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GSK233705

Catalog No. T31207 CAS 850607-58-8

Synonyms: Darotropium bromide, GSK 233705, GSK-233705B, GSK233705, GSK233705B, GSK-233705, GSK 233705B

GSK233705 (Darotropium bromide) is a muscarinic receptor antagonist used in conjunction with the prevention and treatment of chronic obstructive pulmonary disease (COPD) and asthma in humans.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

GSK233705, CAS 850607-58-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 130.00
5 mg	In stock	$ 320.00
10 mg	In stock	$ 480.00
25 mg	In stock	$ 786.00
50 mg	In stock	$ 1,080.00
100 mg	In stock	$ 1,480.00
500 mg	In stock	$ 2,960.00

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Purity: 99.76%

ee: 100%

Purity: 99.67%

ee: 100%

Biological Description

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Storage & Solubility Information

Description

GSK233705 (Darotropium bromide) is a muscarinic receptor antagonist used in conjunction with the prevention and treatment of chronic obstructive pulmonary disease (COPD) and asthma in humans.

In vivo

Patients were randomized to receive 12.5 µg, 25 µg, 50 µg, 100 µg or 200 µg of GSK233705 or placebo once daily for 28 days. The primary endpoint was a change from baseline in trough forced expiratory volume in 1 s (FEV(1)) on day 29. RESULTS: The intent-to-treat population consisted of 576 patients (mean predicted FEV(1) 51%; mean age 62 years). Treatment with GSK233705 produced statistically significant improvements in pulmonary function compared with placebo. Only the 200 µg dose exceeded the predefined target threshold of 130-mL difference compared with placebo for the primary endpoint of change from baseline in trough FEV(1) on day 29. No clear pattern of dose-response was observed for the other doses. Serial FEV(1) (0-24 h) showed a peak effect around 2 h postdose and tended to decline to clinically insignificant levels compared with placebo at 23 and 24 h. Each dose of GSK233705 was well tolerated. The incidence of adverse events was low and similar across all treatment groups. There were no clinically significant effects on laboratory parameters, vital signs, or electrocardiograms. CONCLUSION: All doses of GSK233705 demonstrated bronchodilatory activity and were well tolerated. Although the onset of bronchodilation was rapid, it was not sustained over 24 h making it unsuitable for once-daily dosing.[2]

Synonyms	Darotropium bromide, GSK 233705, GSK-233705B, GSK233705, GSK233705B, GSK-233705, GSK 233705B
Molecular Weight	425.4
Formula	C24H29BrN2
CAS No.	850607-58-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Beier J, et al. Safety and efficacy of dual therapy with GSK233705 and salmeterol versus monotherapy with salmeterol, tiotropium, or placebo in a crossover pilot study in partially reversible COPD patients. Int J Chron Obstruct Pulmon Dis. 2012;7:153-64. 2. Bateman E, et al. Efficacy and safety of the long-acting muscarinic antagonist GSK233705 delivered once daily in patients with COPD. Clin Respir J. 2012 Oct;6(4):248-57. 3. Cazzola M, et al. Novel long-acting bronchodilators for COPD and asthma. Br J Pharmacol. 2008 Oct;155(3):291-9.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Drug Repurposing Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

GSK233705 850607-58-8 Neuroscience AChR Darotropium bromide GSK 233705 GSK-233705B GSK233705B GSK-233705 GSK 233705B Darotropium Bromide inhibitor inhibit

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