GAT211
Based on 1 Customer Validation
GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM). GAT211 activates cAMP and β-arrestin2 with EC50 values of 260 nM and 650 nM, respectively. GAT211 inhibits GAT211 can be used for neuropathic and/or inflammatory pain research.
For research use only. We do not sell to patients.
- Purity: 99.96%
- CAS No.: 102704-40-5
- Formula: C22H18N2O2
- Molecular Weight:342.39
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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CB1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
72 nM
Compound: 6d; GAT211
|
Agonist activity at human CB1 receptor expressed in CHO cell membranes assessed as increase in G-protein coupling by measuring [35S]GTPgammaS binding after 90 mins in presence of [35S]GTPgammaS by liquid scintillation analysis
Agonist activity at human CB1 receptor expressed in CHO cell membranes assessed as increase in G-protein coupling by measuring [35S]GTPgammaS binding after 90 mins in presence of [35S]GTPgammaS by liquid scintillation analysis
|
[PMID: 31756109] |
| CHO-K1 | EC50 |
1200 nM
Compound: 6d; GAT211
|
Allosteric agonist activity at human CB1R expressed in CHO-K1 cells assessed as increase in beta arrestin2 recruitment after 90 mins by pathhunter beta-arrestin assay
Allosteric agonist activity at human CB1R expressed in CHO-K1 cells assessed as increase in beta arrestin2 recruitment after 90 mins by pathhunter beta-arrestin assay
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[PMID: 31756109] |
| CHO-K1 | EC50 |
200 nM
Compound: 6d; GAT211
|
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta arrestin2 recruitment after 90 mins in presence of 100 nM CP55940 by pathhunter beta-arrestin assay
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta arrestin2 recruitment after 90 mins in presence of 100 nM CP55940 by pathhunter beta-arrestin assay
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[PMID: 31756109] |
| CHO-K1 | EC50 |
230 nM
Compound: 1; GAT211
|
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as CP55940-induced cAMP level by hit-hunter cAMP assay
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as CP55940-induced cAMP level by hit-hunter cAMP assay
|
[PMID: 31413808] |
| CHO-K1 | EC50 |
230 nM
Compound: 6d; GAT211
|
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assay
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assay
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[PMID: 31756109] |
| CHO-K1 | EC50 |
78 nM
Compound: 6d; GAT211
|
Allosteric agonist activity at human CB1R expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 90 mins by hit-hunter cAMP assay
Allosteric agonist activity at human CB1R expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 90 mins by hit-hunter cAMP assay
|
[PMID: 31756109] |
| CHO-K1 | EC50 |
8.1 nM
Compound: 6d; GAT211
|
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-induced cAMP accumulation after 90 mins in presence of 100 nM CP55940 by hit-hunter cAMP assay
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-induced cAMP accumulation after 90 mins in presence of 100 nM CP55940 by hit-hunter cAMP assay
|
[PMID: 31756109] |
| CHO-K1 | EC50 |
940 nM
Compound: 1; GAT211
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Positive allosteric modulatory activity at mouse CB1R expressed in CHO-K1 cells assessed as CP55940-induced beta-arrestin2 recruitment by pathhunter beta-arrestin assay
Positive allosteric modulatory activity at mouse CB1R expressed in CHO-K1 cells assessed as CP55940-induced beta-arrestin2 recruitment by pathhunter beta-arrestin assay
|
[PMID: 31413808] |
| CHO-K1 | EC50 |
940 nM
Compound: 6d; GAT211
|
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta-arrestin2 recruitment after 90 mins in presence of CP55940 at EC20 concentration by pathhunter beta-arrestin assay
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta-arrestin2 recruitment after 90 mins in presence of CP55940 at EC20 concentration by pathhunter beta-arrestin assay
|
[PMID: 31756109] |
| HEK293 | EC50 |
17 nM
Compound: 6d; GAT211
|
Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.001 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)
Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.001 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)
|
[PMID: 31756109] |
| HEK293 | EC50 |
17 nM
Compound: 6d; GAT211
|
Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.03 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)
Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.03 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)
|
[PMID: 31756109] |
| HEK293 | EC50 |
17 nM
Compound: 6d; GAT211
|
Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.1 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)
Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.1 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)
|
[PMID: 31756109] |
| HEK293 | EC50 |
17 nM
Compound: 6d; GAT211
|
Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.3 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)
Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.3 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)
|
[PMID: 31756109] |
| HEK293 | EC50 |
240 nM
Compound: 6d; GAT211
|
Allosteric agonist activity at N-terminal GFP-tagged rat CB1R expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production after 30 min by TR-FRET assay
Allosteric agonist activity at N-terminal GFP-tagged rat CB1R expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production after 30 min by TR-FRET assay
|
[PMID: 31756109] |
GAT211 is stable in both human- and rat-liver microsomal incubations, with t1/2 of 28.4 min and 8.67 min, repsectively[2].
GAT211 limits dopamine D2 receptor-mediated extracellular regulated kinase (ERK) phosphorylation in Neuro2a cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GAT211 (0.3 mg/kg, 1 mg/kg, 3 mg/kg; 5 mL/kg; ip; 2 doses with 5 min interval) dose-dependently reduced locomotor activity and the acoustic startle response.GAT211 is dissolved in a vehicle of ethanol, kolliphor, and saline at a ratio of 1:1:6 and injected at a volume of 5 mL/kg[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 102704-40-5
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Appearance Solid
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Molecular Weight 342.39
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Formula C22H18N2O2
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Color White to off-white
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SMILES
O=[N+]([O-])CC(C1=CC=CC=C1)C2=C(NC3=C2C=CC=C3)C4=CC=CC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (292.06 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.
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.
Purity & Documentation
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Data Sheet (283 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)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Garai S, et al. Design, synthesis, and pharmacological profiling of cannabinoid 1 receptor allosteric modulators: Preclinical efficacy of C2-group GAT211 congeners for reducing intraocular pressure. Bioorg Med Chem. 2021 Nov 15;50:116421. [Content Brief]
[2]. McElroy DL, et al. Antipsychotic potential of the type 1 cannabinoid receptor positive allosteric modulator GAT211: preclinical in vitro and in vivo studies. Psychopharmacology (Berl). [Content Brief]
[3]. Richard A Slivicki, et al. Positive Allosteric Modulation of Cannabinoid Receptor Type 1 Suppresses Pathological Pain Without Producing Tolerance or Dependence. Biol Psychiatry. 2018 Nov 15;84(10):722-733. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9206 mL | 14.6032 mL | 29.2065 mL | 73.0161 mL |
| 5 mM | 0.5841 mL | 2.9206 mL | 5.8413 mL | 14.6032 mL | |
| 10 mM | 0.2921 mL | 1.4603 mL | 2.9206 mL | 7.3016 mL | |
| 15 mM | 0.1947 mL | 0.9735 mL | 1.9471 mL | 4.8677 mL | |
| 20 mM | 0.1460 mL | 0.7302 mL | 1.4603 mL | 3.6508 mL | |
| 25 mM | 0.1168 mL | 0.5841 mL | 1.1683 mL | 2.9206 mL | |
| 30 mM | 0.0974 mL | 0.4868 mL | 0.9735 mL | 2.4339 mL | |
| 40 mM | 0.0730 mL | 0.3651 mL | 0.7302 mL | 1.8254 mL | |
| 50 mM | 0.0584 mL | 0.2921 mL | 0.5841 mL | 1.4603 mL | |
| 60 mM | 0.0487 mL | 0.2434 mL | 0.4868 mL | 1.2169 mL | |
| 80 mM | 0.0365 mL | 0.1825 mL | 0.3651 mL | 0.9127 mL | |
| 100 mM | 0.0292 mL | 0.1460 mL | 0.2921 mL | 0.7302 mL |
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