GAT-211
- Product Name
- GAT-211
- CAS No.
- 102704-40-5
- Chemical Name
- GAT-211
- Synonyms
- AZ4;AZ 4;AZ-4;GAT-211;GAT211 >=98% (HPLC);3-(2-nitro-1-phenylethyl)-2-phenyl-1H-indole;1H-Indole, 3-(2-nitro-1-phenylethyl)-2-phenyl-
- CBNumber
- CB84667931
- Molecular Formula
- C22H18N2O2
- Formula Weight
- 342.39
- MOL File
- 102704-40-5.mol
GAT-211 Property
- storage temp.
- Store at -20°C
- solubility
- DMF: 25 mg/ml; DMF:PBS (pH 7.2)(1:3): 0.25 mg/ml; DMSO: 10 mg/ml; Ethanol: 5 mg/ml
- form
- A crystalline solid
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- SML1926
- Product name
- GAT211
- Purity
- ≥98% (HPLC)
- Packaging
- 25 mg
- Price
- $467
- Updated
- 2026/03/19
- Product number
- SML1926
- Product name
- GAT211
- Purity
- ≥98% (HPLC)
- Packaging
- 5 mg
- Price
- $86.1
- Updated
- 2025/07/31
- Product number
- 24484
- Product name
- GAT211
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 24484
- Product name
- GAT211
- Packaging
- 5mg
- Price
- $172
- Updated
- 2024/03/01
- Product number
- 7131CM
- Product name
- 3-(2-Nitro-1-phenylethyl)-2-phenyl-1H-indole
- Packaging
- 5mg
- Price
- $289
- Updated
- 2021/12/16
GAT-211 Chemical Properties,Usage,Production
Description
GAT211, aslo known as AZ-4, is a small molecule CB1 positive allosteric modulator. GAT211 suppresses allodynia and produces synergistic antiallodynic effects with fatty acid amide hydrolase and monoacylglycerol lipase inhibitors in paclitaxel-treated mice. Positive allosteric modulation of CB1-receptor signaling with GAT211shows promise as a safe and effective analgesic strategy that lacks tolerance, dependence, and abuse liability.
Uses
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[1].
in vivo
GAT211 potentiates the inhibition of electrically evoked vas deferens contraction in the same system (EC50=11 nM, Emax=70)[2].
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].
IC 50
CB1
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. DOI:10.1016/j.bmc.2021.116421
[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). DOI:10.1007/s00213-020-05755-x
[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. DOI:10.1016/j.biopsych.2017.06.032
GAT-211 Preparation Products And Raw materials
Raw materials
Preparation Products
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