UCPH-101
Based on 1 publication(s) in Google Scholar
UCPH-101 is an excitatory amino acid transporter subtype 1 (EAAT1) inhibitor with an IC50 of 0.66 μM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.61%
- No. CAS: 1118460-77-7
- Fòrmula: C27H22N2O3
- Peso molecular:422.48
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) UCPH-101
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Actividad biológica
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EAAT1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>300 μM
Compound: 1o
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Displacement of [3H]D-Asp from human EAAT2 receptor expressed in HEK293 cells
Displacement of [3H]D-Asp from human EAAT2 receptor expressed in HEK293 cells
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[PMID: 19161278] |
| HEK293 | IC50 |
>300 μM
Compound: 1o
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Displacement of [3H]D-Asp from human EAAT3 receptor expressed in HEK293 cells
Displacement of [3H]D-Asp from human EAAT3 receptor expressed in HEK293 cells
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[PMID: 19161278] |
| HEK293 | IC50 |
0.66 μM
Compound: 1b, UCPH-101
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Inhibition of human EAAT1 expressed in HEK293 cells by [3H]D-Asp uptake assay
Inhibition of human EAAT1 expressed in HEK293 cells by [3H]D-Asp uptake assay
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[PMID: 20857912] |
| HEK293 | IC50 |
0.66 μM
Compound: 26; UCPH-101
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Inhibition of EAAT1 (unknown origin) stably expressed in HEK293 cells assessed as reduction in [14C]glutamate uptake incubated for 5 mins by microbeta scintillation counting method
Inhibition of EAAT1 (unknown origin) stably expressed in HEK293 cells assessed as reduction in [14C]glutamate uptake incubated for 5 mins by microbeta scintillation counting method
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[PMID: 31774679] |
| HEK293 | IC50 |
0.66 μM
Compound: UCPH-101
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Inhibition of human EAAT1 expressed in HEK293 cells assessed as inhibition of 3[H]-D-Aspartate uptake after 6 mins by scintillation counting method
Inhibition of human EAAT1 expressed in HEK293 cells assessed as inhibition of 3[H]-D-Aspartate uptake after 6 mins by scintillation counting method
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[PMID: 22594609] |
| HEK293 | IC50 |
0.66 μM
Compound: 1o
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Displacement of [3H]D-Asp from human EAAT1 receptor expressed in HEK293 cells
Displacement of [3H]D-Asp from human EAAT1 receptor expressed in HEK293 cells
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[PMID: 19161278] |
| HEK293 | IC50 |
120 nM
Compound: 1o
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Activity at human EAAT1 expressed in HEK293 cells assessed as inhibition of Glu-induced fluorescent response by FLIPR membrane potential blue assay
Activity at human EAAT1 expressed in HEK293 cells assessed as inhibition of Glu-induced fluorescent response by FLIPR membrane potential blue assay
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[PMID: 19161278] |
| HEK293 | IC50 |
6.3 μM
Compound: UCPH-101
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Inhibition of the Excitatory Amino Acid Transporter 1 (EAAT1, SLC1A3) as assessed by a phenotypic impedance-based assay detecting changes in cell morphology by L-glutamate uptake in HEK-293 JumpIN-SLC1A3 cells
Inhibition of the Excitatory Amino Acid Transporter 1 (EAAT1, SLC1A3) as assessed by a phenotypic impedance-based assay detecting changes in cell morphology by L-glutamate uptake in HEK-293 JumpIN-SLC1A3 cells
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[PMID: 35677430] |
| HEK293 | IC50 |
6.3 μM
Compound: UCPH-101
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Inhibition of the Excitatory Amino Acid Transporter 1 (EAAT1, SLC1A3) as assessed by a phenotypic impedance-based assay detecting changes in cell morphology by L-glutamate uptake in HEK-293 JumpIN-SLC1A3 cells (PubChem AID: 1745862)
Inhibition of the Excitatory Amino Acid Transporter 1 (EAAT1, SLC1A3) as assessed by a phenotypic impedance-based assay detecting changes in cell morphology by L-glutamate uptake in HEK-293 JumpIN-SLC1A3 cells (PubChem AID: 1745862)
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[PMID: 35677430] |
UCPH-101 and UCPH-102 inhibit EAAT1 anion currents in a concentration-dependent manner, with KD values of 0.34±0.03 μM (Hill=1.3±0.13, n≥9) for UCPH-101 and 0.17±0.02 μM (Hill=0.97±0.11, n≥7) for UCPH-102. A small but significant decrease in the total expression levels of both HA-EAAT1 and HA-GLAST is observed in cells preincubated with 100 μM UCPH-101 (p=0.048)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1118460-77-7
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Appearance Solid
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Peso molecular 422.48
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Fòrmula C27H22N2O3
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Color White to off-white
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SMILES
O=C(C1)C2=C(OC(N)=C(C#N)C2C3=CC=C(OC)C=C3)CC1C4=CC=CC5=C4C=CC=C5
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Antioxid Redox Signal
Selective clearance of senescent chondrocytes in osteoarthritis by targeting EAAT1 to induce ferroptosis. [Abstract]2023 Aug;39(4-6):262-277. PMID: 36601724
Solvente y solubilidad
DMSO : ≥ 50 mg/mL (118.35 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (5.92 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.
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.
Protocolo
Cells are split into poly-D-lysine-coated black 96-well plates with clear bottom. At 16 to 24 h later, the medium is aspirated, and the cells are washed with 100 μL Krebs buffer [140 mM NaCl/4.7 mM KCl/2.5 mM CaCl2/1.2 mM MgCl2/11 mM HEPES/10 mM D-glucose, pH 7.4]; 50 μL Krebs buffer supplemented with various concentrations of UCPH-101 or TBOA is added to the wells, after which an additional 50 μL Krebs buffer supplemented with the FMP assay dye (1 mg/mL) is added to each well. The plate is incubated at 37°C in a humidified 5% CO2 incubator for 30 min and assayed in a reader measuring emission at 560 nm caused by excitation at 530 nm before and up to 1 min after addition of 33 μL Glu solution[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (278 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3670 mL | 11.8349 mL | 23.6698 mL | 59.1744 mL |
| 5 mM | 0.4734 mL | 2.3670 mL | 4.7340 mL | 11.8349 mL | |
| 10 mM | 0.2367 mL | 1.1835 mL | 2.3670 mL | 5.9174 mL | |
| 15 mM | 0.1578 mL | 0.7890 mL | 1.5780 mL | 3.9450 mL | |
| 20 mM | 0.1183 mL | 0.5917 mL | 1.1835 mL | 2.9587 mL | |
| 25 mM | 0.0947 mL | 0.4734 mL | 0.9468 mL | 2.3670 mL | |
| 30 mM | 0.0789 mL | 0.3945 mL | 0.7890 mL | 1.9725 mL | |
| 40 mM | 0.0592 mL | 0.2959 mL | 0.5917 mL | 1.4794 mL | |
| 50 mM | 0.0473 mL | 0.2367 mL | 0.4734 mL | 1.1835 mL | |
| 60 mM | 0.0394 mL | 0.1972 mL | 0.3945 mL | 0.9862 mL | |
| 80 mM | 0.0296 mL | 0.1479 mL | 0.2959 mL | 0.7397 mL | |
| 100 mM | 0.0237 mL | 0.1183 mL | 0.2367 mL | 0.5917 mL |
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