| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
pKi: 10.7 (MT1)[1]. pKi: 10.4 (MT2)[1]
MT1 and MT2 melatonin membrane receptors. UCM 608 is a high-affinity agonist at these receptors. |
|---|---|
| ln Vitro |
A strong agonist of the melatonin membrane receptor is UCM 608. MT1 and MT2 had pKi values of 10.7 and 10.4, respectively [1].
UCM 608 (2-Phenylmelatonin) is a high-affinity melatonin receptor agonist with pKi values of 10.7 for MT1 and 10.4 for MT2 receptors. It is a strong agonist of the melatonin membrane receptor. The compound has been observed to demonstrate mixed antagonist/agonist activity in systems with differential expression of the receptor subtypes. It is a highly potent melatonin agonist that displays higher potency than melatonin itself in some assays. |
| ln Vivo |
No detailed in vivo activity data are publicly available for UCM 608. As a potent melatonin receptor agonist, its in vivo effects would be expected to be related to the physiological roles of melatonin, including regulation of circadian rhythms, sleep, and neuroprotection.
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| Enzyme Assay |
In vitro receptor binding assays are performed to determine the affinity of UCM 608 for MT1 and MT2 receptors. Radioligand binding studies using membrane preparations from cells expressing the receptors are conducted. The compound's ability to displace a specific radiolabeled ligand from each receptor is measured to calculate its pKi values.
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| Cell Assay |
In vitro cell-based assays are conducted using cells expressing recombinant MT1 or MT2 receptors. The cells are treated with UCM 608, and receptor activation is measured by assessing downstream signaling events such as inhibition of cAMP accumulation. The potency of the compound at each receptor is determined from these functional assays.
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| Animal Protocol |
In vivo studies would be conducted in animal models to evaluate the effects of UCM 608 on circadian rhythms, sleep, and other melatonin-mediated processes. The compound's effects on sleep-wake cycles, body temperature, and melatonin receptor-mediated behaviors could be assessed.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for UCM 608. As a small molecule with high receptor affinity, its ADME properties would be characterized in standard preclinical studies to guide in vivo experiments.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for UCM 608. As a melatonin receptor agonist, its toxicity profile is expected to be related to its mechanism of action. Standard safety assessments would be required for any therapeutic development.
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| References |
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| Additional Infomation |
N-[2-(5-methoxy-2-phenyl-1H-indole-3-yl)ethyl]acetamide is a phenylindole.
UCM 608 (2-Phenylmelatonin) is a high-affinity melatonin receptor agonist with pKi values of 10.7 for MT1 and 10.4 for MT2 receptors. It is used as a research tool to study melatonin receptor pharmacology and physiology. The compound is not approved for human therapeutic use and is strictly for research purposes. |
| Molecular Formula |
C19H20N2O2
|
|---|---|
| Molecular Weight |
308.37
|
| Exact Mass |
308.152
|
| CAS # |
151889-03-1
|
| PubChem CID |
4018512
|
| Appearance |
Off-white to yellow solid powder
|
| Density |
1.172g/cm3
|
| Boiling Point |
612.4ºC at 760 mmHg
|
| Flash Point |
324.2ºC
|
| Vapour Pressure |
6.16E-15mmHg at 25°C
|
| Index of Refraction |
1.619
|
| LogP |
3.913
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
23
|
| Complexity |
395
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(=O)NCCC1=C(NC2=C1C=C(C=C2)OC)C3=CC=CC=C3
|
| InChi Key |
OFCLARYYBGKCHN-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H20N2O2/c1-13(22)20-11-10-16-17-12-15(23-2)8-9-18(17)21-19(16)14-6-4-3-5-7-14/h3-9,12,21H,10-11H2,1-2H3,(H,20,22)
|
| Chemical Name |
N-[2-(5-methoxy-2-phenyl-1H-indol-3-yl)ethyl]acetamide
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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) |
DMSO: 100 mg/mL (324.29 mM)
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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 | 3.2429 mL | 16.2143 mL | 32.4286 mL | |
| 5 mM | 0.6486 mL | 3.2429 mL | 6.4857 mL | |
| 10 mM | 0.3243 mL | 1.6214 mL | 3.2429 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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