| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| A409018-1ml |
1ml |
现货  |
|
| 英文别名 | LAS 34273, LAS-W 330 | 1-Azoniabicyclo[2.2.2]octane, 3-[(2-hydroxy-2,2-di-2-thienylacetyl)oxy]-1-(3-phenoxypropyl)-, bromide (1:1), (3R)- |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | Aclidinium Bromide |
| 生化机理 | Aclidinium Bromide（LAS 34273，LAS-W 330）可抑制人毒蕈碱 AChR M1、M2、M3、M4 和 M5，其Ki值分别为 0.1 nM、0.14 nM、0.14 nM、0.21 nM 和 0.16 nM。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 拮抗剂 |
| 作用机制 | 肌卡因乙酰胆碱受体 M3 拮抗剂 |
| 产品介绍 |
Information Aclidinium Bromide (LAS 34273, LAS-W 330) inhibits human muscarinicAChRM1, M2, M3, M4 and M5 withKiof 0.1 nM, 0.14 nM, 0.14 nM, 0.21 nM and 0.16 nM, respectively. [3H]Aclidinium binds to a homogeneous receptor of M2 with Kd of 0.34 nM and Bmax of 3.13 pmol/mg, and binds to M3 with Kd of 0.34 nM and Bmax of 3.13 pmol/mg. Aclidinium (< 100 nM) dose-dependently inhibits carbachol-induced contractions in isolated guinea pig trachea. Aclidinium shows an onset of action with t1/2 of 6.8 min, tmax of 35.9 min in isolated guinea pig trachea. Aclidinium is hydrolysed in plasma samples from all species studied, with apparent half-lives at 37℃ of 11.7 min, 38.3 min, 1.8 min and 2.4 min in rat, guinea pig, dog and human plasma, respectively. Aclidinium (0.1 μM) inhibits carbachol and TGF-β1 induced upregulation of collagen type I and α-SMA mRNA and protein expression in human bronchial fibroblasts. Aclidinium (0.1 μM) inhibits TGF-β1 induced upregulation of ChAT expression in human bronchial fibroblasts. Aclidinium (0.1 μM) inhibits carbachol- and TGF-β1-induced increases in ERK1/2 phosphorylation and RhoA-GTP formation in human bronchial fibroblasts. Aclidinium pretreatment prevents the upregulation of M1 and M3, but not M2 downregulation induced by carbachol or TGF-β1 in human lung fibroblasts. Aclidinium (0.1 μM) dose-dependently inhibits the TGF-β1 and carbachol-induced cell proliferation of human lung fibroblasts. In vivo Aclidinium shows an onset of action with IC50 (95% CI) of 140 μg/mL and tmax of 30 min in the acetylcholine-induced bronchoconstriction model in anesthetized guinea pigs. Aclidinium (500 μg/kg) induces a maximal increase in heart rate of 55% after 1 hour in conscious beagle dogs. Aclidinium (1 mg/ml) produces a potent and sustained bronchoprotection (72%–88.4%) over the 120-min study period in anaesthetised guinea pigs. cell lines： Concentrations：100 nM Incubation Time：48 hours Powder Purity:≥99% |
| Ki Data | M5 mAChR, Ki: 0.16 nM; M4 mAChR, Ki: 0.21 nM; M3 mAChR, Ki: 0.14 nM; M2 mAChR, Ki: 0.14 nM; M1 mAChR, Ki: 0.1 nM |
|---|---|
| ALogP | 0.979 |
| hba_count | 3 |
| Rotatable Bond | 10 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | [Br-].OC(C(=O)OC1C[N+]2(CCCOC3=CC=CC=C3)CCC1CC2)(C4=CC=CS4)C5=CC=CS5 |
| 分子量 | 564.55 |
| Reaxy-Rn | 14488516 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=14488516&ln= |
| 溶解性 | Solubility (25°C) In vitro Water: 59 mg/mL (198.76 mM); DMSO: 30 mg/mL (101.06 mM); Ethanol: Insoluble; |
|---|---|
| DMSO(mg / mL) Max Solubility | 113 |
| DMSO(mM) Max Solubility | 200.16 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 14488516 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=14488516&ln= |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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