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

Cat. No.: HY-13243 Purity: 98.66%: FAQs
Data Sheet SDS COA Handling Instructions

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Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC₅₀ of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (K_i=0.47 nM) over κ- and δ-opioid receptors (K_is=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus.

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

Alvimopan Chemical Structure

CAS No. : 156053-89-3

Size	Price	Stock	Quantity
5 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 480	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 720	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Other Forms of Alvimopan:

Alvimopan dihydrate In-stock
Alvimopan monohydrate Get quote

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Opioid Receptor Isoform Specific Products:

View All Isoforms

μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 1.7 nM (μ-opioid receptor)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK-293T	IC₅₀	0.003 μM Compound: 1	Antagonist activity at recombinant human MOR expressed in HEK293T cells assessed as reduction in DAMGO-induced inhibition of forskolin-stimulated cAMP level preincubated for 15 to 20 mins followed by DAMGO and forskolin addition by GloSensor assay Antagonist activity at recombinant human MOR expressed in HEK293T cells assessed as reduction in DAMGO-induced inhibition of forskolin-stimulated cAMP level preincubated for 15 to 20 mins followed by DAMGO and forskolin addition by GloSensor assay	[PMID: 28726402]

In Vitro

Alvimopan inhibits the loperamide-stimulated [³⁵S]GTPγS binding to membranes containing the cloned human μ-opioid receptor, with an IC₅₀ value of 1.7 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Alvimopan (0.1-1.0 mg/kg; p.o.) partially antagonizes the slowing of small intestinal transit of ¹¹³Sn-labelled microspheres produced by morphine in rats^[3].
Alvimopan (3 mg/kg; p.o.) has no effect on the visceromotor behavioural responses (VMR) induced by noxious colorectal distension (CRD) in conscious rats^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

424.53

Formula

C₂₅H₃₂N₂O₄

CAS No.

156053-89-3

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(CNC([C@@H](CC1=CC=CC=C1)CN2C[C@@H]([C@](C3=CC=CC(O)=C3)(CC2)C)C)=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 : ≥ 100 mg/mL (235.55 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3555 mL	11.7777 mL	23.5555 mL
5 mM	0.4711 mL	2.3555 mL	4.7111 mL
10 mM	0.2356 mL	1.1778 mL	2.3555 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.66%

Select Batch:

Data Sheet (273 KB) SDS (597 KB)

COA (246 KB) HNMR (260 KB) RP-HPLC (274 KB)

Handling Instructions (2659 KB)

References

[1]. Bourdonnec BL, et, al. Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2006-12. [Content Brief]

[2]. Erowele GI, et, al. Alvimopan (Entereg), a Peripherally Acting mu-Opioid Receptor Antagonist For Postoperative Ileus. P T. 2008 Oct;33(10):574-83. [Content Brief]

[3]. Meerveld BG, et, al. Preclinical studies of opioids and opioid antagonists on gastrointestinal function. Neurogastroenterol Motil. 2004 Oct;16 Suppl 2:46-53. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3555 mL	11.7777 mL	23.5555 mL	58.8887 mL
	5 mM	0.4711 mL	2.3555 mL	4.7111 mL	11.7777 mL
	10 mM	0.2356 mL	1.1778 mL	2.3555 mL	5.8889 mL
	15 mM	0.1570 mL	0.7852 mL	1.5704 mL	3.9259 mL
	20 mM	0.1178 mL	0.5889 mL	1.1778 mL	2.9444 mL
	25 mM	0.0942 mL	0.4711 mL	0.9422 mL	2.3555 mL
	30 mM	0.0785 mL	0.3926 mL	0.7852 mL	1.9630 mL
	40 mM	0.0589 mL	0.2944 mL	0.5889 mL	1.4722 mL
	50 mM	0.0471 mL	0.2356 mL	0.4711 mL	1.1778 mL
	60 mM	0.0393 mL	0.1963 mL	0.3926 mL	0.9815 mL
	80 mM	0.0294 mL	0.1472 mL	0.2944 mL	0.7361 mL
	100 mM	0.0236 mL	0.1178 mL	0.2356 mL	0.5889 mL

Alvimopan Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Alvimopan156053-89-3ADL 8-2698 LY 246736LY246736LY 246736LY-246736Opioid Receptorμ-opioidpostoperativeileusInhibitorinhibitorinhibit

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