A cell-permeable, blood-brain barrier permeant, non-toxic phenethylpiperidine compound that binds reversibly and with high affinity to the uOR-deltaOR-heteromer. Exhibits a robust beta-arrestin recruitment activity (EC50 = 8.3uM, Emax = 1,197% over basal), which is at least two to three-fold higher than that obtained with ubetagalOR (EC50 = 1.8uM, Emax = 557%) or deltabetagalOR (EC50 = 2.7uM, Emax = 423%) alone. Induces a strong increase in [35S]GTPupsilonS binding (EC50 = 54, 210, and 300nM, and Emax (% basal) = 168, 138 and 113 for with ubetagalOR-deltaOR, ubetagalOR and deltabetagalOR, respectively). Potentiates antinociceptive activity similar to morphine (10mg/kg, s.c. in a tail-flick assay) with less side effects and dependency. However, chronic administration of CYM51010 results in reduced antinociceptive tolerance compared with morphine. Synonyms: CID23723457, CYM-51010, ML335, Opiod Receptor Ligand, Ethyl-1-(4-acetamidobenzyl)-4-phenethylpiperidine-4-carboxylate, Ethyl-1-(4-acetamidobenzyl)-4-(2-phenylethyl)-4-piperidinecarboxylate, Ethyl 1-(4-(acetylamino)benzyl)-4-(2-phenylethyl)-4-piperidinecarboxylate CAS Number: 1069498-96-9 Molecular Formula: C25H32N2O3 Solubility: DMSO Primary Target: muOR-deltaOR-heteromer Storage and Stability: May be stored at 4C. For long-term storage, aliquot and store at 4C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
Purity:
90% (HPLC)
Form:
Supplied as a white solid.
CAS Number:
[1069498-96-9]
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