| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg |
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| 250mg | |||
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| Targets |
OMDM-5 targets two distinct receptors and a cellular uptake mechanism. It is a selective inhibitor of anandamide cellular uptake (ACU) with a Ki of 4.8 μM, which increases the extracellular concentration of anandamide by blocking its uptake into cells. OMDM-5 is also a potent agonist of TRPV1 with an EC50 of 75 nM. Additionally, it shows weak activity as a ligand for CB1 with a Ki of 4.9 μM. This dual activity at TRPV1 and ACU, combined with weak CB1 binding, makes OMDM-5 a valuable tool for studying pain pathways.
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| ln Vitro |
OMDM-5 demonstrates potent in vitro activity as a TRPV1 agonist (EC50 = 75 nM) and a selective inhibitor of anandamide cellular uptake (Ki = 4.8 μM). It shows weak activity as a CB1 ligand with a Ki of 4.9 μM. The compound's potent TRPV1 agonist activity suggests it may be useful for studying pain and inflammatory pathways, while its ACU inhibitory activity modulates endocannabinoid signaling. The weak CB1 binding indicates that its effects are primarily mediated through TRPV1 and ACU inhibition rather than direct CB1 activation.
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| ln Vivo |
In vivo activity data for OMDM-5 are limited, as the compound is primarily used as a research tool in cell-based assays. Its potent TRPV1 agonist activity and ACU inhibitory activity suggest potential applications in pain research, but comprehensive in vivo studies evaluating its pharmacokinetic properties and efficacy have not been extensively reported. The compound's weak CB1 binding may limit its effects on the endocannabinoid system in vivo. Further research is needed to assess its potential for in vivo applications.
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| Enzyme Assay |
The in vitro receptor binding assay for OMDM-5 involves measuring its affinity for TRPV1 and CB1 receptors. For TRPV1, the assay typically uses cells expressing the receptor and measures calcium flux or membrane potential changes in response to the compound. The EC50 for TRPV1 activation is determined from dose-response curves. For CB1, a radioligand binding assay is performed using membrane preparations from cells expressing CB1, and the Ki value is calculated from competition binding experiments. The anandamide uptake inhibition assay measures the uptake of radiolabeled anandamide into cells in the presence of OMDM-5.
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| Cell Assay |
The in vitro cellular assay for OMDM-5 typically involves measuring its effects on anandamide cellular uptake (ACU) and TRPV1 activation. For ACU inhibition, cells are incubated with radiolabeled anandamide in the presence of various concentrations of OMDM-5, and the amount of anandamide taken up is measured. The Ki value for ACU inhibition is calculated from the dose-response curve. For TRPV1 activation, calcium imaging or FLIPR assays are performed using cells expressing TRPV1. Cytotoxicity is assessed in parallel to ensure that the observed effects are not due to cell death.
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| Animal Protocol |
In vivo animal experiments for OMDM-5 would typically involve administering the compound to rodents via intraperitoneal or intravenous injection. Pain models, such as the formalin test or hot plate test, could be used to assess the compound's analgesic effects mediated by TRPV1 activation and increased anandamide levels. Anandamide levels in tissues could be measured to assess the compound's effects on anandamide uptake. However, comprehensive in vivo studies have not been extensively reported. Further research is needed to evaluate its pharmacokinetic properties and efficacy in animal models.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of OMDM-5 have not been extensively characterized. With a molecular weight of 432.64, the compound is expected to have moderate lipophilicity and reasonable membrane permeability. However, detailed studies on its absorption, distribution, metabolism, and excretion are limited. The compound's stability in plasma and its half-life have not been well defined. Further pharmacokinetic studies would be required to assess its potential for in vivo applications.
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| Toxicity/Toxicokinetics |
Toxicological data for OMDM-5 are limited. In vitro cytotoxicity assays are typically performed to ensure that the compound does not adversely affect cell viability at the concentrations used in activity assays. Comprehensive in vivo toxicology studies, including acute and chronic toxicity, have not been reported. Researchers handling this compound should follow standard safety protocols for handling research chemicals, including the use of personal protective equipment and working in a well-ventilated area.
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| References | |
| Additional Infomation |
OMDM-5 is a research compound that has not entered clinical trials or received regulatory approval for therapeutic use. It is primarily used as a tool compound to study the endocannabinoid system, TRPV1-mediated pain pathways, and anandamide uptake. The compound's potent TRPV1 agonist activity and selective ACU inhibition make it valuable for investigating pain and inflammatory pathways. Further research is needed to explore its potential therapeutic applications.
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| Molecular Formula |
C26H44N2O3
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|---|---|
| Molecular Weight |
432.64
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| Exact Mass |
432.335
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| CAS # |
616884-66-3
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| PubChem CID |
146026184
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
7.9
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
19
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| Heavy Atom Count |
31
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| Complexity |
456
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCCCCC/C=C\CCCCCCCC(=O)NNCC1=CC(=C(C=C1)O)OC
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| InChi Key |
VDYSULCKCSIIIK-KHPPLWFESA-N
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| InChi Code |
InChI=1S/C26H44N2O3/c1-3-4-5-6-7-8-9-10-11-12-13-14-15-16-17-18-26(30)28-27-22-23-19-20-24(29)25(21-23)31-2/h10-11,19-21,27,29H,3-9,12-18,22H2,1-2H3,(H,28,30)/b11-10-
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| Chemical Name |
(Z)-N'-[(4-hydroxy-3-methoxyphenyl)methyl]octadec-9-enehydrazide
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| Synonyms |
OMDM5; OMDM 5
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| 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 | 2.3114 mL | 11.5570 mL | 23.1139 mL | |
| 5 mM | 0.4623 mL | 2.3114 mL | 4.6228 mL | |
| 10 mM | 0.2311 mL | 1.1557 mL | 2.3114 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.
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