SML1951

GAT229

≥98% (HPLC)

• Sinônimo(s): S-(-)-3-(2-Nitro-1-phenylethyl)-2-phenyl-1H-indole
• Fórmula empírica (Notação de Hill): C₂₂H₁₈N₂O₂
• Número CAS: 889860-85-9
• Peso molecular: 342.39
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Ensaio: ≥98% (HPLC)
• Formulário: powder
• atividade óptica: [α]/D -80 to -94°, c = 1 in methanol
• cor: white to beige
• solubilidade: DMSO: 20 mg/mL, clear
• temperatura de armazenamento: 2-8°C

Descrição

Ações bioquímicas/fisiológicas

GAT229 is the S-(-)-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. GAT229 was found to be a potent, Gαi/o-biased CB1 PAM without intrinsic activity, while the R-(+)-enantiomer, GAT228, was found to be an unbiased CB1 allosteric agonist. In radioligand binding assays, both GAT228 and GAT229 behaved as PAMs of orthosteric ligand binding, with GAT229 exhibiting higher potency and efficacy. 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.

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable