| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C22H18N2O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM) that activates cAMP and β-arrestin2 with EC50 values of 260 nM and 650 nM, respectively. It can be used for neuropathic and/or inflammatory pain research[1]. It is supplied as a white to off-white solid (C22H18N2O2, MW 342.39) at 99.96% purity.
Physical & Chemical Properties
| CAS Number | 102704-40-5 |
|---|---|
| Molecular Formula | C22H18N2O2 |
| Molecular Weight | 342.39 g/mol |
| Purity | 99.96% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | O=[N+]([O-])CC(C1=CC=CC=C1)C2=C(NC3=C2C=CC=C3)C4=CC=CC=C4 |
| Target | CB1 |
| Signaling Pathway | GPCR/G Protein; Neuronal Signaling |
| Solubility | In Vitro: DMSO: 100 mg/mL (292.06 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (292.06 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (7.30 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
GAT211 is stable in human- and rat-liver microsomal incubations, with t1/2 values of 28.4 min and 8.67 min, respectively[2]. In Neuro2a cells, GAT211 limits dopamine D2 receptor-mediated extracellular regulated kinase (ERK) phosphorylation[3].
In Vivo
In the same system, GAT211 potentiates inhibition of electrically evoked vas deferens contraction (EC50=11 nM, Emax=70)[2]. GAT211 (0.3, 1, and 3 mg/kg; 5 mL/kg; ip; 2 doses 5 min apart) reduced locomotor activity and the acoustic startle response in a dose-dependent manner. The vehicle for GAT211 was ethanol, kolliphor, and saline at 1:1:6, injected at 5 mL/kg[3].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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