| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
Purity: ≥98%
| Targets |
Bevenopran targets μ-opioid receptors (MOR) as a peripherally acting antagonist. It selectively inhibits μ-opioid receptors located in the gastrointestinal tract. Bevenopran does not significantly penetrate the central nervous system (CNS), which minimizes centrally mediated side effects such as analgesia, euphoria, or respiratory depression. Its peripheral selectivity makes it a promising candidate for treating opioid-induced constipation (OIC) and opioid-induced bowel dysfunction (OBD) without interfering with opioid analgesia.
|
|---|---|
| ln Vitro |
In vitro, bevenopran is a peripheral μ-opioid receptor antagonist. It selectively binds to μ-opioid receptors, inhibiting their activation by opioid agonists. In cell-based assays, bevenopran treatment results in inhibition of μ-opioid receptor-mediated signaling in cells expressing the receptor. The compound's selectivity for peripheral μ-opioid receptors over central receptors is assessed using binding assays and functional assays.
|
| ln Vivo |
An antagonist of peripheral μ-opioid receptors is bevenopran. Right now, bevinopram is being investigated as a potential treatment for opioid-induced bowel dysfunction (OBD) [1]. When bevinopram is taken at 0.1 mg twice daily and 4 mg daily, in particular, it tends to increase the frequency of bowel movements (BM) [1].
In vivo, bevenopran is currently under investigation for the treatment of opioid-induced bowel dysfunction (OBD). As a peripherally acting μ-opioid receptor antagonist (PAMORA), it blocks μ-opioid receptors in the gastrointestinal tract, reducing opioid-induced constipation without affecting central opioid analgesia. Bevenopran has also been studied for its potential use in the treatment of depression and other mood disorders. Comprehensive in vivo efficacy studies are ongoing. |
| Enzyme Assay |
In vitro receptor binding assays for bevenopran involve measuring its binding affinity to μ-opioid receptors. The receptor is incubated with a radiolabeled ligand and varying concentrations of bevenopran. The displacement of the radiolabeled ligand is measured, and the IC₅₀ or Ki value is calculated. The compound's selectivity for peripheral μ-opioid receptors is assessed by comparing its binding to central and peripheral receptor preparations. These assays confirm the compound's mechanism as a peripherally selective μ-opioid receptor antagonist.
|
| Cell Assay |
In vitro cell-based assays for bevenopran evaluate its effects on μ-opioid receptor signaling. Cells expressing μ-opioid receptors are cultured and treated with bevenopran in the presence or absence of opioid agonists. The compound's inhibition of agonist-induced signaling is assessed by measuring cAMP accumulation or downstream signaling. These assays confirm the compound's functional activity as a μ-opioid receptor antagonist.
|
| Animal Protocol |
In vivo animal experiments for bevenopran have been conducted in models of opioid-induced constipation. Animals are treated with opioids to induce constipation, followed by treatment with bevenopran. The compound's effects on gastrointestinal motility, fecal output, and constipation are assessed. Bevenopran's effects on central opioid analgesia are assessed to confirm its peripheral selectivity. Pharmacokinetic studies are conducted to determine the compound's half-life, clearance, and tissue distribution. Comprehensive in vivo studies are ongoing.
|
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) data for bevenopran are limited. The compound has a molecular weight of 386.44 g/mol and a molecular formula of C₂₀H₂₆N₄O₄. It is a synthetic small molecule. The compound's metabolic stability, half-life, and bioavailability have not been fully characterized. Comprehensive ADME studies are needed.
|
| Toxicity/Toxicokinetics |
The toxicity profile of bevenopran has not been extensively characterized. As a peripherally acting μ-opioid receptor antagonist, it is expected to have a favorable safety profile compared to centrally acting antagonists. However, the compound should be handled with appropriate safety precautions in the laboratory. For research use only, not for human therapeutic use without proper authorization. Comprehensive toxicological studies are needed.
|
| References | |
| Additional Infomation |
Bevinoplan is an aromatic ether. Bevinoplan has been used in trials investigating its use for the treatment of kidney damage and opioid-induced constipation.
Bevenopran (CB-5945) is a peripherally acting μ-opioid receptor antagonist (PAMORA) under investigation for the treatment of opioid-induced bowel dysfunction (OBD). It selectively inhibits μ-opioid receptors in the GI tract without significant CNS penetration. Bevenopran has a molecular formula of C₂₀H₂₆N₄O₄ and a molecular weight of 386.44 g/mol. It has also been studied for depression and mood disorders. Bevenopran has not yet received regulatory approval. |
| Molecular Formula |
C20H26N4O4
|
|---|---|
| Molecular Weight |
386.4448
|
| Exact Mass |
386.195
|
| CAS # |
676500-67-7
|
| PubChem CID |
10452732
|
| Appearance |
White to off-white solid powder
|
| LogP |
3.557
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
28
|
| Complexity |
475
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
ZGCYVRNZWGUXNQ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H26N4O4/c1-26-18-10-15(11-22-7-4-14-5-8-27-9-6-14)2-3-17(18)28-19-13-23-16(12-24-19)20(21)25/h2-3,10,12-14,22H,4-9,11H2,1H3,(H2,21,25)
|
| Chemical Name |
5-[2-methoxy-4-[[2-(oxan-4-yl)ethylamino]methyl]phenoxy]pyrazine-2-carboxamide
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~323.47 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5877 mL | 12.9386 mL | 25.8772 mL | |
| 5 mM | 0.5175 mL | 2.5877 mL | 5.1754 mL | |
| 10 mM | 0.2588 mL | 1.2939 mL | 2.5877 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA