127308-98-9
中文名称
Zamifenacinfumarate
英文名称
Zamifenacinfumarate
CAS
127308-98-9
分子式
C27H29NO3.C4H4O4
分子量
531.602
MOL 文件
127308-98-9.mol
127308-98-9 结构式
基本信息
中文别名
扎非那星富马酸盐 英文别名
UK-76654 fumarateZamifenacinfumarate
(3R)-1-[2-(1-,3-Benzodioxol-5-yl)ethyl]-3-(diphenylmethoxy)piperidinefumarate
物理化学性质
储存条件Inert atmosphere,2-8°C
溶解度Soluble to 100 mM in DMSO and to 25 mM in ethanol
形态Powder
颜色White to off-white
Zamifenacinfumarate价格(试剂级)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2024/11/08 | HY-107649 | Zamifenacinfumarate Zamifenacin fumarate | 127308-98-9 | 5mg | 1000元 |
| 2024/11/08 | HY-107649 | Zamifenacinfumarate Zamifenacin fumarate | 127308-98-9 | 10mM * 1mLin DMSO | 1170元 |
| 2024/11/08 | HY-107649 | Zamifenacinfumarate Zamifenacin fumarate | 127308-98-9 | 10mg | 1500元 |
常见问题列表
生物活性
Zamifenacin fumarate (UK-76654 fumarate) 是一种有效的肠道选择性毒蕈碱 M3 受体拮抗剂。Zamifenacin 可显着降低肠易激综合症的结肠蠕动。靶点
Muscarinic M3 receptor
体内研究
Zamifenacin exhibits moderate oral bioavailability (mouse 26%, rat 64%, dog 100%) and C
max
(mouse 92, rat 905, dog 416 ng/mL) following oral administration (mouse 13.2, rat 20 and, dog 5 mg/kg).
Zamifenacin exhibits terminal elimination half-lives (mouse 2.1, rat 6.0 and, dog 1.1 h) due to high plasma clearance (68, 35, and 39 mL/min/kg respectively combined with large volumes of distribution (12.5, 19.0, and 3.5 L/kg respectively) following intravenous administration (mouse 5.3, rat 5.0 and, dog 1.0 mg/kg).
| Animal Model: | Male CDl mice (mean weight 23 g) |
| Dosage: | 5.3 mg/kg for i.v.; 13.2 mg/kg for oral (Pharmacokinetic Analysis) |
| Administration: | Intravenous administration and oral administration |
| Result: | Oral bioavailability (26%), C max (92 ng/mL), T 1/2 (1.1 h). |
| Animal Model: | Male and female CD rats (mean weight 210 g) |
| Dosage: | 5.0 mg/kg for i.v.; 20 mg/kg for oral (Pharmacokinetic Analysis) |
| Administration: | Intravenous administration and oral administration |
| Result: | Oral bioavailability (64%), C max (905 ng/mL), T 1/2 (6.0 h). |
| Animal Model: | Male and two female beagle dogs (13-16 kg) |
| Dosage: | 1.0 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis) |
| Administration: | Intravenous administration and oral administration |
| Result: | Oral bioavailability (100%), C max (416 ng/mL), T 1/2 (1.1 h). |