1. GPCR/G Protein
    Neuronal Signaling
  2. Opioid Receptor
  3. Alvimopan dihydrate

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

Cat. No.: HY-76657A Purity: 98.02%
Handling Instructions

Alvimopan dihydrate (ADL 8-2698 dihydrate) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.

For research use only. We do not sell to patients.

Alvimopan dihydrate Chemical Structure

Alvimopan dihydrate Chemical Structure

CAS No. : 170098-38-1

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Description

Alvimopan dihydrate (ADL 8-2698 dihydrate) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery. IC50 Value: 1.7 nM (Mu-type opioid receptor) [1] Target: mu-opioid receptor in vitro: The dissociation rate of alvimopan from the micro opioid receptor (t(1/2)=30--44 min) was comparable to that of the long acting partial agonist buprenorphine (t(1/2)=44 min), but was slower than those of the antagonists naloxone (t(1/2)=0.82 min) and N-methylnaltrexone (t(1/2)=0.46 min) [2]. in vivo: Alvimopan did not significantly accelerate GI-3 compared with placebo [6 mg: hazard ratio (HR) = 1.20, p = 0.080; 12 mg: HR = 1.24, p = 0.038). However, after adjustment for significant covariates (sex/surgical duration), benefits were significant for both doses (6 mg: HR = 1.24, p = 0.037; 12 mg: HR = 1.26, p = 0.028). Alvimopan also significantly accelerated time to GI-2 (6 mg: HR = 1.37, p = 0.008; 12 mg: HR = 1.33, p = 0.018) and DCO (6 mg: HR = 1.31, p = 0.008; 12 mg: HR = 1.28, p = 0.015) [3]. Alvimopan (1 and 3 mg/kg) significantly reversed this delayed GI transit when administered 45 min prior to surgery. However, the effects of alvimopan were less pronounced when administered following surgery [4]. Toxicity:The most common treatment-emergent adverse events across all treatment groups were nausea, vomiting, and hypotension; the incidence of nausea and vomiting was reduced by 53 percent in thealvimopan 12-mg group [5]. Clinical trial: Intercostal Nerve Block With Liposome Bupivacaine in Subjects Undergoing Posterolateral Thoracotomy. Phase 3

Clinical Trial
Molecular Weight

460.56

Formula

C₂₅H₃₆N₂O₆

CAS No.

170098-38-1

SMILES

OC1=CC=CC([[email protected]@]2(C)[[email protected]@H](C)CN(C[[email protected]](CC3=CC=CC=C3)C(NCC(O)=O)=O)CC2)=C1.O.O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (72.37 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1713 mL 10.8563 mL 21.7127 mL
5 mM 0.4343 mL 2.1713 mL 4.3425 mL
10 mM 0.2171 mL 1.0856 mL 2.1713 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

Alvimopan dihydrateADL 8-2698 dihydrateLY 246736 dihydrateOpioid ReceptorInhibitorinhibitorinhibit

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Alvimopan dihydrate
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