Cebranopadol

This product is for research use only, not for human use. We do not sell to patients.

Cebranopadol
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
5mg$1003-6 Days
10mg$1503-6 Days
25mg$2503-6 Days
50mg$4153-6 Days
100mg$6193-6 Days
250mg$10503-6 Days
500mg$15503-6 Days

Cat #: V2977 CAS #: 863513-91-1 Purity ≥ 98%

Description: Cebranopadol (also known as GRT-6005) is a novel, first in class compound with potent agonist activity on ORL-1 (opioid receptor like -1) and the well established mu opioid receptor. Cebranopadol is an analgesic nociceptin/orphanin FQ peptide (NOP) that exhibits high potency and efficacy in several rat models of acute and chronic pain (tail-flick, rheumatoid arthritis, bone cancer, spinal nerve ligation, diabetic neuropathy) with ED50 values of 0.5-5.6 µg/kg after intravenous and 25.1 µg/kg after oral administration. It is being evaluated in clinical Phase 2 and Phase 3 trials for the treatment of chronic and acute pain. Recent evidence indicates that the combination of opioid and NOP receptor agonism may be a new treatment strategy for cocaine addiction.

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Molecular Weight (MW)378.49
Molecular FormulaC24H27FN2O
CAS No.863513-91-1
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility In VitroDMSO: >10mM
Water: <1 mg/mL
Ethanol:
SMILES CodeCN(C)[C@]1(C2=CC=CC=C2)CC[C@]3(C(N4)=C(CCO3)C5=C4C=CC(F)=C5)CC1
SynonymsGRT6005; GRT 6005; GRT-6005; Cebranopadol
ProtocolIn VitroIn vitro activity: Cebranopadol (also known as GRT-6005) is a novel, first in class compound with potent agonist activity on ORL-1 (opioid receptor like -1) and the well established mu opioid receptor. Cebranopadol is an analgesic nociceptin/orphanin FQ peptide (NOP) that exhibits high potency and efficacy in several rat models of acute and chronic pain (tail-flick, rheumatoid arthritis, bone cancer, spinal nerve ligation, diabetic neuropathy) with ED50 values of 0.5-5.6 µg/kg after intravenous and 25.1 µg/kg after oral administration. It is being evaluated in clinical Phase 2 and Phase 3 trials for the treatment of chronic and acute pain. Recent evidence indicates that the combination of opioid and NOP receptor agonism may be a new treatment strategy for cocaine addiction. Kinase Assay: Human MOP, DOP, KOP, and NOP receptor binding assays were run in microtiter plates (Costar 3632; Corning Life Sciences, Tewksbury, MA) with wheat germ agglutinin-coated scintillation proximity assay beads (GE Healthcare, Chalfont St. Giles, UK). Cell membrane preparations of Chinese hamster ovary K1 cells transfected with the human MOP receptor (Art.-No. RBHOMM, lot-No. 307-065-A) or the human DOP receptor (Art.-No. RBHODM, lot-No. 423-553-B), and human embryonic kidney cell line 293 cells transfected with the human NOP receptor (Art.-No. RBHORLM, lot-No. 1956) or the human KOP receptor (Art.-No. 6110558, lot-No. 295-769-A) were purchased from PerkinElmer Life and Analytical Sciences (Boston, MA). [N-allyl-2,3-3H]naloxone and [tyrosyl-3,5-3H]deltorphin II (both purchased from PerkinElmer Life and Analytical Sciences), [3H]Ci-977, and [leucyl-3H]nociceptin (both purchased from GE Healthcare) were used as ligands for the MOP, DOP, KOP, and NOP receptor binding studies, respectively. Cell Assay: To test the agonistic activity of cebranopadol on human recombinant MOP, DOP, or NOP receptor-expressing cell membranes from Chinese hamster ovary K1 cells, or KOP receptor-expressing cell membranes from human embryonic kidney cell line 293 cells, 10 µg of membrane proteins per assay was incubated with 0.4 nM [35S]GTPγS (GE Healthcare) and different concentrations of agonists in buffer containing 20 mM HEPES (pH 7.4), 100 mM NaCl, 10 mM MgCl2, 1 mM EDTA, 1 mM dithiothreitol, 1.28 mM NaN3, and 10 µM guanosine diphosphate for 45 minutes at 25°C. The bound radioactivity was determined as previously described.
In VivoBehavioral studies in pain models and pharmacokinetic evaluations were conducted in Sprague-Dawley rats (weight range 134−423 g; tail-flick model: Iffa Credo, Brussels, Belgium; bone cancer model: Harlan Laboratories, Indianapolis, IN; all other pain models and pharmacokinetics: Janvier Laboratories, Le Genest Saint Isle, France); male rats were used for most of the experiments, except for the tail-flick and bone cancer models, for which female Sprague-Dawley rats were used. Studies in side effect models were conducted in male Wistar rats (weight range 150−375 g; Dépré, Saint Doulchard, France). Rats were housed under standard conditions (room temperature 20−24°C, 12 hour light/dark cycle, relative air humidity 35−70%, 10−15 air changes per hour, air movement<0.2 m/s) with food and water available ad libitum in the home cage. Animals were used only once in all in vivo models, except for models of mononeuropathy, for which they were tested repeatedly with a washout period of at least 1 week between tests. Apart from the exceptions mentioned below, animal testing was performed in accordance with the recommendations and policies of the International Association for the Study of Pain and the German Animal Welfare Law. All study protocols were approved by the local government committee for animal research, which is advised by an independent ethics committee. Animals were assigned randomly to treatment groups. Different doses and vehicles were tested in a randomized fashion. Although the operators performing the behavioral tests were not formally 'blinded' with respect to the treatment, they were not aware of the study hypothesis or the nature of differences between drugs.
Animal modelSprague-Dawley rats
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.6421 mL13.2104 mL26.4208 mL52.8416 mL
5mM0.5284 mL2.6421 mL5.2842 mL10.5683 mL
10mM0.2642 mL1.3210 mL2.6421 mL5.2842 mL
20mM0.1321 mL0.6605 mL1.3210 mL2.6421 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
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The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

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Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.