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506418 µ-δ Opiod Receptor Agonist, CYM51010 - CAS 1069498-96-9 - Calbiochem

506418
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Key Specifications Table

Empirical FormulaCAS #
C₂₅H₃₂N₂O₃ 1069498-96-9

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      Description
      OverviewA cell-permeable, blood-brain barrier permeant, non-toxic phenethylpiperidine compound that binds reversibly and with high affinity to the μOR-δOR-heteromer. Exhibits a robust β-arrestin recruitment activity (EC50 = 8.3 µM; Emax = 1,197% over basal), which is at least two to three-fold higher than that obtained with μβgalOR (EC50 = 1.8 µM; Emax = 557%) or δβgalOR (EC50 = 2.7 µM; Emax = 423%) alone. Induces a strong increase in [35S]GTPγS binding (EC50 = 54, 210, and 300 nM; and Emax (% basal) = 168, 138 and 113 for with μβgalOR-δOR, μβgalOR and δβgalOR, respectively). Potentiates antinociceptive activity similar to morphine (10 mg/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.
      Catalogue Number506418
      Brand Family Calbiochem®
      SynonymsCID23723457, 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
      References
      ReferencesGomes, I., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 12072.
      Product Information
      CAS number1069498-96-9
      FormWhite solid
      Hill FormulaC₂₅H₃₂N₂O₃
      Chemical formulaC₂₅H₃₂N₂O₃
      ReversibleY
      Structure formula ImageStructure formula Image
      Applications
      Biological Information
      Primary TargetµOR-δOR-heteromer
      Purity≥90% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      References

      Reference overview
      Gomes, I., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 12072.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision06-December-2013 JSW
      SynonymsCID23723457, 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
      DescriptionA cell-permeable, blood-brain barrier permeant, non-toxic phenethylpiperidine compound that binds reversibly and with high affinity to the μOR-δOR-heteromer. Exhibits a robust β-arrestin recruitment activity (EC50 = 8.3 µM; Emax = 1,197% over basal), which is at least two to three-fold higher than that obtained with μβgalOR (EC50 = 1.8 µM; Emax = 557%) or δβgalOR (EC50 = 2.7 µM; Emax = 423%) alone. Induces a strong increase in [35S]GTPγS binding (EC50 = 54, 210, and 300 nM; and Emax (% basal) = 168, 138 and 113 for with μβgalOR-δOR, μβgalOR and δβgalOR, respectively). Potentiates antinociceptive activity similar to morphine (10 mg/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.
      FormWhite solid
      CAS number1069498-96-9
      Chemical formulaC₂₅H₃₂N₂O₃
      Structure formulaStructure formula
      Purity≥90% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesGomes, I., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 12072.