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

506418
Price could not be retrieved
Minimum Quantity needs to be mulitiple of
Upon Order Completion More Information
You Saved ()
 
Request Pricing
Limited AvailabilityLimited Availability
Stocked 
Discontinued
Limited Quantities Available
Available
    Remaining : Will advise
      Remaining : Will advise
      Will advise
      Contact Customer Service
      View Pricing & Availability
      Click To Print This Page

      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₅H₃₂N₂O₃ 1069498-96-9

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.06418.0001
      Retrieving availability...
      Limited AvailabilityLimited Availability
      Stocked 
      Discontinued
      Limited Quantities Available
      Available
        Remaining : Will advise
          Remaining : Will advise
          Will advise
          Contact Customer Service

          Glass bottle 10 mg
          Retrieving price...
          Price could not be retrieved
          Minimum Quantity needs to be mulitiple of
          Upon Order Completion More Information
          You Saved ()
           
          Request Pricing
          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.