Zamifenacin fumarate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Zamifenacin fumarate 是一种有效的肠道选择性毒蕈碱 M3 受体拮抗剂。

Zamifenacin fumarate is a potent and gut-selective antagonist of muscarinic M3 receptor.(In Vivo):In male CDl mice, male and female CD rats and male and two female beagle dogs, Zamifenacin(mouse 5.3, rat 5.0 and, dog 1.0 mg/kg) exhibited 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). Zamifenacin(mouse 13.2, rat 20 and dog 5 mg/kg) exhibited moderate oral bioavailability (mouse 26%, rat 64%, dog 100%) and Cmax (mouse 92, rat 905, dog 416 ng/mL).

——

Zamifenacin exhibits moderate oral bioavailability (mouse 26%, rat 64%, dog 100%) and Cmax (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%), Cmax (92 ng/mL), T1/2 (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%), Cmax (905 ng/mL), T1/2 (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%), Cmax (416 ng/mL), T1/2 (1.1 h).

UK-76654 fumarate

Cell Cycle/DNA Damage

AChR

Cytochrome P450

——

——

127308-98-9

531.605

C31H33NO7

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (188.11 mM)

OC(=O)\C=C\C(O)=O.C(Cc1ccc2OCOc2c1)N1CCC[C@H](C1)OC(c1ccccc1)c1ccccc1

——

(-20℃)

With Ice Pack

≥ 2 years