Fedovapagon
Based on 1 publication(s) in Google Scholar
Fedovapagon (VA106483) is a selective and orally active vasopressin V2 receptor (V2R) agonist with an EC50 of 24 nM. Fedovapagon can be used in the research of nocturia.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.43%
- No. CAS: 347887-36-9
- Fòrmula: C27H34N4O3
- Peso molecular:462.58
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Almacenamiento:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Fedovapagon
MoreVer todos los productos específicos de isoformas Vasopressin Receptor
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
V2 Receptor |
V2 Receptor 24 nM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
150 nM
Compound: 20e, VA106483
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Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
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[PMID: 19053774] |
| HEK293 | EC50 |
24 nM
Compound: 20e, VA106483
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Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
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[PMID: 19053774] |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Brattleboro rats[1]
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Dosage:1 mg/kg, 3 mg/kg
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Administration:Oral administration
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Result:Reduced urine volume with almost full inhibition of urine output for 2 h.
Returned the urine to normal levels 5 h after dosing.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 347887-36-9
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Appearance Solid
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Peso molecular 462.58
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Fòrmula C27H34N4O3
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Color Off-white to light yellow
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SMILES
CC1=C(CNC(N2CCC[C@]2(C(N(C)C)=O)[H])=O)C=CC(C(N3CCCCC4=C3C=CC=C4)=O)=C1
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Synonyms
VA106483
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
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Continence (Amst)
Endogenous vasopressin and vasopressin receptor 2 in bladder as anti-diuretic / anti-spasmodic targets for the treatment of multifactorial nocturia. [Abstract]2025 Dec:16:102292. PMID: 41503219
Solvente y solubilidad
In Vitro:
DMSO : ≥ 125 mg/mL (270.22 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (stored under nitrogen). 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 (stored under nitrogen). 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: ≥ 2.08 mg/mL (4.50 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.50 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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 (273 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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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 (stored under nitrogen). 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 | 2.1618 mL | 10.8089 mL | 21.6179 mL | 54.0447 mL |
| 5 mM | 0.4324 mL | 2.1618 mL | 4.3236 mL | 10.8089 mL | |
| 10 mM | 0.2162 mL | 1.0809 mL | 2.1618 mL | 5.4045 mL | |
| 15 mM | 0.1441 mL | 0.7206 mL | 1.4412 mL | 3.6030 mL | |
| 20 mM | 0.1081 mL | 0.5404 mL | 1.0809 mL | 2.7022 mL | |
| 25 mM | 0.0865 mL | 0.4324 mL | 0.8647 mL | 2.1618 mL | |
| 30 mM | 0.0721 mL | 0.3603 mL | 0.7206 mL | 1.8015 mL | |
| 40 mM | 0.0540 mL | 0.2702 mL | 0.5404 mL | 1.3511 mL | |
| 50 mM | 0.0432 mL | 0.2162 mL | 0.4324 mL | 1.0809 mL | |
| 60 mM | 0.0360 mL | 0.1801 mL | 0.3603 mL | 0.9007 mL | |
| 80 mM | 0.0270 mL | 0.1351 mL | 0.2702 mL | 0.6756 mL | |
| 100 mM | 0.0216 mL | 0.1081 mL | 0.2162 mL | 0.5404 mL |
Fedovapagon Related Classifications
HY-14887 Related Classifications
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