| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Cannabinoid 1 receptor (CB1R).
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|---|---|
| ln Vitro |
GAT211 had a t1/2 of 8.67 minutes and 28.4 minutes, respectively, in both scaffold and human liver microsomes [2].
GAT211 is a selective CB1R positive allosteric modulator (PAM) with a pKb of 7.26. It has an Arrestin2 EC50 of 775 nM. GAT211 amplifies the therapeutic effect of endocannabinoids without the negative side effects of psychoactivity or tolerance. The compound is a racemic mixture of GAT228 and GAT229, which have enantiomer-specific activities. GAT211 can be used for neuropathic and/or inflammatory pain research. It is valuable for studying CB1-mediated neurological processes, including pain modulation, appetite control, and neuroprotection. |
| ln Vivo |
GAT211 (0.3 mg/kg, 1 mg/kg, 3 mg/kg; 5 ml/kg; intraperitoneally; 2 doses 5 minutes apart) dose-like reductions in auditory startle reactions and locomotor activity. GAT211 was administered with a volume of 5 mL/kg after being dissolved in ethanol, kolliphor, and saline at a ratio of 1:1:6[3].
In vivo efficacy of GAT211 has been demonstrated in animal models of neuropathic and inflammatory pain. As a CB1R PAM, GAT211 enhances the effects of endocannabinoids, leading to pain relief without producing tolerance or dependence. The compound's unique mechanism allows for the amplification of endocannabinoid signaling with fewer psychoactive side effects compared to direct CB1R agonists. Specific dosing regimens and detailed efficacy data are available in the primary literature. |
| Enzyme Assay |
CB1R positive allosteric modulation is assessed using in vitro cell-based assays. Cells expressing CB1R are treated with a CB1R agonist (e.g., CP55,940) in the presence or absence of GAT211 at various concentrations (typically 0.001-100 µM). Receptor signaling is measured by assessing downstream pathways such as cAMP inhibition (Gαi signaling) or β-arrestin recruitment. The pKb value is calculated from the potentiation of the agonist response. Arrestin2 EC50 is determined from β-arrestin recruitment assays.
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| Cell Assay |
Cellular activity is evaluated in cells expressing CB1R. Cells are treated with GAT211 at various concentrations (typically 0.001-100 µM) and CB1R agonist-induced signaling is measured. Gαi-mediated inhibition of cAMP accumulation is measured by ELISA or HTRF-based assays. β-arrestin recruitment is measured using PathHunter or Tango assays. The potentiation of agonist-induced signaling by GAT211 is assessed to determine its PAM activity. Selectivity is evaluated by testing against other cannabinoid receptors (CB2R) and other GPCRs.
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| Animal Protocol |
In vivo efficacy is studied in animal models of neuropathic and inflammatory pain. GAT211 is administered via various routes (oral, intraperitoneal, subcutaneous) at doses determined from pharmacokinetic and tolerability studies. Pain responses are assessed using behavioral tests such as von Frey filaments (mechanical allodynia), hot plate (thermal hyperalgesia), and formalin-induced paw licking. Tolerance development is assessed by repeated dosing. Locomotor activity and other behavioral parameters are monitored to assess potential psychoactive effects.
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| ADME/Pharmacokinetics |
GAT211 has a molecular formula of C22H18N2O2 and a molecular weight of 342.39 g/mol. CAS Number: 102704-40-5. Appearance: Solid. Storage: Powder at -20°C for 3 years or at 4°C for 2 years; in solvent at -80°C for 6 months or at -20°C for 1 month. The compound is a racemic mixture of GAT228 and GAT229. It is soluble in DMSO.
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| Toxicity/Toxicokinetics |
Safety data for GAT211 indicate it is a research compound for laboratory use only. As a CB1R PAM, it may have central nervous system effects. However, its allosteric mechanism is designed to minimize the psychoactive side effects associated with direct CB1R agonists. Specific toxicological profiles including acute toxicity, organ toxicity, genotoxicity, and reproductive toxicity are not extensively published. Standard laboratory safety practices should be followed during handling, including the use of personal protective equipment and adequate ventilation.
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| References |
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| Additional Infomation |
GAT211 is a research tool compound for studying CB1R biology and cannabinoid signaling. It is not approved for clinical use. The compound is a positive allosteric modulator (PAM) of CB1R, which enhances the activity of endogenous cannabinoids at the receptor. This unique mechanism makes GAT211 a valuable tool for investigating the therapeutic potential of CB1R modulation in pain, inflammation, and neurological disorders while avoiding the psychoactive effects and tolerance associated with direct CB1R agonists. GAT211 has been shown to suppress pathological pain without producing tolerance or dependence.
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| Molecular Formula |
C22H18N2O2
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|---|---|
| Molecular Weight |
342.4
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| Exact Mass |
342.136
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| CAS # |
102704-40-5
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| PubChem CID |
4402318
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
585.8±50.0 °C at 760 mmHg
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| Flash Point |
308.1±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.668
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| LogP |
6.23
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
465
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)C2=C(C3=CC=CC=C3N2)C(C[N+](=O)[O-])C4=CC=CC=C4
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| InChi Key |
OHZDCJJHWPHZJD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H18N2O2/c25-24(26)15-19(16-9-3-1-4-10-16)21-18-13-7-8-14-20(18)23-22(21)17-11-5-2-6-12-17/h1-14,19,23H,15H2
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| Chemical Name |
3-(2-nitro-1-phenylethyl)-2-phenyl-1H-indole
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| Synonyms |
GAT-211; GAT 211; GAT211
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~292.06 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9206 mL | 14.6028 mL | 29.2056 mL | |
| 5 mM | 0.5841 mL | 2.9206 mL | 5.8411 mL | |
| 10 mM | 0.2921 mL | 1.4603 mL | 2.9206 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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