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Glycopyrrolate AChR antagonist

Name: Glycopyrrolate
Brand: Selleck Chemicals
SKU: S4660
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S4660

Glycopyrrolate (Glycopyrronium, Robinul, Gastrodyn) is a muscarinic antagonist used as an antispasmodic, in some disorders of the gastrointestinal tract, and to reduce salivation with some anesthetics.

Chemical Structure

Molecular Weight: 398.33

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Quality Control

Batch: Purity: 99.91%

99.91

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:

Water : 79 mg/mL

DMSO : 65 mg/mL (163.18 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 59 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.
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.	3.25mg/ml (8.16mM)	Taking the 1 mL working solution as an example, add 50 μL of 65 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.	0.46mg/ml (1.15mM)	Taking the 1 mL working solution as an example, add 50 μL of 9.2 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.

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	398.33	Formula	C₁₉H₂₈NO₃.Br	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	596-51-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Glycopyrrolate bromide, Glycopyrronium bromide, Robinul, Gastrodyn			Smiles	C[N+]1(CCC(C1)OC(=O)C(C2CCCC2)(C3=CC=CC=C3)O)C.[Br-]

Mechanism of Action

Targets/IC₅₀/Ki	Muscarinic receptor
In vitro	Glycopyrrolate inhibits EFS-induced contraction of guinea-pig trachea and human airways in a concentration-dependent manner. In competition studies, this compound binds human peripheral lung and human airway smooth muscle (HASM) muscarinic receptors with affinities in the nanomolar range (Ki values 0.5–3.6 nM). It showed no selectivity in its binding to the M1–M3 receptors. Kinetics studies show that this chemical dissociates slowly from HASM muscarinic receptors.
References	[1] https://pubmed.ncbi.nlm.nih.gov/10385241/ [2] https://pubmed.ncbi.nlm.nih.gov/22069044/

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06291363	Not yet recruiting	Opioid Use Unspecified\|Anesthesia\|Nociceptive Pain	Ciusss de L''Est de l''Île de Montréal	April 4 2024	Phase 4
NCT04979039	Unknown status	Cesarean Section	Seoul National University Bundang Hospital	August 1 2021	--
NCT04554589	Unknown status	Effect of Drugs	Tanta University	September 14 2020	Phase 1

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