Zamifenacin

(Synonyms: UK-76654)
目录号: PL06827 纯度: ≥99%
Zamifenacin (UK-76654) 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。
CAS No. :127308-82-1
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中文名称
Zamifenacin
中文别名
扎非那新
英文名称
Zamifenacin
英文别名
(R)-3-(Benzhydryloxy)-1-(2-(benzo[d][1,3]dioxol-5-yl)ethyl)piperidine;(3R)-3-benzhydryloxy-1-[2-(1,3-benzodioxol-5-yl)ethyl]piperidine;Piperidine,1-[2-(1,3-benzodioxol-5-yl)ethyl]-3-(diphenylmethoxy)-, (3R)-;ZAMIFENACIN;Zamifenacin
Cas No.
127308-82-1
分子式
C27H29NO3
分子量
415.52
包装储存
Powder -20°C 3 years;4°C 2 years
详情描述
Zamifenacin (UK-76654) 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。
产品详情
Zamifenacin (UK-76654) 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。
生物活性
Zamifenacin (UK-76654) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome.
性状
Solid
IC50 & Target[1][2]
Muscarinic M3 receptor
体内研究(In Vivo)
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). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Houghton LA, et al. Zamifenacin (UK-76, 654) a potent gut M3 selective muscarinic antagonist, reduces colonic motor activity in patients with irritable bowel syndrome. Aliment Pharmacol Ther. 1997 Jun;11(3):561-8.
[2]. Beaumont KC, et al. Pharmacokinetics and metabolism of Zamifenacin in mouse, rat, dog and man. Xenobiotica. 1996 Apr;26(4):459-71.
溶解度数据
In Vitro: DMSO : 100 mg/mL (240.66 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)
[1]. Houghton LA, et al. Zamifenacin (UK-76, 654) a potent gut M3 selective muscarinic antagonist, reduces colonic motor activity in patients with irritable bowel syndrome. Aliment Pharmacol Ther. 1997 Jun;11(3):561-8.
[2]. Beaumont KC, et al. Pharmacokinetics and metabolism of Zamifenacin in mouse, rat, dog and man. Xenobiotica. 1996 Apr;26(4):459-71.

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2