Pilocarpine Hydrochloride

Name: Pilocarpine Hydrochloride
Brand: MedChemExpress
SKU: HY-B0726
Rating: 5.0 (29 reviews)

Cat. No.: HY-B0726 Purity: 99.98%: FAQs
Data Sheet SDS COA Handling Instructions

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Pilocarpine Hydrochloride is a potent M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.

For research use only. We do not sell to patients.

Pilocarpine Hydrochloride Chemical Structure

CAS No. : 54-71-7

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
500 mg	USD 35	In-stock	Estimated Time of Arrival: December 31
1 g	USD 64	In-stock	Estimated Time of Arrival: December 31
5 g	USD 229	In-stock	Estimated Time of Arrival: December 31
10 g	USD 390	In-stock	Estimated Time of Arrival: December 31
50 g		Get quote

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Customer Review

Based on 29 publication(s) in Google Scholar

Other Forms of Pilocarpine Hydrochloride:

Pilocarpine-d₃ hydrochloride Get quote
Pilocarpine-d₅ hydrochloride Get quote
Pilocarpine Get quote
Pilocarpine nitrate Get quote
Pilocarpine Hydrochloride (Standard) Get quote

29 Publications Citing Use of MCE Pilocarpine Hydrochloride

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mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Pilocarpine Hydrochloride is a potent M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.

IC₅₀ & Target

mAChR3

In Vitro

To evaluate the cytotoxicity of Pilocarpine, the morphology and viability of human corneal stromal (HCS) cells are examined by light microscopy and MTT assay, respectively. Morphological observations show that HCS cells exposed to Pilocarpine at a concentration from 0.625 to 20 g/L exhibit dose- and time-dependent proliferation retardation and morphological abnormality such as cellular shrinkage, cytoplasmic vacuolation, detachment from culture matrix, and eventually death, while no obvious difference is observed between those exposed to Pilocarpine below the concentration of 0.625 g/L and controls. Results of MTT assay reveal that the cell viability of HCS cells decrease with time and concentration after exposing to Pilocarpine above the concentration of 0.625 g/L (P<0.01 or 0.05), while that of HCS cells treated with Pilocarpine below the concentration of 0.625 g/L show no significant difference to controls^[2]. The partial muscarinic agonist, Pilocarpine, evokes concentration-dependent relaxation with an EC₅₀ of 2.4 mM in isolated segments of rat tail artery that were constricted with Penylephrine (10 to 200 nM)^[3].

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

In Vivo

The Pilocarpine-induced saliva secretion of the control rats (CN) and exercised (EX) rats is examined. A significantly greater amount of saliva is induced by Pilocarpine in the EX rats than in the CN rats (P<0.01). Conversely, the Na⁺ concentration in the saliva of the EX rats is significantly lower than that of the CN rats (P<0.05)^[1].

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

Clinical Trial

Molecular Weight

244.72

Formula

C₁₁H₁₇ClN₂O₂

CAS No.

54-71-7

Appearance

Solid

Color

White to off-white

SMILES

CN1C(C[C@@H](COC2=O)[C@@H]2CC)=CN=C1.Cl

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (408.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : ≥ 37 mg/mL (151.19 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	4.0863 mL	20.4315 mL	40.8630 mL
5 mM	0.8173 mL	4.0863 mL	8.1726 mL
10 mM	0.4086 mL	2.0432 mL	4.0863 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (8.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (8.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (8.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 130 mg/mL (531.22 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.98%

Select Batch:

Data Sheet (282 KB) SDS (420 KB)

COA (251 KB) HNMR (278 KB) LCMS (265 KB) OR (170 KB)

Handling Instructions (2659 KB)

References

[1]. Matsuzaki K, et al. Daily voluntary exercise enhances pilocarpine-induced saliva secretion and aquaporin 1 expression in rat submandibular glands. FEBS Open Bio. 2017 Dec 7;8(1):85-93. [Content Brief]

[2]. Tonta MA, et al. Pilocarpine-induced relaxation of rat tail artery by a non-cholinergic mechanism and in the absence of an intact endothelium. Br J Pharmacol. 1994 Jun;112(2):525-32. [Content Brief]

[3]. Yuan XL, et al. Cytotoxicity of pilocarpine to human corneal stromal cells and its underlying cytotoxic mechanisms. Int J Ophthalmol. 2016 Apr 18;9(4):505-11. [Content Brief]

[4]. Wang RF, et al. Post-treatment with the GLP-1 analogue liraglutide alleviate chronic inflammation and mitochondrial stress induced by Status epilepticus. Epilepsy Res. 2018 Mar 9;142:45-52. [Content Brief]

Cell Assay ^[2]	Cell viability is determined by MTT assay. Briefly, HCS cells are inoculated into a 96-well culture plate (Nunc) at a density of 1×10⁴ cells/100 µL/well, and are cultured and treated. At a 4h interval, the Pilocarpine (0.625 to 20 g/L)-containing medium is replaced entirely with 100 µL serum-free DMEM/F12 medium containing 1.0 g/L MTT, and the cells are incubated at 37°C in the dark for 4h. After the MTT-containing medium is discarded with caution, 150 µL DMSO is added to dissolve the produced formazan crystals at 37°C in the dark for 15 min, and the absorbance at 490 nm is measured with a Multiskan GO microplate reader^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Rats^[1] Male, 10-week-old Wistar rats are assigned to one of two groups, exercise (EX, n=6) and control (CN, n=6). The EX rats are kept for 40 days in cages with a running wheel (SN-451), allowing them to undertake voluntary exercise, while the CN rats are kept in cages with the running wheel locked. On the 40th day, Pilocarpine-induced saliva is measured as follows. Briefly, the rats are anesthetized, preweighed cotton was placed in their mouths sublingually, and Pilocarpine (0.5 mg/kg) is intraperitoneally injected to induce saliva secretion. Each cotton ball is then changed every 10 min for 1 h. The collected cotton balls are weighed again, and the mass of saliva secreted is calculated by subtracting the initial from the final weight. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Matsuzaki K, et al. Daily voluntary exercise enhances pilocarpine-induced saliva secretion and aquaporin 1 expression in rat submandibular glands. FEBS Open Bio. 2017 Dec 7;8(1):85-93. [Content Brief] [2]. Tonta MA, et al. Pilocarpine-induced relaxation of rat tail artery by a non-cholinergic mechanism and in the absence of an intact endothelium. Br J Pharmacol. 1994 Jun;112(2):525-32. [Content Brief] [3]. Yuan XL, et al. Cytotoxicity of pilocarpine to human corneal stromal cells and its underlying cytotoxic mechanisms. Int J Ophthalmol. 2016 Apr 18;9(4):505-11. [Content Brief] [4]. Wang RF, et al. Post-treatment with the GLP-1 analogue liraglutide alleviate chronic inflammation and mitochondrial stress induced by Status epilepticus. Epilepsy Res. 2018 Mar 9;142:45-52. [Content Brief]

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	4.0863 mL	20.4315 mL	40.8630 mL	102.1576 mL
	5 mM	0.8173 mL	4.0863 mL	8.1726 mL	20.4315 mL
	10 mM	0.4086 mL	2.0432 mL	4.0863 mL	10.2158 mL
	15 mM	0.2724 mL	1.3621 mL	2.7242 mL	6.8105 mL
	20 mM	0.2043 mL	1.0216 mL	2.0432 mL	5.1079 mL
	25 mM	0.1635 mL	0.8173 mL	1.6345 mL	4.0863 mL
	30 mM	0.1362 mL	0.6811 mL	1.3621 mL	3.4053 mL
	40 mM	0.1022 mL	0.5108 mL	1.0216 mL	2.5539 mL
	50 mM	0.0817 mL	0.4086 mL	0.8173 mL	2.0432 mL
	60 mM	0.0681 mL	0.3405 mL	0.6811 mL	1.7026 mL
	80 mM	0.0511 mL	0.2554 mL	0.5108 mL	1.2770 mL
	100 mM	0.0409 mL	0.2043 mL	0.4086 mL	1.0216 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.