SML1952

GAT228

≥98% (HPLC)

• 別名: 3-[(1R)-2-nitro-1-phenylethyl]-2-phenyl-1H-Indole, R-(+)-3-(2-Nitro-1-phenylethyl)-2-phenyl-1H-indole
• 実験式（ヒル表記法）: C₂₂H₁₈N₂O₂
• CAS番号: 1446648-15-2
• 分子量: 342.39
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• フォーム: powder
• 光学活性: [α]/D 80 to 94°, c = 1 in methanol
• 色: white to beige
• 溶解性: DMSO: 20 mg/mL, clear
• 保管温度: 2-8°C
• SMILES記法: O=[N+]([O-])C[C@H](C1=CC=CC=C1)C2=C(C3=CC=CC=C3)NC4=CC=CC=C42
• InChI: 1S/C22H18N2O2/c25-24(26)15-19(16-9-3-1-4-10-16)21-18-13-7-8-14-20(18)23-22(21)17-11-5-2-6-12-17/h1-14,19,23H,15H2/t19-/m1/s1
• InChI Key: OHZDCJJHWPHZJD-LJQANCHMSA-N

詳細

生物化学的／生理学的作用

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.

Unbiased cannabinoid CB1 allosteric agonist

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable