GI-530159
Based on 1 Customer Validation
GI-530159 is a selective opener of TREK1 and TREK2 potassium channels. GI-530159 displays selectivity for TREK1/2 over TRAAK, TASK3 and other potassium channels, with an EC50 of 0.76 μM for TREK1. GI-530159 reduces rat dorsal root ganglion neuron excitability and shows potential analgesic effect.
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- Pureté: 99.45%
- CAS No.: 69563-88-8
- Formule: C27H20F6N2O2
- Masse moléculaire:518.45
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Target: TREK1/2[1]
TREK (TWIK-related K) two pore domain potassium (K2P) channels regulate the excitability of somatosensory nociceptive neurons and mediate pain perception[1].
GI-530159 (1 μM or 10 μM) shows selectivity and activates TREK1 and TREK2 channels but shows no significant effects on TRAAK channels or K channels tested[1].
GI-530159 (0.1-30 μM) activates recombinant human TREK1 channels with EC50s of 0.8 μM and 0.9 μM from Rb efflux and electrophysiological experiments, respectively[1].
GI-530159 (1 μM) reduces rat dorsal root ganglion (DRG) neuron excitability, results in firing frequency reduction and a small hyperpolarisation of resting membrane potential (RMP)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 69563-88-8
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Appearance Solid
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Masse moléculaire 518.45
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Formule C27H20F6N2O2
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Color White to off-white
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SMILES
FC(C(C1=CC=C(OC2=CC=C(N)C=C2)C=C1)(C3=CC=C(OC4=CC=C(N)C=C4)C=C3)C(F)(F)F)(F)F
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : ≥ 100 mg/mL (192.88 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. 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (9.64 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.
Pureté et documentation
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Fiche technique (271 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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Instruction de manipulation (2659 KB)
Références
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 | 1 mM | 1.9288 mL | 9.6441 mL | 19.2883 mL | 48.2207 mL |
| 5 mM | 0.3858 mL | 1.9288 mL | 3.8577 mL | 9.6441 mL | |
| 10 mM | 0.1929 mL | 0.9644 mL | 1.9288 mL | 4.8221 mL | |
| 15 mM | 0.1286 mL | 0.6429 mL | 1.2859 mL | 3.2147 mL | |
| 20 mM | 0.0964 mL | 0.4822 mL | 0.9644 mL | 2.4110 mL | |
| 25 mM | 0.0772 mL | 0.3858 mL | 0.7715 mL | 1.9288 mL | |
| 30 mM | 0.0643 mL | 0.3215 mL | 0.6429 mL | 1.6074 mL | |
| 40 mM | 0.0482 mL | 0.2411 mL | 0.4822 mL | 1.2055 mL | |
| 50 mM | 0.0386 mL | 0.1929 mL | 0.3858 mL | 0.9644 mL | |
| 60 mM | 0.0321 mL | 0.1607 mL | 0.3215 mL | 0.8037 mL | |
| 80 mM | 0.0241 mL | 0.1206 mL | 0.2411 mL | 0.6028 mL | |
| 100 mM | 0.0193 mL | 0.0964 mL | 0.1929 mL | 0.4822 mL |
GI-530159 Related Classifications
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