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Cebranopadol

Cat. No. M5065
Cebranopadol Structure
Synonym:

GRT-6005

Size Price Availability Quantity
10mM*1mL USD 220  USD220 In stock
2mg USD 180  USD180 In stock
5mg USD 270  USD270 In stock
10mg USD 350  USD350 In stock
50mg USD 930  USD930 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Cebranopadol has successfully completed initial proof-of-concept studies in nociceptive and neuropathic pain with further Phase II studies planned prior to initiation of Phase III studies.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 378.48
Formula C24H27FN2O
CAS Number 863513-91-1
Purity >98%
Solubility 10 mM in DMSO
Storage at -20°C
References

[1] Kinga Sałat, et al. Cebranopadol : a first-in-class potent analgesic agent with agonistic activity at nociceptin/orphanin FQ and opioid receptors

[2] Huimei Wei, et al. Cebranopadol reduces cocaine self-administration in male rats: Dose, treatment and safety consideration

[3] R B Raffa, et al. Cebranopadol: novel dual opioid/NOP receptor agonist analgesic

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