GPV0057
Based on 1 Customer Validation
GPV0057 (Compound 5d) is a selective and potent P-glycoprotein (P-gp) inhibitor. GPV0057 is also a selective potassium channel Kir2.1 activator. GPV0057 competitively binds to the substrate-binding site of P-gp, inhibiting ATP-dependent drug efflux to reverse multidrug resistance in tumor cells. GPV0057 can also stabilizes the open state of Kir2.1 and promotes potassium ion influx. GPV0057 is promising for research of tumors with high P-gp expression, Kir2.1-deficient diseases such as heart failure and Andersen-Tawil Syndrome.
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- Purity: 99.20%
- CAS No.: 86383-89-3
- 화학식: C22H27NO4
- 분자량:369.45
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보관: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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CCRF-CEM | ED50 |
359 nM
Compound: 4i
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The chemosensitizing effect was measured against P-glycoprotein expressing CCRF-CEM cells in the presence of 5 uM daunomycin
The chemosensitizing effect was measured against P-glycoprotein expressing CCRF-CEM cells in the presence of 5 uM daunomycin
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[PMID: 7629817] |
| CCRF-CEM | ED50 |
1.49 μM
Compound: 1i
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Effective dose against CCRF-CEM vcr 100 cells by using MTT assay
Effective dose against CCRF-CEM vcr 100 cells by using MTT assay
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[PMID: 8941391] |
| CCRF-CEM | ED50 |
1.49 μM/L
Compound: 1i
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Effective dose against CCRF-CEM vcr 100 cells by using MTT assay
Effective dose against CCRF-CEM vcr 100 cells by using MTT assay
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[PMID: 8941391] |
| CCRF-CEM | ED50 |
13.56 μM
Compound: 1i
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Effective dose against CCRF-CEM vcr 100 cells by using rhodamine efflux studies.
Effective dose against CCRF-CEM vcr 100 cells by using rhodamine efflux studies.
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[PMID: 8941391] |
| CCRF-CEM | ED50 |
13.56 μM/L
Compound: 1i
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Effective dose against CCRF-CEM vcr 100 cells by using rhodamine efflux studies.
Effective dose against CCRF-CEM vcr 100 cells by using rhodamine efflux studies.
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[PMID: 8941391] |
| CCRF-CEM/VCR-1000 | IC50 |
3.75 μM
Compound: 5
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In vitro multi drug resistance (MDR) reversal inhibitory activity against CCRF-CEM/VCR-1000 cell line
In vitro multi drug resistance (MDR) reversal inhibitory activity against CCRF-CEM/VCR-1000 cell line
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[PMID: 14584949] |
| MDR | EC50 |
3.645 μM
Compound: 39
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Inhibition of P-glycoprotein expressed in MDR CCRF vcr1000 cells by daunorubicin efflux assay
Inhibition of P-glycoprotein expressed in MDR CCRF vcr1000 cells by daunorubicin efflux assay
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[PMID: 17352460] |
Chemical Information
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CAS No. 86383-89-3
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Appearance Solid
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분자량 369.45
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화학식 C22H27NO4
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Color White to off-white
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SMILES
O=C(CCC1=CC=CC=C1)C2=C(OCC(CN3CCOCC3)O)C=CC=C2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (270.67 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)
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: ≥ 5 mg/mL (13.53 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (13.53 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
순도&문서
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Cseke A, et al. Propafenone analogue with additional H-bond acceptor group shows increased inhibitory activity on P-glycoprotein. Arch Pharm (Weinheim). 2020 Mar;353(3):e1900269. [Content Brief]
[2]. Li E, et al. Development of new Kir2.1 channel openers from propafenone analogues. Br J Pharmacol. 2025 Feb;182(3):633-650. [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 |
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| DMSO | 1 mM | 2.7067 mL | 13.5336 mL | 27.0673 mL | 67.6682 mL |
| 5 mM | 0.5413 mL | 2.7067 mL | 5.4135 mL | 13.5336 mL | |
| 10 mM | 0.2707 mL | 1.3534 mL | 2.7067 mL | 6.7668 mL | |
| 15 mM | 0.1804 mL | 0.9022 mL | 1.8045 mL | 4.5112 mL | |
| 20 mM | 0.1353 mL | 0.6767 mL | 1.3534 mL | 3.3834 mL | |
| 25 mM | 0.1083 mL | 0.5413 mL | 1.0827 mL | 2.7067 mL | |
| 30 mM | 0.0902 mL | 0.4511 mL | 0.9022 mL | 2.2556 mL | |
| 40 mM | 0.0677 mL | 0.3383 mL | 0.6767 mL | 1.6917 mL | |
| 50 mM | 0.0541 mL | 0.2707 mL | 0.5413 mL | 1.3534 mL | |
| 60 mM | 0.0451 mL | 0.2256 mL | 0.4511 mL | 1.1278 mL | |
| 80 mM | 0.0338 mL | 0.1692 mL | 0.3383 mL | 0.8459 mL | |
| 100 mM | 0.0271 mL | 0.1353 mL | 0.2707 mL | 0.6767 mL |
GPV0057 Related Classifications
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