40 mg/kg), 0.317 mmol/L (20 mg/kg), 0.304 mmol/L (12 mg/kg), and 0.347 mmol/L (6 mg/kg), with significant decreases for all doses compared to normal groups (p < 0.05 to p < 0.01).
Reduced FRAP levels to 18.22 μmol/L (40 mg/kg), 24.70 μmol/L (20 mg/kg), 20.31 μmol/L (12 mg/kg), and 23.25 μmol/L (6 mg/kg), with significant decreases for all doses compared to normal or ellagic acid-only groups (p < 0.001).
Increased TNF-α levels to 546.43 pg/mg protein (40 mg/kg), 433.87 pg/mg protein (20 mg/kg), 375.13 pg/mg protein (12 mg/kg), and 309.50 pg/mg protein (6 mg/kg), with significant elevations for 40 mg/kg and 20 mg/kg groups compared to normal or ellagic acid-only groups (p < 0.05 to p < 0.001).
Increased IL-6β levels to 21.55 pg/mg protein (40 mg/kg), 17.54 pg/mg protein (20 mg/kg), 16.60 pg/mg protein (12 mg/kg), and 14.83 pg/mg protein (6 mg/kg), with significant elevations for all doses compared to normal groups (p < 0.001).
Increased NF-κB levels to 51.41 pg/mg protein (40 mg/kg), 32.36 pg/mg protein (20 mg/kg), 31.68 pg/mg protein (12 mg/kg), and 26.87 pg/mg protein (6 mg/kg), with significant elevations for all doses compared to normal groups (p < 0.05 to p < 0.001).
Molecular Weight

367.81

Formula

C12H15ClNO4PS2

CAS No.
Appearance

Solid

Color

Off-white to pink

SMILES

S=P(OCC)(SCN1C(OC2=CC(Cl)=CC=C12)=O)OCC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 41 mg/mL (111.47 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7188 mL 13.5940 mL 27.1880 mL
5 mM 0.5438 mL 2.7188 mL 5.4376 mL
View the Complete Stock Solution Preparation Table

* 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7188 mL 13.5940 mL 27.1880 mL 67.9699 mL
5 mM 0.5438 mL 2.7188 mL 5.4376 mL 13.5940 mL
10 mM 0.2719 mL 1.3594 mL 2.7188 mL 6.7970 mL
15 mM 0.1813 mL 0.9063 mL 1.8125 mL 4.5313 mL
20 mM 0.1359 mL 0.6797 mL 1.3594 mL 3.3985 mL
25 mM 0.1088 mL 0.5438 mL 1.0875 mL 2.7188 mL
30 mM 0.0906 mL 0.4531 mL 0.9063 mL 2.2657 mL
40 mM 0.0680 mL 0.3398 mL 0.6797 mL 1.6992 mL
50 mM 0.0544 mL 0.2719 mL 0.5438 mL 1.3594 mL
60 mM 0.0453 mL 0.2266 mL 0.4531 mL 1.1328 mL
80 mM 0.0340 mL 0.1699 mL 0.3398 mL 0.8496 mL
100 mM 0.0272 mL 0.1359 mL 0.2719 mL 0.6797 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Phosalone
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