Alvimopan-d5

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白、同位素标记物，专注于信号通路和疾病研究领域。
Alvimopan-d5 

Alvimopan-d5 是 Alvimopan 的氘代物。Alvimopan (ADL 8-2698) 是一种有效，选择性，具有口服活性和可逆的 μ-阿片受体 (μ-opioid receptor) 拮抗剂，IC50 值为 1.7 nM。Alvimopan 对 μ-阿片受体 (Ki=0.47 nM) 的选择性高于 κ- (Ki=100 nM) 和 δ-阿片受体 (Ki=12 nM)。Alvimopan 可用于术后肠梗阻的研究。

Alvimopan-d5

Alvimopan-d5 Chemical Structure

CAS No. : 1217616-62-0

规格 是否有货
1 mg Check price and availability
10 mg Check price and availability

* Please select Quantity before adding items.

生物活性

Alvimopan-d5 is the deuterium labeled Alvimopan. Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus[1][2][3].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

429.56

Formula

C25H27D5N2O4
CAS 号

1217616-62-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Bourdonnec BL, et, al. Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2006-12.

    [3]. Erowele GI, et, al. Alvimopan (Entereg), a Peripherally Acting mu-Opioid Receptor Antagonist For Postoperative Ileus. P T. 2008 Oct;33(10):574-83.

    [4]. Meerveld BG, et, al. Preclinical studies of opioids and opioid antagonists on gastrointestinal function. Neurogastroenterol Motil. 2004 Oct;16 Suppl 2:46-53.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务