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).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 850607-58-8
- 分子式: C24H29BrN2
- 分子量:425.40
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
|
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 |
化学情報
-
CAS 番号 850607-58-8
-
分子量 425.40
-
分子式 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-]
-
別名
GSK233705
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)