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Umeclidinium bromide (GSK573719A) is a novel mAChR antagonist.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $34 | In Stock | In Stock | |
| 2 mg | $48 | In Stock | In Stock | |
| 5 mg | $77 | In Stock | In Stock | |
| 10 mg | $126 | In Stock | In Stock | |
| 25 mg | $223 | In Stock | In Stock | |
| 50 mg | $369 | In Stock | In Stock | |
| 100 mg | $553 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $89 | In Stock | In Stock |
| Description | Umeclidinium bromide (GSK573719A) is a novel mAChR antagonist. |
| Targets&IC50 | M2 mAChR:0.15 nM(Ki), M4 mAChR:0.05 nM(Ki), M3 mAChR:0.06 nM(Ki), M1 mAChR:0.16 nM(Ki), M5 mAChR:0.13 nM(Ki) |
| 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). |
| In vivo | Administering Umeclidinium bromide (GSK573719A) intranasally at a dose of 0.025 μg to mice once daily for five days incrementally enhances its inhibitory effect on bronchomotor tone, with inhibition increasing from 35% after the first dose to 60% by the fifth day. Following a five-day rest period, where bronchomotor tone reverts to baseline, a subsequent dose yields an inhibition level comparable to that of the initial dose, indicating the absence of tolerance development with repeated intranasal administration. Conversely, oral administration of Umeclidinium bromide at 2.0 mg/kg, equivalent to 100 times the intranasal ED50 value, fails to offer any protective effect against an Mch challenge, demonstrating the method-specific efficacy of this compound. |
| Animal Research | Mice: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. |
| Synonyms | GSK573719A |
| Molecular Weight | 508.49 |
| Formula | C29H34BrNO2 |
| Cas No. | 869113-09-7 |
| Smiles | [Br-].OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 |
| Relative Density. | no data available |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 34 mg/mL (66.86 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Saline: 2 mg/mL (3.93 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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