Org 27569 868273-06-7

Org-27569
分子式：C24H28ClN3O   分子量：409.95
 
產(chǎn)品描述
Org 27569是cannabinoid CB1 receptor變構(gòu)調(diào)節(jié)劑，通過增強激動劑親和力而誘導(dǎo)CB1受體狀態(tài)改變，且降低逆向激動劑的親和力。
靶點
annabinoid CB1 receptor
         
IC50
           
體外研究
Org 27569 is an allosteric modulator of CB1 cannabinoid receptor. It significantly increases the binding of CB1 receptor agonist and causes a significant decrease in specific binding of CB1 receptor inverse agonist. Org 27569 induces CB1 high affinity agonist binding, receptor internalization, and downstream ERK phosphorylation. The allosteric ligand Org 27569 promotes agonist binding to CB1, yet blocks the agonist-induced conformational changes in TM6. Org 27569 traps the receptor in a distinct agonist-bound, but nonsignaling conformational state.
體內(nèi)研究
 
溶解性
DMSO 82 mg/mL，水 <1 mg/mL，乙醇 <1 mg/mL
穩(wěn)定性
2年 -20°C粉狀，6月-80°C溶于DMSO