Zamifenacinfumarate

生物活性靶点体内研究 Zamifenacinfumarate 试剂级价格

Zamifenacinfumarate

CAS号:127308-98-9
英文名:Zamifenacinfumarate
中文名:Zamifenacinfumarate
CBNumber:CB81075168
分子式:C31H33NO7
分子量:531.61
MOL File:127308-98-9.mol

Zamifenacinfumarate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性质、用途与生产工艺

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).