Alvimopan dihydrate (LY246736 dihydrate)
Molecular Weight(MW): 460.56
Alvimopan (LY-246736) is a potent, relatively nonselective opioid antagonist with Ki values of 0.77, 4.4, and 40 nM for the μ, δ, and κ opioid receptors, respectively, displaying >100-fold selectivity over other aminergic G-protein-coupled receptors.
Purity & Quality Control
Choose Selective Opioid Receptor Inhibitors
|Description||Alvimopan (LY-246736) is a potent, relatively nonselective opioid antagonist with Ki values of 0.77, 4.4, and 40 nM for the μ, δ, and κ opioid receptors, respectively, displaying >100-fold selectivity over other aminergic G-protein-coupled receptors.|
Alvimopan is highly selective (by ≥227-fold) for the human μ receptor over the κ subtype, but has a more modest (≥6-fold) μ/δ receptor selectivity. In the guinea pig isolated ileum, alvimopan is a potent antagonist of morphine, DAMGO or endomorphin-1-induced, and μ opioid receptor-mediated, inhibition of electrically-evoked contractions (pA2 values of 9.6 or 9.7). The δ and κ antagonist potencies of alvimopan are lower in the guinea pig ileum (pA2 values of 8.7 and 7.8, respectively). Alvimopan (1 or 10 μM) has no significant affinity for a broad range of non-opioid receptors, ion channels and enzymes at which it has been tested.
|In vivo||In animals, alvimopan antagonizes centrally mediated, morphine-induced analgesia only at relatively high doses, with very high plasma concentrations needed to cross the blood-brain barrier. After intravenous administration, alvimopan is approximately 200-times more potent at blocking peripheral verses central μ-receptors. After oral administration, alvimopan is also highly active. In dogs, intravenous administration of alvimopan provided dose-dependent increases in peak plasma concentrations and plasma area under the concentration-time curve. However, as a result of poor systemic absorption, oral doses up to 100 mg/kg produced low plasma concentrations (mean Cmax =92.9 ng/ml), which resulted in an oral bioavailability of approximately 0.03%. The half-life of alvimopan is estimated to be approximately 10 min after intravenous administration in dogs and rabbits.|
|In vitro||DMSO||92 mg/mL (199.75 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.