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


| 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] |
| Synonyms | Pilocarpine HCl, NSC 5746 HCl, (+)-Pilocarpine hydrochloride |
| Molecular Weight | 244.72 |
| Formula | C11H16N2O2·HCl |
| Cas No. | 54-71-7 |
| Smiles | Cl.CCC1C(Cc2cncn2C)COC1=O |
| Relative Density. | no data available |
| Storage | Store 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
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. | ||||||||||||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
stock solution to 400 µL PEG300
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 ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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