Alvimopan monohydrate
Based on 2 publication(s) in Google Scholar
Alvimopan monohydrate (ADL 8-2698 monohydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan monohydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan monohydrate can be used for the research of postoperative ileus.
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- CAS No.: 1383577-62-5
- Formule: C25H34N2O5
- Masse moléculaire:442.55
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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HY-13243
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DAMGOμ-OPR Agonist -
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LY2795050κ(kappa)-opioid Receptor (KOR) Antagonist -
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ADL-5859 hydrochlorideOpioid Receptor Agonist -
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JDTic dihydrochloride -
HY-101202
SNC80δ-opioid Receptor Agonist -
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Norbinaltorphimine dihydrochlorideκ-opioid receptor Antagonist -
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Naloxone hydrochlorideOpioid Receptor Antagonist -
HY-13274
JTC-801Opioid Receptor Antagonist
Publications Citing Use of MedChemExpress (MCE) Alvimopan monohydrate
MoreVoir tous les produits spécifiques à Isoform Opioid Receptor
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Activité biologique
Description
IC50 & Target
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μ Opioid Receptor/MOR |
In Vitro
Alvimopan inhibits the loperamide-stimulated [35S]GTPγS binding to membranes containing the cloned human μ-opioid receptor, with an IC50 of 1.7 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Alvimopan (3 mg/kg; p.o.) has no effect on the visceromotor behavioural responses (VMR) induced by noxious colorectal distension (CRD) in conscious rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1383577-62-5
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Appearance Solid
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Masse moléculaire 442.55
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Formule C25H34N2O5
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Color White to off-white
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SMILES
OC1=CC=CC([C@@]2(C)[C@@H](C)CN(C[C@H](CC3=CC=CC=C3)C(NCC(O)=O)=O)CC2)=C1.O
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Synonyms
ADL 8-2698 monohydrate; LY 246736 monohydrate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
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Fiche technique (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[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. [Content Brief]
[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. [Content Brief]
[3]. Meerveld BG, et, al. Preclinical studies of opioids and opioid antagonists on gastrointestinal function. Neurogastroenterol Motil. 2004 Oct;16 Suppl 2:46-53. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Alvimopan monohydrate Related Classifications
HY-76657 Related Classifications
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