Alvimopan dihydrate

μ-opioid receptor antagonist,peripherally acting CAS# 170098-38-1

Alvimopan dihydrate

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Chemical structure

Alvimopan dihydrate

3D structure

Chemical Properties of Alvimopan dihydrate

Cas No. 170098-38-1 SDF Download SDF
PubChem ID 5488547 Appearance Powder
Formula C25H36N2O6 M.Wt 460.56
Type of Compound N/A Storage Desiccate at -20°C
Synonyms LY 246736 dihydrate; ADL 8-2698 dihydrate
Solubility DMSO : 33.33 mg/mL (72.37 mM; Need ultrasonic)
Chemical Name 2-[[(2S)-2-benzyl-3-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]propanoyl]amino]acetic acid;dihydrate
SMILES CC1CN(CCC1(C)C2=CC(=CC=C2)O)CC(CC3=CC=CC=C3)C(=O)NCC(=O)O.O.O
Standard InChIKey USPVLEIQIUNQGE-DBFLIVQGSA-N
Standard InChI InChI=1S/C25H32N2O4.2H2O/c1-18-16-27(12-11-25(18,2)21-9-6-10-22(28)14-21)17-20(24(31)26-15-23(29)30)13-19-7-4-3-5-8-19;;/h3-10,14,18,20,28H,11-13,15-17H2,1-2H3,(H,26,31)(H,29,30);2*1H2/t18-,20-,25+;;/m0../s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Alvimopan dihydrate

DescriptionAlvimopan dihydrate(LY 246736; ADL 8-2698) 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

References:
[1]. NCBI BioAssay: 325959 [2]. Cassel JA, et al. [(3)H]Alvimopan binding to the micro opioid receptor: comparative binding kinetics of opioid antagonists. Eur J Pharmacol. 2005 Sep 27;520(1-3):29-36. [3]. Viscusi ER, et al. Alvimopan, a peripherally acting mu-opioid receptor antagonist, compared with placebo in postoperative ileus after major abdominal surgery: results of a randomized, double-blind, controlled study. Surg Endosc. 2006 Jan;20(1):64-70. [4]. Fukuda H, et al. The selective mu opioid receptor antagonist, alvimopan, improves delayed GI transit of postoperative ileus in rats. Brain Res. 2006 Aug 2;1102(1):63-70. [5]. Delaney CP, et al. Phase III trial of alvimopan, a novel, peripherally acting, mu opioid antagonist, for postoperative ileus after major abdominal surgery. Dis Colon Rectum. 2005 Jun;48(6):1114-25; discussion 1125-6; author reply 1127-9.

Alvimopan dihydrate Dilution Calculator

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Alvimopan dihydrate Molarity Calculator

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Preparing Stock Solutions of Alvimopan dihydrate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.1713 mL 10.8563 mL 21.7127 mL 43.4254 mL 54.2817 mL
5 mM 0.4343 mL 2.1713 mL 4.3425 mL 8.6851 mL 10.8563 mL
10 mM 0.2171 mL 1.0856 mL 2.1713 mL 4.3425 mL 5.4282 mL
50 mM 0.0434 mL 0.2171 mL 0.4343 mL 0.8685 mL 1.0856 mL
100 mM 0.0217 mL 0.1086 mL 0.2171 mL 0.4343 mL 0.5428 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Alvimopan dihydrate

Alvimopan dihydrate is a selective antagonist of opioid receptor with IC50 value of 1.7 nM.
Opioid receptor is a G protein-coupled receptor with opioids as ligands.
The dissociation rate of alvimopan from the micro opioid receptor (t(1/2)=30-44 min) was slower than those of the antagonists N-methylnaltrexone (t(1/2)=0.46 min) and naloxone (t(1/2)=0.82 min), and was similar to that of the long acting partial agonist buprenorphine (t(1/2)=44 min). When preincubation with the micro opioid receptor, the affinity and potency of alvimopan increased apparently, which is consistent with its long duration of action [1].
Patients with opioid induced bowel dysfunction (OBD) orally received alvimopan 0.5 mg twice daily (BID), 1 mg once daily (QD), 1 mg BID, or placebo for 6 weeks. Alvimopan significantly increased spontaneous bowel movements (SBMs) frequency each week in the last three weeks with alvimopan 0.5 mg BID (+1.71 mean SBMs/week), alvimopan 1 mg QD (+1.64) and alvimopan 1 mg BID (+2.52), respectively. While, Alvimopan caused side effects such as abdominal pain, nausea, and diarrhea, which was the same as the placebo. Alvimopan restored GI function and relieved OBD without affecting analgesia [2].
References:
[1]. Cassel JA, Daubert JD, DeHaven RN. [(3)H]Alvimopan binding to the micro opioid receptor: comparative binding kinetics of opioid antagonists. Eur J Pharmacol, 2005, 520(1-3): 29-36.
[2]. Webster L, Jansen JP, Peppin J, et al. Alvimopan, a peripherally acting mu-opioid receptor (PAM-OR) antagonist for the treatment of opioid-induced bowel dysfunction: results from a randomized, double-blind, placebo-controlled, dose-finding study in subjects taking opioids for chronic non-cancer pain. Pain, 2008, 137(2): 428-440.

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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.

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