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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].
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $52 | 5 days |
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]. |
Molecular Weight | 460.56 |
Formula | C25H36N2O6 |
Cas No. | 170098-38-1 |
Relative Density. | 1.166g/cm3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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