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SML1952 Sigma

GAT228

≥98% (HPLC)

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

  • CAS Number 1446648-15-2

  • Empirical Formula (Hill Notation) C22H18N2O2

  • Molecular Weight 342.39

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Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, G
assay   ≥98% (HPLC)
form   powder
optical activity   [α]/D 80 to 94°, c = 1 in methanol
color   white to beige
solubility   DMSO: 20 mg/mL clear
storage temp.   2-8°C

Description

Biochem/physiol Actions

GAT228 is the R-(+)-enantiomer of GAT211, a positive allosteric modulator (PAM) of cannabinoid CB1 receptor signaling that was found to amplify the therapeutic effect of endocannabinoids without the negative side effects of psychoactivity or tolerance. GAT228 was found to be an unbiased CB1 allosteric agonist, while the S-(-)-enantiomer, GAT229,was found to be a potent, Gαi/o-biased CB1 PAM without intrinsic activity. In radioligand binding assays, both GAT228 and GAT229 behaved as PAMs of orthosteric ligand binding. Allosteric CB1R activation by GAT211 and its enantiomers could be a better therapeutic strategy for enhancing endogenous cannabinergic activity than targeting endocannabinoid-degrading enzymes with small-molecule inhibitors, with a lower likelihood of tolerance and dependence.

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Safety Information

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Documents

Certificate of Analysis

Protocols & Articles
Peer-Reviewed Papers
15

References

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