VPC 23019
Based on 1 Customer Validation
VPC 23019, an aryl amide-containing Sphingosine 1-phosphate (S1P) analog, is a competitive antagonist at the S1P1 and S1P3 receptors (pKi= 7.86 and 5.93, respectively) and an agonist at the S1P4 and S1P5 receptors (pEC50= 6.58 and 7.07, respectively).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.20%
- No. CAS: 449173-19-7
- Fòrmula: C17H29N2O5P
- Peso molecular:372.40
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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)
Actividad biológica
pKi: 7.86 (S1P1); 5.93 (S1P3). pEC50: 6.58 (S1P1); 7.07 (S1P3)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | EC50 |
450 nM
Compound: VPC22173
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Activity at human S1P3 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
Activity at human S1P3 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
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[PMID: 17113298] |
| HEK-293T | EC50 |
500 nM
Compound: VPC22173
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Activity at human S1P4 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
Activity at human S1P4 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
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[PMID: 17113298] |
| HEK-293T | EC50 |
52 nM
Compound: VPC22173
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Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
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[PMID: 17113298] |
| HEK-293T | EC50 |
58 nM
Compound: VPC22173
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Activity at human S1P1 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
Activity at human S1P1 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
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[PMID: 17113298] |
Chemical Information
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No. CAS 449173-19-7
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Appearance Solid
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Peso molecular 372.40
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Fòrmula C17H29N2O5P
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Color Light yellow to yellow
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SMILES
O=C(NC1=CC=CC(CCCCCCCC)=C1)[C@H](N)COP(O)(O)=O
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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)
Solvente y solubilidad
DMSO : 100 mg/mL (268.53 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: 2.08 mg/mL (5.59 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 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 (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 (5.59 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.
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 (268 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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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 | 2.6853 mL | 13.4264 mL | 26.8528 mL | 67.1321 mL |
| 5 mM | 0.5371 mL | 2.6853 mL | 5.3706 mL | 13.4264 mL | |
| 10 mM | 0.2685 mL | 1.3426 mL | 2.6853 mL | 6.7132 mL | |
| 15 mM | 0.1790 mL | 0.8951 mL | 1.7902 mL | 4.4755 mL | |
| 20 mM | 0.1343 mL | 0.6713 mL | 1.3426 mL | 3.3566 mL | |
| 25 mM | 0.1074 mL | 0.5371 mL | 1.0741 mL | 2.6853 mL | |
| 30 mM | 0.0895 mL | 0.4475 mL | 0.8951 mL | 2.2377 mL | |
| 40 mM | 0.0671 mL | 0.3357 mL | 0.6713 mL | 1.6783 mL | |
| 50 mM | 0.0537 mL | 0.2685 mL | 0.5371 mL | 1.3426 mL | |
| 60 mM | 0.0448 mL | 0.2238 mL | 0.4475 mL | 1.1189 mL | |
| 80 mM | 0.0336 mL | 0.1678 mL | 0.3357 mL | 0.8392 mL | |
| 100 mM | 0.0269 mL | 0.1343 mL | 0.2685 mL | 0.6713 mL |