GAT228

产品名称：

1446648-15-2
GAT228
3-[(1R)-2-nitro-1-phenylethyl]-2-phenyl-1H-Indole
R-(+)-3-(2-Nitro-1-phenylethyl)-2-phenyl-1H-indole

产品介绍：

产品说明

生化/生理作用

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.

基本信息

经验(实验)分子式	C₂₂H₁₈N₂O₂
分子量	342.39
NACRES	NA.77

产品性质

质量水平	100
测定	≥98% (HPLC)
形式	powder
旋光性	[α]/D 80 to 94°, c = 1 in methanol
颜色	white to beige
溶解性	DMSO: 20 mg/mL, clear
储存温度	2-8℃
SMILES string	O=[N+]([O-])C[C@H](C1=CC=CC=C1)C2=C(C3=CC=CC=C3)NC4=CC=CC=C42

安全信息

储存分类代码	13 - Non Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable