Mepenzolate bromide

Name: Mepenzolate bromide
Brand: MedChemExpress
SKU: HY-17585
Rating: 5.0 (3 reviews)

Cat. No.: HY-17585 Purity: 99.90%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Mepenzolate bromide is an orally administered muscarinic receptor antagonist with K_is of 0.68 and 2.6 nM for hM2R and hM3R, respectively. Mepenzolate bromide can be used to suppress the gastrointestinal hypermotility associated with irritable bowel syndrome.Mepenzolate bromide is a GPR109A inhibitor.

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

Mepenzolate bromide Chemical Structure

CAS No. : 76-90-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
1 g		Get quote
5 g		Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

3 Publications Citing Use of MCE Mepenzolate bromide

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mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

mAChR^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	64.9 μM Compound: Mepensolate	Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy	[PMID: 18788725]

In Vitro

Mepenzolate not only exerts an anti-inflammatory effect via a muscarinic receptor-independent mechanism, but also a bronchodilatory effect via a muscarinic receptor-dependent mechanism. Mepenzolate is a subtype-non-specific muscarinic antagonist whose bronchodilatory effect and inhibitory effect on intestinal motility can be explained by its antagonistic action on M3R^[1].

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

In Vivo

Mepenzolate bromide, a GPR109A receptor blocker, abolishes the beneficial effects of niacin on body weight, colon wet weight as well as colonic levels of myeloperoxidase (MPO) and VEGF^[2].
Mepenzolate bromide is a muscarinic antagonist. Intratracheal administration or inhalation of Mepenzolate bromide decreases the severity of elastase-induced airspace enlargement and respiratory dysfunction. Mepenzolate bromide may be an effective therapeutic for the treatment of chronic obstructive pulmonary disease (COPD) due to its anti-inflammatory and bronchodilatory activities^[3].

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

Animal Model:	Adult male Wistar rats, weighing 150-200 g^[2]
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection
Result:	Abolished the protective effect of niacin against iodoacetamide-induced rise in colon wet weight as well as the colonic levels of both MPO and VEGF.

Animal Model:	ICR mice (4-6 weeks old, male) and DBA/2 mice (5 weeks old, female)^[3]
Dosage:	0.04, 0.38, 3.8, 38 μg/kg; 45.2 and 226 μg per chamber
Administration:	"0.04, 0.38, 3.8, 38 μg/kg administered intratracheally once daily for 14 days 45.2 and 226 μg per chamber by inhalation once daily for 14 days"
Result:	The simultaneous daily intratracheal administration suppressed this enlargement in a dose-dependent manner. The inhalation route was similar to those observed with the intratracheal mode of administration.

Molecular Weight

420.34

Formula

C₂₁H₂₆BrNO₃

CAS No.

76-90-4

Appearance

Solid

Color

White to off-white

SMILES

C[N+]1(C)CC(OC(C(C2=CC=CC=C2)(O)C3=CC=CC=C3)=O)CCC1.[Br-]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (594.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 10 mg/mL (23.79 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3790 mL	11.8951 mL	23.7903 mL
5 mM	0.4758 mL	2.3790 mL	4.7581 mL
10 mM	0.2379 mL	1.1895 mL	2.3790 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* 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 (4.95 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 (4.95 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 (4.95 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: Saline
Solubility: 10 mg/mL (23.79 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.90%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (250 KB) HNMR (253 KB) LCMS (261 KB)

Handling Instructions (2659 KB)

References

[1]. Yasunobu Yamashita,et al.Synthesis and biological comparison of enantiomers of mepenzolate bromide, a muscarinic receptor antagonist with bronchodilatory and anti-inflammatory activities. Bioorg Med Chem. 2014 Jul 1;22(13):3488-97. [Content Brief]

[2]. Hesham Aly Salem, et al. Effect of Niacin on Inflammation and Angiogenesis in a Murine Model of Ulcerative Colitis. Sci Rep. 2017 Aug 2;7(1):7139. [Content Brief]

[3]. Ken-Ichiro Tanaka, et al. Mepenzolate bromide displays beneficial effects in a mouse model of chronic obstructive pulmonary disease. Nat Commun. 2013;4:2686. [Content Brief]

Complete Stock Solution Preparation Table

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

H₂O / DMSO	1 mM	2.3790 mL	11.8951 mL	23.7903 mL	59.4757 mL
	5 mM	0.4758 mL	2.3790 mL	4.7581 mL	11.8951 mL
	10 mM	0.2379 mL	1.1895 mL	2.3790 mL	5.9476 mL
	15 mM	0.1586 mL	0.7930 mL	1.5860 mL	3.9650 mL
	20 mM	0.1190 mL	0.5948 mL	1.1895 mL	2.9738 mL
DMSO	25 mM	0.0952 mL	0.4758 mL	0.9516 mL	2.3790 mL
	30 mM	0.0793 mL	0.3965 mL	0.7930 mL	1.9825 mL
	40 mM	0.0595 mL	0.2974 mL	0.5948 mL	1.4869 mL
	50 mM	0.0476 mL	0.2379 mL	0.4758 mL	1.1895 mL
	60 mM	0.0397 mL	0.1983 mL	0.3965 mL	0.9913 mL
	80 mM	0.0297 mL	0.1487 mL	0.2974 mL	0.7434 mL
	100 mM	0.0238 mL	0.1190 mL	0.2379 mL	0.5948 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.