UBP316
Based on 1 Customer Validation
UBP316 (ACET) is a highly potent and selective kainate receptor GluK1 (GluR5) antagonist, with a Kb value of 1.4 nM. UBP316 is effective at blocking the depression of both field excitatory postsynaptic potentials (fEPSPs) and monosynaptically-evoked GABAergic transmission induced by ATPA, a GluK1 selective agonist.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.06%
- No. CAS: 936095-50-0
- Fòrmula: C20H19N3O6S
- Peso molecular:429.45
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Almacenamiento: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
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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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Ver todos los productos específicos de isoformas iGluR
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Actividad biológica
Kb: 1.4 nM (GluK1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>100 μM
Compound: 67
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Antagonist activity at human recombinant GLUA2-AMPA receptor expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay
Antagonist activity at human recombinant GLUA2-AMPA receptor expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay
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[PMID: 17348638] |
| HEK293 | IC50 |
>100 μM
Compound: 67
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Antagonist activity at human recombinant GLUK6 expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay
Antagonist activity at human recombinant GLUK6 expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay
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[PMID: 17348638] |
| HEK293 | IC50 |
>100 μM
Compound: 67
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Antagonist activity at human recombinant GLUK6/GLUK2 expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay
Antagonist activity at human recombinant GLUK6/GLUK2 expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay
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[PMID: 17348638] |
UBP316 is ineffective at GluK2 (GluR6) receptors at all concentrations tested (up to 100 μM) and had no effect at GluK3 (GluR7) when tested at 1 μM[1].
UBP316 (200 nM) reduces short-term facilitation of pre-synaptic calcium transients following repetitive spikes[1].
UBP316 effectively antagonises GluK1-mediated depression of excitatory transmission in CA1 region of the hippocampus in vitro[1].
UBP316 blocks induction of NMDA receptor-independent long-term potentiation (LTP)[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 936095-50-0
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Appearance Solid
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Peso molecular 429.45
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Fòrmula C20H19N3O6S
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Color White to off-white
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SMILES
OC(C(SC(C1=CC=CC=C1)=C2)=C2CN3C(N(C=C(C)C3=O)C[C@H](N)C(O)=O)=O)=O
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Synonyms
ACET
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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 6 months -20°C 1 month
Solvente y solubilidad
1M NaOH : 80 mg/mL (186.28 mM; ultrasonic and adjust pH to 11 with NaOH)
DMSO : 2 mg/mL (4.66 mM; ultrasonic and warming and heat to 60°C; 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: ≥ 0.2 mg/mL (0.47 mM); Clear solution
This protocol yields a clear solution of ≥ 0.2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.0 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: ≥ 0.2 mg/mL (0.47 mM); Clear solution
This protocol yields a clear solution of ≥ 0.2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.0 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.
Pureza y Documentación
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Ficha de datos (276 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. 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 / 1M NaOH | 1 mM | 2.3286 mL | 11.6428 mL | 23.2856 mL | 58.2140 mL |
| 1M NaOH | 5 mM | 0.4657 mL | 2.3286 mL | 4.6571 mL | 11.6428 mL |
| 10 mM | 0.2329 mL | 1.1643 mL | 2.3286 mL | 5.8214 mL | |
| 15 mM | 0.1552 mL | 0.7762 mL | 1.5524 mL | 3.8809 mL | |
| 20 mM | 0.1164 mL | 0.5821 mL | 1.1643 mL | 2.9107 mL | |
| 25 mM | 0.0931 mL | 0.4657 mL | 0.9314 mL | 2.3286 mL | |
| 30 mM | 0.0776 mL | 0.3881 mL | 0.7762 mL | 1.9405 mL | |
| 40 mM | 0.0582 mL | 0.2911 mL | 0.5821 mL | 1.4553 mL | |
| 50 mM | 0.0466 mL | 0.2329 mL | 0.4657 mL | 1.1643 mL | |
| 60 mM | 0.0388 mL | 0.1940 mL | 0.3881 mL | 0.9702 mL | |
| 80 mM | 0.0291 mL | 0.1455 mL | 0.2911 mL | 0.7277 mL | |
| 100 mM | 0.0233 mL | 0.1164 mL | 0.2329 mL | 0.5821 mL |
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