| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg | |||
| Other Sizes |
| Targets |
Axomadol targets opioid receptors as an agonist and also inhibits the reuptake of monoamines (such as serotonin and norepinephrine). This dual mechanism is similar to that of tramadol, combining opioid receptor activation with monoaminergic modulation to produce analgesic effects. The compound has opioid agonistic properties.
|
|---|---|
| ln Vitro |
In vitro, Axomadol demonstrates opioid agonistic properties, activating opioid receptors to produce analgesic effects. It also inhibits the reuptake of monoamines, enhancing monoaminergic neurotransmission. These activities contribute to its centrally active analgesic profile. Detailed in vitro potency data are available in the primary literature.
|
| ln Vivo |
In vivo, Axomadol has been studied as a centrally active analgesic agent for the treatment of pain, including postoperative pain. Its dual mechanism of action—opioid agonism and monoamine reuptake inhibition—provides analgesic effects through complementary pathways. Detailed in vivo efficacy data including pain models and analgesic dose ranges are available in preclinical literature.
|
| Enzyme Assay |
In vitro receptor binding assays for Axomadol typically involve evaluating its affinity for opioid receptors (mu, delta, kappa) and monoamine transporters (SERT, NET) using radioligand binding. Membrane preparations from cells expressing the receptors or transporters are incubated with radiolabeled ligands and varying concentrations of the compound. Ki or IC50 values are calculated from displacement curves.
|
| Cell Assay |
Cell-based assays for Axomadol involve culturing cells expressing opioid receptors or monoamine transporters. Cells are treated with Axomadol at concentrations ranging from 0.1 nM to 10 µM. Receptor activation is measured by downstream signaling such as cAMP accumulation or G protein activation. Monoamine reuptake inhibition is assessed by measuring the uptake of radiolabeled serotonin or norepinephrine.
|
| Animal Protocol |
In vivo animal experiments for Axomadol typically involve administration to rodent models of pain via oral gavage or subcutaneous injection. Analgesic efficacy is assessed by behavioral tests such as the tail-flick test, hot plate test, or formalin test. Pharmacokinetic parameters are evaluated by measuring compound levels in blood and brain tissue. Toxicity is assessed by monitoring body weight and behavior.
|
| ADME/Pharmacokinetics |
Axomadol (molecular weight 279.37, formula C16H25NO3) is a centrally active small molecule. It is soluble in DMSO at 100 mg/mL. Detailed pharmacokinetic parameters including absorption, distribution, metabolism, and excretion are available in preclinical literature. Its dual mechanism of action may influence its pharmacokinetic and pharmacodynamic profile.
|
| Toxicity/Toxicokinetics |
No detailed toxicology data are specifically available for Axomadol from the search results. As an opioid agonist, potential toxicity may include opioid-related side effects such as respiratory depression, constipation, and dependence. Comprehensive toxicological evaluation including acute, subchronic, and genotoxicity studies has likely been conducted in preclinical development. The compound is for research use only.
|
| References | |
| Additional Infomation |
Axomadol is being investigated in the clinical trial NCT01043263 (EN3324) for the efficacy and safety of (Axomadol) in patients with chronic low back pain.
Axomadol (EN3324) (CAS#: 187219-99-4) is a centrally active analgesic agent with opioid agonistic properties and inhibitory effects on monoamine reuptake. It is used in pain relief studies. Molecular weight: 279.37, formula: C16H25NO3. It is not an approved therapeutic agent. |
| Molecular Formula |
C16H25NO3
|
|---|---|
| Molecular Weight |
279.3746
|
| Exact Mass |
279.183
|
| CAS # |
187219-99-4
|
| PubChem CID |
15344754
|
| Appearance |
Off-white to light yellow solid powder
|
| LogP |
1.5
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
20
|
| Complexity |
310
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
CN(C)C[C@@H]1CC[C@@H](C[C@]1(C2=CC(=CC=C2)OC)O)O
|
| InChi Key |
LQJLLAOISDVBJM-OFQRWUPVSA-N
|
| InChi Code |
InChI=1S/C16H25NO3/c1-17(2)11-13-7-8-14(18)10-16(13,19)12-5-4-6-15(9-12)20-3/h4-6,9,13-14,18-19H,7-8,10-11H2,1-3H3/t13-,14-,16+/m0/s1
|
| Chemical Name |
(1S,3S,6S)-6-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexane-1,3-diol
|
| 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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~100 mg/mL (~357.95 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5795 mL | 17.8974 mL | 35.7948 mL | |
| 5 mM | 0.7159 mL | 3.5795 mL | 7.1590 mL | |
| 10 mM | 0.3579 mL | 1.7897 mL | 3.5795 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
