Darotropium bromide
Darotropium bromide (GSK233705), a long-acting muscarinic antagonist and an inhaled anticholinergic, can be used for the research of chronic obstructive pulmonary disease (COPD).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 850607-58-8
- Formule: C24H29BrN2
- Masse moléculaire:425.40
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
<10 nM
Compound: 34
|
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
|
[PMID: 19630384] |
| CHO | IC50 |
<10 nM
Compound: 4a
|
Antagonist activity against human cloned muscarinic M1 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
Antagonist activity against human cloned muscarinic M1 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
|
[PMID: 19616944] |
| CHO | IC50 |
<10 nM
Compound: 4a
|
Antagonist activity against human cloned muscarinic M2 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
Antagonist activity against human cloned muscarinic M2 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
|
[PMID: 19616944] |
| CHO | IC50 |
<10 nM
Compound: 4a
|
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
|
[PMID: 19616944] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 850607-58-8
-
Masse moléculaire 425.40
-
Formule C24H29BrN2
-
SMILES
[H][C@]1(CC(C2=CC=CC=C2)(C#N)C3=CC=CC=C3)C[C@]4([H])[N+](C)(C)[C@@]([H])(CC4)C1.[Br-]
-
Synonyms
GSK233705
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Jutta Beier, 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. [Content Brief]
[2]. Eric Bateman, 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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)