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 activityIn VivoEST73502 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). Specification: 10mM in DMSO Molecular Formula: C19H27ClF2N2O2 Molecular Weight: 388.88
- UPC:
- 12352107
- Condition:
- New
- Availability:
- 8-12 weeks
- Weight:
- 1.06 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- E655426-1ml
- CAS:
- 2535970-65-9
- Product Size:
- 1ml
