Description
EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity.
Product information
CAS Number: 1838622-25-5
Molecular Weight: 352.42
Formula: C19H26F2N2O2
Chemical Name: (2R)-9-[2-(2,5-difluorophenyl)ethyl]-4-ethyl-2-methyl-1-oxa-4,9-diazaspiro[5.5]undecan-3-one
Smiles: CCN1CC2(CCN(CCC3=CC(F)=CC=C3F)CC2)O[C@H](C)C1=O
InChiKey: KALIKXMQWFLZKB-CQSZACIVSA-N
InChi: InChI=1S/C19H26F2N2O2/c1-3-23-13-19(25-14(2)18(23)24)7-10-22(11-8-19)9-6-15-12-16(20)4-5-17(15)21/h4-5,12,14H,3,6-11,13H2,1-2H3/t14-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vivo:
EST73502 (10-40 mg/kg; p.o.) shows a dose-response analgesic effect reaching a maximum of 64% and an EC50 of 14 mg/kg in the paw pressure test in CD1 male mice. EST73502 (5 mg/kg; i.p.; twice a day; for 10 days) attenuates partial sciatic nerve ligation (PSNL)-induced mechanical allodynia in male CD1 mice.
Products are for research use only. Not for human use.
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