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Alvimopan dihydrate (LY246736 dihydrate)

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Catalog No. T22238Cas No. 170098-38-1

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

Alvimopan dihydrate (LY246736 dihydrate)

Alvimopan dihydrate (LY246736 dihydrate)

😃Good
Catalog No. T22238Cas No. 170098-38-1
Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active, and reversible μ-opioid receptor antagonist with an IC50 of 1.7 nM. Highly selective for the μ-opioid receptor (Ki = 0.47 nM) over κ- and δ-opioid receptors (Kis = 100 and 12 nM, respectively), Alvimopan dihydrate can be used for research on postoperative ileus [1] [2] [3].
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Product Introduction

Bioactivity
Description
Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active, and reversible μ-opioid receptor antagonist with an IC50 of 1.7 nM. Highly selective for the μ-opioid receptor (Ki = 0.47 nM) over κ- and δ-opioid receptors (Kis = 100 and 12 nM, respectively), Alvimopan dihydrate can be used for research on postoperative ileus [1] [2] [3].
In vitro
Alvimopan inhibits the binding of loperamide-stimulated [35 S]GTPγS to membranes containing the cloned human μ-opioid receptor with an IC 50 of 1.7 nM [1].
In vivo
Alvimopan (0.1-1.0 mg/kg; p.o.) partially antagonizes the morphine-induced slowing of small intestinal transit of ^113Sn-labelled microspheres in rats, whereas Alvimopan (3 mg/kg; p.o.) has no effect on noxious colorectal distension (CRD)-induced visceromotor behavioral responses (VMR) in conscious rats [3].
Chemical Properties
Molecular Weight460.56
FormulaC25H36N2O6
Cas No.170098-38-1
Relative Density.1.166g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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