Name: Pilocarpine HCl
Brand: Selleck Chemicals
SKU: S4231
Availability: InStock
Rating: 5 (9 reviews)

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Quality Control

Batch: Purity: 99.6621%

99.6621

Related Targets	Adrenergic Receptor 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other AChR Inhibitors	PNU-120596 Benzethonium Chloride Arecoline HBr Lycorine Otilonium Bromide Hyoscyamine (-)-Huperzine A (HupA) Nitenpyram Cytisine Palmatine

Solubility

In vitro
Batch:

DMSO : 49 mg/mL (200.22 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 49 mg/mL

Ethanol : 49 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.450mg/ml (10.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 49 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.400mg/ml (1.63mM)	Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	244.72	Formula	C₁₁H₁₆N₂O₂.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	54-71-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC 5746 HCl			Smiles	CCC1C(COC1=O)CC2=CN=CN2C.Cl

Mechanism of Action

Targets/IC₅₀/Ki	mAChR
In vitro	Pilocarpine is a parasympathomimetic alkaloid obtained from the leaves of tropical American shrubs from the genus Pilocarpus. It is a non-selective muscarinic receptor agonist in the parasympathetic nervous system, which acts therapeutically at themuscarinic acetylcholine receptor M3 due to its topical application, e.g., in glaucoma and xerostomia. Pilocarpine acts on a subtype of muscarinic receptor (M3) found on the iris sphincter muscle, causing the muscle to contract and engage in miosis. Pilocarpine also acts on the ciliary muscle and causes it to contract. When the ciliary muscle contracts, it opens the trabecular meshwork through increased tension on the scleral spur. This action facilitates the rate that aqueous humorleaves the eye to decrease intraocular pressure. In ophthalmology, pilocarpine is also used to reduce the possibility of glare at night from lights when the patient has undergone implantation of phakic intraocular lenses; the use of pilocarpine would reduce the size of the pupils, relieving these symptoms. The most common concentration for this use is pilocarpine 1%, the weakest concentration. Pilocarpine is also used to treat dry mouth (xerostomia) which can occur, for example, as a side effect of radiation therapy for head and neck cancers. Pilocarpine stimulates the secretion of large amounts of saliva and sweat.
References	[1] https://pubmed.ncbi.nlm.nih.gov/8028781/ [2] https://pubmed.ncbi.nlm.nih.gov/9920179/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05506137	Not yet recruiting	Xerostomia\|Dry Mouth	Maastricht University Medical Center\|ZonMw: The Netherlands Organisation for Health Research and Development	January 2023	Phase 3
NCT05564832	Recruiting	Near Vision	Shahid Beheshti University of Medical Sciences	August 1 2022	Early Phase 1
NCT05006898	Completed	Presbyopia	Optall Vision	June 1 2020	Phase 1
NCT04005079	Withdrawn	Open Angle Glaucoma\|Ocular Hypertension	Montefiore Medical Center	June 5 2019	Phase 3
NCT03912792	Withdrawn	XLHED	Dermelix Biotherapeutics LLC.	June 28 2019	--

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Pilocarpine HCl AChR agonist

Chemical Structure

Molecular Weight: 244.72