Usmarapride
Based on 1 publication(s) in Google Scholar
Usmarapride (SUVN-D4010) (Example 3)is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=27.5 nM). Usmarapride (SUVN-D4010) can be used for the research of cognitive deficits associated with Alzheimer's disease.
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- Pureza: 98.0%
- No. CAS: 1428862-33-2
- Fòrmula: C23H31N5O6
- Peso molecular:473.52
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Usmarapride
MoreVer todos los productos específicos de isoformas 5-HT Receptor
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Actividad biológica
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5-HT4 Receptor 44 nM (EC50) |
Usmarapride (1, 3, and 10 mg/kg; p.o.) significantly reverses the scopolamine-induced amnesia[1].
Usmarapride shows a statistically significant effect at 3.0 mg/kg on both exploration time and recognition index[1].
Usmarapride (SUVN-D4010) shows good oral exposures, good bioavailability, and good brain exposures in rats[1].
Pharmacokinetic of Usmarapride in Rats[1]
(3.0 mg/kg for p.o. dosing; 1.0 mg/kg for i.v.)
| F% | Cmax (ng/mL) | AUC (ng·hr/mL) | t1/2 (h) | Vdss (L/kg) | CL (mLg/min/kg) |
| 34 | 360 | 709 | 1.7 | 8.0 | 76 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1428862-33-2
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Appearance Solid
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Peso molecular 473.52
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Fòrmula C23H31N5O6
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Color White to off-white
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SMILES
CC(N1N=C(C2=NN=C(C3CCN(CCCOC)CC3)O2)C4=C1C=CC=C4)C.O=C(O)C(O)=O
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Synonyms
SUVN-D4010
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
DMSO : 33.33 mg/mL (70.39 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). 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). 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 (5.28 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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 (5.28 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 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.
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)
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.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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). 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 | 2.1118 mL | 10.5592 mL | 21.1184 mL | 52.7961 mL |
| 5 mM | 0.4224 mL | 2.1118 mL | 4.2237 mL | 10.5592 mL | |
| 10 mM | 0.2112 mL | 1.0559 mL | 2.1118 mL | 5.2796 mL | |
| 15 mM | 0.1408 mL | 0.7039 mL | 1.4079 mL | 3.5197 mL | |
| 20 mM | 0.1056 mL | 0.5280 mL | 1.0559 mL | 2.6398 mL | |
| 25 mM | 0.0845 mL | 0.4224 mL | 0.8447 mL | 2.1118 mL | |
| 30 mM | 0.0704 mL | 0.3520 mL | 0.7039 mL | 1.7599 mL | |
| 40 mM | 0.0528 mL | 0.2640 mL | 0.5280 mL | 1.3199 mL | |
| 50 mM | 0.0422 mL | 0.2112 mL | 0.4224 mL | 1.0559 mL | |
| 60 mM | 0.0352 mL | 0.1760 mL | 0.3520 mL | 0.8799 mL |
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