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A 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.
Gomes, I., et al. 2013. Proc. Natl. Acad. Sci. USA110, 12072.
Product Information
CAS number
1069498-96-9
Form
White solid
Hill Formula
C₂₅H₃₂N₂O₃
Chemical formula
C₂₅H₃₂N₂O₃
Reversible
Y
Structure formula Image
Applications
Biological Information
Primary Target
µOR-δOR-heteromer
Purity
≥90% by HPLC
Physicochemical Information
Cell permeable
Y
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 Instructions
Following 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
产品目录编号
GTIN
5.06418.0001
04055977242720
Documentation
参考
参考信息概述
Gomes, I., et al. 2013. Proc. Natl. Acad. Sci. USA110, 12072.
数据表
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.
A 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.
Form
White solid
CAS number
1069498-96-9
Chemical formula
C₂₅H₃₂N₂O₃
Structure formula
Purity
≥90% by HPLC
Solubility
DMSO (100 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity
Standard Handling
References
Gomes, I., et al. 2013. Proc. Natl. Acad. Sci. USA110, 12072.
