GAT2711
Based on 1 Customer Validation
GAT2711 is a full agonist of α9 nAChR with an EC50 of 230 nM. GAT2711 shows 340-fold selective for α9 over α7 nAChRs. GAT2711 inhibits ATP-induced IL-1β release in THP-1 cells. GAT2711 retains full analgesic activity in α7 nAChR knockout mice.
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- Pureté : 98.00%
- Formule: C20H27IN4O
- Masse moléculaire:466.36
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Stockage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
α9 nAChR[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| THP-1 | IC50 |
0.5 μM
Compound: 3h; GAT2711
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Inhibition of ATP-mediated IL-1beta release in LPS primed BzATP induced monocytic human THP-1 cells primed with LPS for 5 hrs followed by BzATP and compound addition for 40 mins by ELISA
Inhibition of ATP-mediated IL-1beta release in LPS primed BzATP induced monocytic human THP-1 cells primed with LPS for 5 hrs followed by BzATP and compound addition for 40 mins by ELISA
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[PMID: 38748608] |
In Vitro
GAT2711 (compound 3h;pretreated LPS (1 μg/mL) for for 5 h and then incubate with BzATP (100 μM) for 40 minutes) significantly inhibits ATP-induced IL-1β release in THP-1 cells, with an IC50 value of 0.5 μM, demonstrating potent anti-inflammatory activity similar to Acetylcholine. GAT2711 does not induce IL-1β release in the absence of ATP, suggesting selective inhibition of ATP-mediated inflammatory responses[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Complete Freund́s adjuvant (CFA; 20 μL; 50%) (HY-153808)-induced inflammatory pain in C57BL/6J mice (WT and α7 knockout mice)[1]
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Dosage:20 mg/kg, 10 mg/kg (1 volume ethanol/1 volume Emulphor-620/18 volumes distilled water)
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Administration:Intraperitoneal injection; once
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Result:Significantly reduced mechanical hypersensitivity and paw edema in CFA-treated mice, showing analgesic effects independent of α7 nAChR.
Chemical Information
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Appearance Solid
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Masse moléculaire 466.36
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Formule C20H27IN4O
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Color White to off-white
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SMILES
C[N+]1(CC)CCN(C2=CC=C(C=C2)NC(C3=NC(C)=CC=C3)=O)CC1.[I-]
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
In Vitro:
DMSO : ≥ 100 mg/mL (214.43 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 (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)
In Vivo:
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 (5.36 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.36 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 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.
In Vivo Dissolution Calculator
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.
Pureté et documentation
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Fiche technique (272 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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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 (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 | 2.1443 mL | 10.7213 mL | 21.4427 mL | 53.6067 mL |
| 5 mM | 0.4289 mL | 2.1443 mL | 4.2885 mL | 10.7213 mL | |
| 10 mM | 0.2144 mL | 1.0721 mL | 2.1443 mL | 5.3607 mL | |
| 15 mM | 0.1430 mL | 0.7148 mL | 1.4295 mL | 3.5738 mL | |
| 20 mM | 0.1072 mL | 0.5361 mL | 1.0721 mL | 2.6803 mL | |
| 25 mM | 0.0858 mL | 0.4289 mL | 0.8577 mL | 2.1443 mL | |
| 30 mM | 0.0715 mL | 0.3574 mL | 0.7148 mL | 1.7869 mL | |
| 40 mM | 0.0536 mL | 0.2680 mL | 0.5361 mL | 1.3402 mL | |
| 50 mM | 0.0429 mL | 0.2144 mL | 0.4289 mL | 1.0721 mL | |
| 60 mM | 0.0357 mL | 0.1787 mL | 0.3574 mL | 0.8934 mL | |
| 80 mM | 0.0268 mL | 0.1340 mL | 0.2680 mL | 0.6701 mL | |
| 100 mM | 0.0214 mL | 0.1072 mL | 0.2144 mL | 0.5361 mL |
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