GAT229

产品名称：

889860-85-9
GAT229
S-(-)-3-(2-Nitro-1-phenylethyl)-2-phenyl-1H-indole

产品介绍：

产品说明

生化/生理作用

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.

基本信息

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

产品性质

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℃

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