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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Neuronal Signal Pathway > Aclidinium BromideCAS：320345-99-1
Molecular Formula：C26H30NO4S2·Br
Molecular Weight：564.55
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Solid
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| CAS | 320345-99-1 |
| Name | Aclidinium Bromide |
| Molecular Formula | C26H30NO4S2·Br |
| Molecular Weight | 564.55 |
| Solubility | Soluble in DMSO ≥5mg/mL |
| Purity | ≥98% |
| Appearance | Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 825-171-6 |
| MDL | MFCD09954105 |
| SMILES | O=C(O[C@H]1C[N+]2(CCCOC3=CC=CC=C3)CCC1CC2)C(C4=CC=CS4)(O)C5=CC=CS5.[Br-] |
| Target Point | mAChR |
| Passage | Neuronal Signaling;GPCR & G Protein |
| Background | Aclidinium Bromide is a long-acting muscarinic antagonist that potently inhibits human muscarinic AChRs M1, M4, M3, and M5. |
| Biological Activity | Aclidinium Bromide (LAS 34273, LAS-W 330)与人源毒蕈碱受体AChR M1， M2， M3， M4和M5结合，Ki值分别为0.1 nM， 0.14 nM， 0.14 nM， 0.21 nM和0.16 nM。[1-3] |
| In Vitro | [3H]Aclidinium与M2的同质受体结合，Kd为0.34 nM，Bmax为3.13 pmol/mg，与M3结合，Kd为0.34 nM，Bmax为3.13 pmol/mg。 Aclidinium(< 100 nM)剂量依赖性抑制乙酰胆碱诱导的离体豚鼠气管的收缩。在离体的豚鼠气管中，Aclidinium显示出起始作用，t1/2为6.8分钟，tmax为35.9分钟。[1] Aclidinium在所有物种的血浆样品中是水解的，37℃下，在大鼠，豚鼠，狗和人的血浆中，表观半衰期分别为11.7 分钟，38.3 分钟，1.8 分钟和2.4 分钟。[2] 在人肺成纤维细胞中，Aclidinium预处理防止M1和M3的上调，但不影响乙酰胆碱或TGF-β1诱导的M2下调。在人肺成纤维细胞中，Aclidinium(0.1 μM)剂量依赖性抑制TGF-β1和乙酰胆碱诱导的细胞增殖。[3] |
| In Vivo | 在麻醉的豚鼠体内，乙酰胆碱诱导的支气管收缩模型中，Aclidinium显示出起始作用，IC50(95% CI)为140微克/毫升，tmax为30分钟。[1]在麻醉的豚鼠体内，超过120分钟的研究期间，Aclidinium(1 毫克/毫升)产生一个有效持久的气管保护作用(72%–88.4%)。[2] |
| Cell Experiment | Animal Models: 比格犬; Dosages: 500微克/千克; Administration: 通过喷雾器给药; 在有意识的比格犬体内，Aclidinium(500 微克/千克)给药1小时后诱导心率最大增加55%。[1] |
| Animal Experiment | Cell lines: 人支气管成纤维细胞; Concentrations: 100 nM; Incubation Time: 48小时; 在人支气管成纤维细胞中，Aclidinium(0.1 μM)抑制乙酰胆碱和TGF-β1诱导的Ⅰ型胶原上调，并抑制α-SMA mRNA和蛋白质表达;Aclidinium(0.1 μM)抑制TGF-β1诱导的ChAT表达上调;Aclidinium(0.1 μM)抑制乙酰胆碱和TGF-β1诱导的ERK1/2磷酸化作用和RhoA-GTP形成的增加。[3] |
| Kinase Experiment | [3H]NMS 与表达人毒蕈碱受体亚型之一的细胞膜制剂结合，Aclidinium对不同人毒蕈碱受体亚型在平衡时的亲和力，通过其置换[3H]NMS的能力测定。对M1，M2，M3，M4，和M5受体膜制剂的蛋白质浓度分别为8.1微克/孔，10.0微克/孔，4.9微克/孔，4.5微克/孔，以及5.0微克/孔。对不同毒蕈碱受体亚型，这些测试在[3H]NMS浓度近似等于放射性配体解离常数(Kd)下进行。[3H]NMS的浓度，对M1和M4的测试为0.3 nM，对M2，M3，和M5的测试为1 nM。重复测定两份一系列拮抗剂浓度(10 14到10 5 M)以得到竞争曲线。非特异性结合在阿托品(1 μM)存在下测定。试验试剂溶解在测试结合缓冲液中(含有钙和镁的磷酸盐缓冲盐溶液)，总体积为200微升。室温下在96孔微量滴定板中培育2小时或6小时(M1–M4和 M5，分别)，以确保达到平衡，将150微升等份反应液转移到GF/C滤板，用含有0.05%聚乙烯亚胺的清洗缓冲液(50 mM Tris，100 mM NaCl，pH 7.4)预处理1小时。结合的和游离的[3H]NMS通过快速真空过滤分离，随后用冰预冷的清洗缓冲液清洗4次。[1] |
| Data Literature Source | [1] Gavald A，et al. J Pharmacol Exp Ther，2009，331(2)，740-751. [2] Sentellas S，et al. Eur J Pharm Sci，2010，39(5)，283-290. [3] Milara J，et al. Thorax，2012，67(3)，229-237. |
| Unit | Bottle |
| Specification | 2mg 5mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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