SML1951

GAT229

≥98% (HPLC)

• 동의어(들): S-(-)-3-(2-Nitro-1-phenylethyl)-2-phenyl-1H-indole
• 실험식(Hill 표기법): C₂₂H₁₈N₂O₂
• CAS Number: 889860-85-9
• Molecular Weight: 342.39
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• 분석: ≥98% (HPLC)
• 양식: powder
• 광학 활성: [α]/D -80 to -94°, c = 1 in methanol
• 색상: white to beige
• solubility: DMSO: 20 mg/mL, clear
• 저장 온도: 2-8°C

설명

생화학적/생리학적 작용

Gαi/o-biased CB1 cannabinoid postive allosteric modulator (PAM) with no intrinsic activity

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.

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable