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Pilocarpine Hydrochloride

(Synonyms: Pilocarpine HCl, NSC 5746 HCl, (+)-Pilocarpine hydrochloride) Copy Product Info
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Synonyms: Pilocarpine HCl, NSC 5746 HCl, (+)-Pilocarpine hydrochloride

Catalog No. T0804 Copy Product Info
Purity: 99.94%
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Pilocarpine Hydrochloride (NSC 5746 HCl) is an M3-type muscarinic acetylcholine receptor agonist. Pilocarpine Hydrochloride is used to generate experimental models of epilepsy.
Pilocarpine Hydrochloride
Cas No. 54-71-7
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Purity:99.94%
Color:White
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Product Introduction

Bioactivity
Description
Pilocarpine Hydrochloride (NSC 5746 HCl) is an M3-type muscarinic acetylcholine receptor agonist. Pilocarpine Hydrochloride is used to generate experimental models of epilepsy.
Targets & IC50
dimethylnitrosamine N-demethylase (mouse liver microsomes):100 μM, Testosterone 15 alpha-hydroxylase (mouse liver microsomes):6 μM, coumarin 7-hydroxylase (human liver microsomes):6 μM, Astrocytes:31.86 mM, Coumarin 7-hydroxylase (mouse liver microsomes):6 μM, Pentoxyresorufin O-dealkylas (mouse liver microsomes):4 μM, CYP2A6 (human liver microsomes):5.31μM, testosterone 6 beta-hydroxylase (mouse liver microsomes):> 1 mM, dimethylnitrosamine N-demethylase (human liver microsomes):10 μM
In vitro
Methods: Rat hippocampal brain slices (450 μm) were used to record field potentials in the CA1 region. Pilocarpine Hydrochloride (dissolved in artificial cerebrospinal fluid, aCSF) was added at concentrations of 10, 50, 100, 200, and 500 μM. Slices were continuously perfused for over 30 minutes under conditions of normal [K⁺] (3.1 mM) and high [K⁺] (6 mM) conditions for over 30 minutes. Record extracellular field potentials and observe spontaneous epileptiform discharges, paroxysmal depolarization drifts, etc.
Results: Under high [K⁺] (6 mM): 50 μM Pilocarpine Hydrochloride induces intense epileptiform discharges. [1]
In vivo
Methods: Approximately 7-week-old NodScid immunodeficient mice (both male and female) were administered 1 mg/kg N-methylscopolamine 15 minutes prior to injection to reduce peripheral cholinergic side effects. Multiple intraperitoneal injections of Pilocarpine Hydrochloride (100 mg/kg per dose) were administered administered every 10 minutes until ≥ Grade 3 seizures (Racine scale) occur, with a maximum of 6 injections. Diazepam (10 mg/kg) was administered 90 minutes after SE onset to terminate seizures. SE incidence and mortality rates were observed and recorded.
Results: Multiple Pilocarpine Hydrochloride injections yielded a high SE incidence (88.1±2.9%), low mortality rate, and high proportion of surviving SE (61.8±5.9%).[2]
SynonymsPilocarpine HCl, NSC 5746 HCl, (+)-Pilocarpine hydrochloride
Chemical Properties
Molecular Weight244.72
FormulaC11H16N2O2·HCl
Cas No.54-71-7
SmilesCl.CCC1C(Cc2cncn2C)COC1=O
Relative Density.no data available
Storage & Solubility Information
StorageStore under nitrogen Powder: -20°C for 3 years Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
H2O: 24.5 mg/mL (100.11 mM), Sonication is recommended.
DMSO: 138 mg/mL (563.91 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (16.35 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
H2O/DMSO
1mg5mg10mg50mg
1 mM4.0863 mL20.4315 mL40.8630 mL204.3151 mL
5 mM0.8173 mL4.0863 mL8.1726 mL40.8630 mL
10 mM0.4086 mL2.0432 mL4.0863 mL20.4315 mL
20 mM0.2043 mL1.0216 mL2.0432 mL10.2158 mL
50 mM0.0817 mL0.4086 mL0.8173 mL4.0863 mL
100 mM0.0409 mL0.2043 mL0.4086 mL2.0432 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 µL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
µL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

Related Tags: Pilocarpine Hydrochloride chemical structure | Pilocarpine Hydrochloride in vivo | Pilocarpine Hydrochloride in vitro | Pilocarpine Hydrochloride formula | Pilocarpine Hydrochloride molecular weight