Alvimopan dihydrate|170098-38-1|(爱维莫潘; ADL 8-2698 dihydrate; LY 246736 dihydrate)-陌孚医药/Medlife

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Alvimopan dihydrate (Synonyms: 爱维莫潘; ADL 8-2698 dihydrate; LY 246736 dihydrate)

目录号: PL08036 纯度: ≥98%

CAS No. :170098-38-1

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中文名称	Alvimopan dihydrate
中文别名	爱维莫潘二水合物;Ly 246736 二水合物;爱维莫潘;爱维莫潘杂质
英文名称	Alvimopan dihydrate
英文别名	Glycine,N-[(2S)-2-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-phenylpropyl]-,hydrate (1:2);2-[[(2S)-2-benzyl-3-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperi dyl]propanoyl]amino]acetic acid dihydrate;2-[[(2S)-2-benzyl-3-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]propanoyl]amino]acetic acid,dihydrate;Alvimopan dihydrate;Glycine,N-[(2S)-2-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-phe...;LY 246736 dihydrate;LY-246736;Adl 8-2698;ADL 8-2698 dihydrate;Alvimopan (USAN);Alvimopan anhydrous;Alvimopan hydrate;Entereg;UNII-677C126AET;N-[(2S)-2-[[(3R,4R)-4-(3-Hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-phenylpropyl]glycine dihydrate;Alvimopan 2H2O;AlviMopan(ADL-8-2698,LY-246736);156053-89-3 (Anhydrous);Alvimopan dihydrate, >=99%;Alvimopan (dihydrate);Alvimopan [USAN];677C126AET;(((2S)-2-(((3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl)methyl)-3-phenylpropanoyl)amino)acetic a
Cas No.	170098-38-1
分子式	C₂₅H₃₆N₂O₆
分子量	460.56
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Alvimopan dihydrate (ADL 8-2698 dihydrate) 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 dehydrate 对 μ-阿片受体 (K_i=0.47 nM) 的选择性高于 κ- (K_i=100 nM) 和 δ-阿片受体 (K_i=12 nM)。Alvimopan dehydrate 可用于术后肠梗阻的研究。

生物活性

Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC 50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioid receptor (K i =0.47 nM) over κ- and δ-opioid receptors (K i s=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus.

性状

Solid

IC50 & Target[1][2]

IC50: 1.7 nM (μ-opioid receptor)

体外研究(In Vitro)

Alvimopan inhibits the loperamide-stimulated [S]GTPγS binding to membranes containing the cloned human μ-opioid receptor, with an IC50 of 1.7 nM. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Alvimopan (0.1-1.0 mg/kg; p.o.) partially antagonizes the slowing of small intestinal transit of Sn-labelled microspheres produced by morphine in rats.
Alvimopan (3 mg/kg; p.o.) has no effect on the visceromotor behavioural responses (VMR) induced by noxious colorectal distension (CRD) in conscious rats. 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

ClinicalTrial

参考文献

[1]. 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.
[2]. Erowele GI, et, al. Alvimopan (Entereg), a Peripherally Acting mu-Opioid Receptor Antagonist For Postoperative Ileus. P T. 2008 Oct;33(10):574-83.

溶解度数据	In Vitro: DMSO : 33.33 mg/mL (72.37 mM; Need ultrasonic)配制储备液

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Data Sheet

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。

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