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Purity: ≥98%
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.
| ln Vitro |
With Ki values of 1±0.5 nM, 2.4±1.2 nM, and 64±11 nM for rat NOP, mu-opioid peptide (MOP) receptor, and kappa-opioid peptide (KOP) receptor, and 0.9±0.2 nM, 0.7±0.3 nM, and 2.6±1.4 nM for rat NOP, MOP, and KOP receptor, respectively, cebranopadol binds to opioid receptors with high affinity (subnanomolar to nanomolar range) to nociceptin/orphanin FQ peptide (NOP) and opioid receptors[1].
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| ln Vivo |
With ED50 values of 0.5-5.6 μg/kg after intravenous and 25.1 μg/kg after oral administration, cebrachanopadol demonstrates highly potent and efficacious antinociceptive and antihypersensitive effects in several rat models of acute and chronic pain (tail-flick, rheumatoid arthritis, bone cancer, spinal nerve ligation, and diabetic neuropathy). Cebranopadol is more effective in models of chronic neuropathic pain than acute nociceptive pain when compared to selective MOP receptor agonists. The long half-life of cebranopadol is demonstrated by its prolonged duration of action (up to 7 hours after intravenous 12 μg/kg; >9 hours after oral 55 μg/kg in the rat tail-flick test). Pretreatment with either opioid receptor antagonist naloxone or selective NOP receptor antagonist J-113397 partially reverses the antihypersensitive activity of cebranopadol in the spinal nerve ligation model, suggesting that both opioid receptor agonism and NOP are involved in this activity[1].
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| References |
[1]. Linz K, et al. Cebranopadol: a novel potent analgesic nociceptin/orphanin FQ peptide and opioid receptor agonist. J Pharmacol Exp Ther. 2014 Jun;349(3):535-48.
[2]. de Guglielmo G, et al. Cebranopadol Blocks the Escalation of Cocaine Intake and Conditioned Reinstatement of Cocaine Seeking in Rats. J Pharmacol Exp Ther. 2017 Sep;362(3):378-384. [3]. Satat K, et al. Evaluation of cebranopadol, a dually acting nociceptin/orphanin FQ and opioid receptor agonist in mouse models of acute, tonic, and chemotherapy-induced neuropathic pain. Inflammopharmacology. 2017 Oct 25 |
| Molecular Formula |
C24H27FN2O
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| Molecular Weight |
378.49
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| CAS # |
863513-91-1
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| Related CAS # |
Cebranopadol ((1α,4α)stereoisomer);863513-93-3
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| SMILES |
CN(C)[C@]1(C2=CC=CC=C2)CC[C@]3(C(N4)=C(CCO3)C5=C4C=CC(F)=C5)CC1
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 0.67 mg/mL (1.77 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 0.67 mg/mL (1.77 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.67 mg/mL (1.77 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6421 mL | 13.2104 mL | 26.4208 mL | |
| 5 mM | 0.5284 mL | 2.6421 mL | 5.2842 mL | |
| 10 mM | 0.2642 mL | 1.3210 mL | 2.6421 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(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.
Duration of action of cebranopadol (12µg/kg) compared with fentanyl (9.4µg/kg) and morphine (1.9 mg/kg) after intravenous administration in the rat tail-flick test.J Pharmacol Exp Ther.2014 Jun;349(3):535-48. |
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Analgesic effect of cebranopadol on spinal nerve ligation-induced mononeuropathic pain (SNL) and complete Freund’s adjuvant-induced chronic rheumatoid arthritic pain (CFA) 30 minutes after, and on tail flick-induced heat nociception (TF) 20 minutes after intravenous administration.J Pharmacol Exp Ther.2014 Jun;349(3):535-48. |
Effect of intravenous cebranopadol on mechanical sensitivity in the ipsilateral and contralateral paws in a rat model of bone cancer pain.J Pharmacol Exp Ther.2014 Jun;349(3):535-48. |
Antihyperalgesic activity of cebranopadol in streptozotocin (STZ)-treated and control rats measured as % MPE (mean ± S.E.M.;n= 10) by means of a paw pressure test in a model of STZ-induced diabetic polyneuropathy.J Pharmacol Exp Ther.2014 Jun;349(3):535-48. |
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Effect of 1.0, 2.15, and 4.64 mg/kg i.p. J-113397 on the antihypersensitive effect of 1.7μg/kg i.v. cebranopadol (A) and 8.9 mg/kg i.v. morphine (B) in the spinal nerve ligation (SNL) model. Effect of 0.3 and 1.0 mg/kg i.p. naloxone on the antihypersensitive effect of 1.7μg/kg i.v. cebranopadol (C) and of 0.1, 0.3, and 1.0 mg/kg i.p.naloxone on the antihypersensitive effect of 8.9 mg/kg i.v. morphine (D) in the SNL model. Data are given as percentage of maximum possible effect (mean ± S.E.M.;n= 10) measured with an electronic von Frey filament based on the measurement of ipsilateral withdrawal thresholds 30 minutes after administration of cebranopadol or morphine.J Pharmacol Exp Ther.2014 Jun;349(3):535-48. |
Antiallodynic effect of repeated daily intraperitoneal administration of cebranopadol or vehicle as measured by number of paw lifts from a cold plate during 2 minutes (mean ± S.E.M.;n= 13–15) (A) or % MPE (B) in the chronic constriction injury model.J Pharmacol Exp Ther.2014 Jun;349(3):535-48. |
Dose-dependent effects of cebranopadol (A) and morphine (B) on motor coordination in rats.J Pharmacol Exp Ther.2014 Jun;349(3):535-48. |
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Effects of cebranopadol (A and C) and morphine (B and D) on respiratory function in the whole-body plethysmography test in conscious rats.J Pharmacol Exp Ther.2014 Jun;349(3):535-48. |
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