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

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

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

Primary Target: µOR-δOR-heteromer
506418
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1069498-96-9C₂₅H₃₂N₂O₃

Products

Catalogue NumberPackaging Qty/Pack
5.06418.0001 Glass bottle 10 mg
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
Global Trade Item Number
Catalogue Number GTIN
5.06418.0001 04055977242720

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 Protect from light
+2°C to +8°C
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.