YM348
Based on 1 publication(s) in Google Scholar
YM348 is a potent and orally active 5-HT2C receptor agonist, which shows a high affinity for cloned human 5-HT2C receptor (Ki: 0.89 nM).
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- Pureté: 98.89%
- CAS No.: 372163-84-3
- Formule: C14H17N3O
- Masse moléculaire:243.30
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Stockage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) YM348
MoreVoir tous les produits spécifiques à Isoform 5-HT Receptor
More
Activité biologique
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5-HT2C Receptor 0.89 nM (Ki) |
5-HT2C Receptor |
5-HT2B Receptor 2.5 nM (Ki) |
5-HT2A Receptor 13 nM (Ki) |
5-HT2C Receptor 1 nM (EC50) |
5-HT2B Receptor 3.2 nM (EC50) |
5-HT2A Receptor 93 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
1 nM
Compound: 7i, YM348
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Agonist activity at human cloned 5HT2C receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysis
Agonist activity at human cloned 5HT2C receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysis
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[PMID: 18035544] |
| CHO | EC50 |
93 nM
Compound: 7i, YM348
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Agonist activity at human cloned 5HT2A receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysis
Agonist activity at human cloned 5HT2A receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysis
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[PMID: 18035544] |
| HEK293-EBNA | EC50 |
3.2 nM
Compound: 7i, YM348
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Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
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[PMID: 18035544] |
YM348 has high affinity for cloned human 5-HT2C receptors with a Ki value of 0.89 nM and lower affinities for human-cloned 5-HT2B (Ki: 2.5 nM) and 5-HT2A receptors (Ki: 13 nM). To assess the binding specificity of YM348, a broad evaluation of an additional 46 binding sites including several other 5-HT receptor subtypes (1A, 1B, 1D, 3, 4, 5A, 6, 7) is performed. IC50 values of YM348 are found to be >1 μM for all of the binding sites except for the human 5-HT1A receptors (Ki: 130 nM), bovine 5-HT1D receptors (Ki: 481 nM), human 5-HT7 receptors (Ki: 177 nM), and human α2A receptors (Ki: 126 nM).YM348 exhibits a full-agonistic activity on human 5-HT2A and 5-HT2B receptors. The EC50 values of YM348 for 5-HT2C, 5-HT2A, and 5-HT2B receptors are 1.0, 93 and 3.2 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 372163-84-3
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Appearance Oil
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Masse moléculaire 243.30
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Formule C14H17N3O
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Color Light yellow to brown
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SMILES
C[C@H](N)CN(N=C1)C2=C1C=CC3=C2C=C(CC)O3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (1)
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Journal Impact Factor
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Most Recent
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J Affect Disord
Uncoupling serotonin (2C) and dopamine (D2) receptor heterodimers ameliorate PTSD-like behaviors. [Abstract]2025 Mar 21:S0165-0327(25)00475-6. PMID: 40122260
Solvant et solubilité
DMSO : 100 mg/mL (411.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (10.28 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocole
Experiments are performed with membranes obtained from Chinese Hamster Ovary (CHO) cells expressing human 5-HT2C or 5-HT2A receptors and Human Embryonic Kidney 293-Epstein-Barr virus nuclear antigen (HEK293-EBNA) cells expressing human 5-HT2B receptors. Binding assays with [3H] 5-HT are carried out. The reaction medium (50 mM Tris-HCl buffer (pH 7.4) containing 4 mM CaCl2, 10 M pargyline and 0.1 mg/ml L-(+)-ascorbic acid) containing [3H] 5-HT, membrane preparation and test compounds are incubated at 37°C for 30 min. Nonspecific binding is determined in the presence of 10 M 5-HT, and specific binding is calculated as the total binding minus the nonspecific binding. After incubation, 4 mL of 50 mM Tris-HCl buffer (pH 7.4) containing 4 mM CaCl2 is added, and the medium is filtrated under decompression through a Whatman GF/B glass filter pretreated with 0.1% polyethyleneimine. The filter is washed with the same buffer solution (4 mL×3). The glass filter is immersed in 6 mL of liquid scintillator (Packard, Aquasol-2), and the radioactivity is measured with a liquid scintillation counter. The amount of protein is measured. The dissociation constants (Kd values) are obtained by Scatchard analysis using SAS (ver. 6.11). The concentrations of compounds showing 50% inhibition of receptor binding, IC50 values, are obtained by nonlinear analysis using SAS (ver. 6.11). The Ki values indicating affinity for receptors are calculated[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[1]
Male Wistar rats (215-350 g) are used. Rats are administered YM348 (0.0677, 0.203, 0.677, and 2.03 mg/kg) orally and moved again to their home cages. After 20 min, thereafter, the rats are individually placed in transparent acrylic plastic cages (35×30×18 cm), and their motor activity is measured for 40 min. The measurements are carried out using a SUPER-MEX sensor. SB242084 (0.1-3 mg/kg i.p.) is administered 30 min before YM348 treatment.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.1102 mL | 20.5508 mL | 41.1015 mL | 102.7538 mL |
| 5 mM | 0.8220 mL | 4.1102 mL | 8.2203 mL | 20.5508 mL | |
| 10 mM | 0.4110 mL | 2.0551 mL | 4.1102 mL | 10.2754 mL | |
| 15 mM | 0.2740 mL | 1.3701 mL | 2.7401 mL | 6.8503 mL | |
| 20 mM | 0.2055 mL | 1.0275 mL | 2.0551 mL | 5.1377 mL | |
| 25 mM | 0.1644 mL | 0.8220 mL | 1.6441 mL | 4.1102 mL | |
| 30 mM | 0.1370 mL | 0.6850 mL | 1.3701 mL | 3.4251 mL | |
| 40 mM | 0.1028 mL | 0.5138 mL | 1.0275 mL | 2.5688 mL | |
| 50 mM | 0.0822 mL | 0.4110 mL | 0.8220 mL | 2.0551 mL | |
| 60 mM | 0.0685 mL | 0.3425 mL | 0.6850 mL | 1.7126 mL | |
| 80 mM | 0.0514 mL | 0.2569 mL | 0.5138 mL | 1.2844 mL | |
| 100 mM | 0.0411 mL | 0.2055 mL | 0.4110 mL | 1.0275 mL |
YM348 Related Classifications
HY-100330 Related Classifications
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