EST73502 monohydrochloride

EST73502 单盐酸盐

EST73502 monohydrochloride

E655426-1ml

1ml

10mM in DMSO

干燥,-80℃储存

超低温冰袋运输

EST73502 monohydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with K i s of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 monohydrochloride has antinociceptive activity In Vivo EST73502 monohydrochloride (10-40 mg/kg; p.o.) shows a dose-response analgesic effect reaching a maximum of 64% and an EC 50 of 14 mg/kg in the paw pressure test in CD1 male mice . EST73502 monohydrochloride (5 mg/kg; i.p.; twice a day; for 10 days) attenuates partial sciatic nerve ligation (PSNL)-induced mechanical allodynia in male CD1 mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male CD1 mice, PSNL model Dosage: 5 mg/kg Administration: Intraperitoneal injection, twice a day, for 10 days Result: Attenuated the expression of mechanical allodynia induced by PSNL, reaching a maximal effect of 56%. IC50& Target:Ki: 64 nM (MOR), 118 nM (σ1R)

EST73502单盐酸盐是一种选择性、口服活性和血脑屏障（BBB）穿透性双重μ-阿片受体（MOR）激动剂和σ1受体（σ1R）拮抗剂，MOR和σ1R的K i分别为64 nM和118 nM。EST73502单盐酸盐

2535970-65-9(DMSO)

C19H27ClF2N2O2

388.88 g/mol

CCN1CC2(CCN(CC2)CCC3=C(C=CC(=C3)F)F)OC(C1=O)C.Cl

59898787