2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. Umeclidinium bromide

Umeclidinium bromide  (Synonyms: GSK573719A)

Cat. No.: HY-12100 Purity: 99.54%
SDS COA Handling Instructions

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Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.

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

Umeclidinium bromide Chemical Structure

Umeclidinium bromide Chemical Structure

CAS No. : 869113-09-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 111 In-stock
Solution
10 mM * 1 mL in DMSO USD 111 In-stock
Solid
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10 mg USD 165 In-stock
25 mg USD 297 In-stock
50 mg USD 495 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Umeclidinium bromide:

Umeclidinium bromide Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Umeclidinium bromide

View All mAChR Isoform Specific Products:

View All Isoforms
mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.

IC50 & Target

mAChR1

 

mAChR5

 

Cellular Effect
Cell Line Type Value Description References
CHO IC50
< 10 μM
Compound: 14o
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
[PMID: 19317446]
In Vitro

In human embryonic kidney 293 cells, Umeclidinium bromide (GSK573719A) inhibits the human ether-a-go-go-related gene channel tail current in a concentration-dependent manner (IC50=9.4 μM)[1]. Umeclidinium bromide, previously known as GSK573719, is a novel high-affinity specific mAChR antagonist. It is a potent agent that demonstrates slow functional reversibility at cloned human M3 mAChRs and at endogenous mAChR in isolated human bronchus[2].

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

Umeclidinium bromide Related Antibodies
In Vivo

When Umeclidinium bromide (GSK573719A) is given once daily to mice for 5 consecutive days (0.025 μg intranasally), the level of inhibition on the fifth day is modestly increased above that obtained after a single administration to the same mice (60 versus 35%, respectively). After the fifth day of dosing, the mice are rested for 5 additional days, allowing bronchomotor tone to return to baseline levels. On the sixth day, the mice receive one last dose of antagonist and are once again challenged with Mch. The level of inhibition is essentially the same as that found on the first day of testing, indicating that tolerance is not evident with repeated intranasal delivery of Umeclidinium bromide. By contrast, when Umeclidinium bromide is given orally (2.0 mg/kg) to mice at a dose 100 times the ED50 value (intranasal), there is no observable protection against an Mch challenge[1].

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

508.49

Formula

C29H34BrNO2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(C12CC[N+](CC2)(CCOCC3=CC=CC=C3)CC1)(C4=CC=CC=C4)C5=CC=CC=C5.[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 : ≥ 25 mg/mL (49.17 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9666 mL 9.8330 mL 19.6661 mL
5 mM 0.3933 mL 1.9666 mL 3.9332 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.

  • Molarity Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.92 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 2.5 mg/mL (4.92 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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: 99.72%

SDS (393 KB)

COA (249 KB) HNMR (178 KB) LCMS (278 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

Ligand binding assays with Umeclidinium bromide (GSK573719A) and [3H]-N-methyl scopolamine (0.5 nM) are performed using a scintillation proximity assay for M1, M2, and M3 mAChRs and a filtration assay for M4 and M5 mAChRs. For the scintillation proximity assay assay, membranes are incubated with wheat germ agglutinin beads in 50 mM HEPES buffer, pH 7.4, at 4°C for 30 minutes and then with the radioligand in a 96-well OptiPlate for 2 hours at room temperature in the presence of vehicle (1% DMSO) or GSK573719 (0.01-300 nM). At the end of the incubation, the plates are centrifuged (for 5 minutes at 2000g), and radioactivity is counted. For the filtration assay, membranes (M4 and M5) are similarly incubated in HEPES buffer containing the radioligand for 2 hours at room temperature in the presence of vehicle (1% DMSO) or Umeclidinium bromide (0.03-300 nM). Atropine is used as a reference agent. Reactions are terminated by rapid filtration through GF/C filters (glass microfiber binder free 1.2 μ). Membranes are washed with ice-cold 50 mM HEPES and transferred to scintillation vials. Radioactivity is counted in a Scintillation Counter. Reactions are terminated by rapid filtration. Data are obtained from three independent experiments. Specific binding is determined by subtracting nonspecific binding (using 0.3 μM atropine) from total binding. The inhibition constant (Ki) for Umeclidinium bromide is calculated. Membranes containing M3 mAChRs are also incubated for 2 hours at room temperature with increasing concentrations of [3H]-N-methyl scopolamine (0.08-9.24 nM) in the presence or absence of Umeclidinium bromide (0.2-0.5 nM) in 50 mM HEPES, pH 7.4. Nonspecific binding is determined using 10 μM atropine. The saturation data are converted to a scatchard plot for analysis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
Age-matched male BALB/c mice (23-25 gm) are pretreated intranasally (50 μL per mouse) with vehicle (0.9% saline) or Umeclidinium bromide at intervals (0.25-48 hours) prior to methacholine challenge, and placed into individual plethysmograph chambers. Fresh air is supplied by bias flow pumps to the chambers. After baseline respiratory [enhanced pause (Penh)] values are collected, the mice received methacholine (30 mg/mL or EC80) by aerosol delivery (flow=1.6 mL/min×2 minutes). An average Penh is then calculated for 5 minutes. Penh=[(expiratory time/relaxation time)−1]×(peak expiratory flow/peak inspiratory flow), and relaxation time is the amount of time required for 70% of the tidal volume to expire. In some cases, animals are treated on multiple, consecutive days as described in the figure legends. The data are expressed as the mean±S.E.M. percent inhibition of Penh or (mean Penh value of vehicle treated group-Penh for each drug-treated animal) divided by (mean Penh value of vehicle treated group)×100%. Data are analyzed using commercially available software.

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

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9666 mL 9.8330 mL 19.6661 mL 49.1652 mL
5 mM 0.3933 mL 1.9666 mL 3.9332 mL 9.8330 mL
10 mM 0.1967 mL 0.9833 mL 1.9666 mL 4.9165 mL
15 mM 0.1311 mL 0.6555 mL 1.3111 mL 3.2777 mL
20 mM 0.0983 mL 0.4917 mL 0.9833 mL 2.4583 mL
25 mM 0.0787 mL 0.3933 mL 0.7866 mL 1.9666 mL
30 mM 0.0656 mL 0.3278 mL 0.6555 mL 1.6388 mL
40 mM 0.0492 mL 0.2458 mL 0.4917 mL 1.2291 mL
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Umeclidinium bromide Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Umeclidinium869113-09-7GSK573719AmAChRMuscarinic acetylcholine receptorInhibitorinhibitorinhibit

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