Esamisulpride
Based on 1 Customer Validation
Esamisulpride ((S)-Amisulpride) is the S-isomer of Amisulpride (HY-14545). Esamisulpride is a potent dopamine D2/D3 receptor antagonist with Ki values of 4.43 nM for D2R and 0.72 nM for D3R. Esamisulpride is a 5-HT7 receptor antagonist with a Ki of 900 nM. Esamisulpride can be used in the research of schizophrenia and depression.
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- Pureté : 99.04%
- CAS No.: 71675-92-8
- Formule: C17H27N3O4S
- Masse moléculaire:369.48
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
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5-HT7 Receptor |
D2 Receptor |
D3 Receptor |
In Vitro
Esamisulpride is a 5-HT7 receptor antagonist with a Ki of 900 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 71675-92-8
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Appearance Solid
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Masse moléculaire 369.48
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Formule C17H27N3O4S
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Color White to light yellow
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SMILES
O=C(C1=CC(S(=O)(CC)=O)=C(C=C1OC)N)NC[C@H]2N(CCC2)CC
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Synonyms
(S)-Amisulpride; (S)-Aramisulpride; (S)-DAN 2163
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (270.65 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. 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. 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)
In Vivo:
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 (6.77 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.77 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
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.
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.
Pureté et documentation
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Fiche technique (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Timothy J Donahue, et al. (S)-amisulpride as a discriminative stimulus in C57BL/6 mice and its comparison to the stimulus effects of typical and atypical antipsychotics. Eur J Pharmacol. 2014 Jul 5;734:15-22. [Content Brief]
[2]. Vincent Grattan, et al. Antipsychotic Benzamides Amisulpride and LB-102 Display Polypharmacy as Racemates, S Enantiomers Engage Receptors D2 and D3, while R Enantiomers Engage 5-HT7. ACS Omega. 2019 Aug 15;4(9):14151-14154. [Content Brief]
[3]. Hopkins SC, et al. Discovery of Nonracemic Amisulpride to Maximize Benefit/Risk of 5-HT7 and D2 Receptor Antagonism for the Treatment of Mood Disorders. Clin Pharmacol Ther. 2021 Sep;110(3):808-815. [Content Brief]
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. 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 | 2.7065 mL | 13.5325 mL | 27.0651 mL | 67.6627 mL |
| 5 mM | 0.5413 mL | 2.7065 mL | 5.4130 mL | 13.5325 mL | |
| 10 mM | 0.2707 mL | 1.3533 mL | 2.7065 mL | 6.7663 mL | |
| 15 mM | 0.1804 mL | 0.9022 mL | 1.8043 mL | 4.5108 mL | |
| 20 mM | 0.1353 mL | 0.6766 mL | 1.3533 mL | 3.3831 mL | |
| 25 mM | 0.1083 mL | 0.5413 mL | 1.0826 mL | 2.7065 mL | |
| 30 mM | 0.0902 mL | 0.4511 mL | 0.9022 mL | 2.2554 mL | |
| 40 mM | 0.0677 mL | 0.3383 mL | 0.6766 mL | 1.6916 mL | |
| 50 mM | 0.0541 mL | 0.2707 mL | 0.5413 mL | 1.3533 mL | |
| 60 mM | 0.0451 mL | 0.2255 mL | 0.4511 mL | 1.1277 mL | |
| 80 mM | 0.0338 mL | 0.1692 mL | 0.3383 mL | 0.8458 mL | |
| 100 mM | 0.0271 mL | 0.1353 mL | 0.2707 mL | 0.6766 mL |
Esamisulpride Related Classifications
HY-126068 Related Classifications
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