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GAT-211

Names

[ CAS No. ]:
102704-40-5

[ Name ]:
GAT-211

[Synonym ]:
MFCD02165420
1H-Indole, 3-(2-nitro-1-phenylethyl)-2-phenyl-
GAT211
3-(2-Nitro-1-phenylethyl)-2-phenyl-1H-indole

Biological Activity

[Description]:

GAT-211 (GAT211) is a selective cannabinoid 1 receptor (CB1R) positive allosteric modulator with pKb of 7.26, Arrestin2 EC50 of 775 nM; engages CB1R allosteric site(s), enhances the binding of the orthosteric full agonist [3H]CP55,490, and reduces the binding of the orthosteric antagonist/inverse agonist [3H]SR141716A; displayed both PAM and agonist activity in HEK293A and Neuro2a cells expressing human recombinant CB1R (hCB1R) and in mouse-brain membranes rich in native CB1R.

[References]

References 1. Laprairie RB, et al. ACS Chem Neurosci. 2017 Jun 21;8(6):1188-1203. View Related Products by Target Cannabinoid Receptor

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
585.8±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C22H18N2O2

[ Molecular Weight ]:
342.391

[ Flash Point ]:
308.1±30.1 °C

[ Exact Mass ]:
342.136841

[ LogP ]:
6.23

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.668

Related Compounds