Cebranopadol -Biokitchen

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Cebranopadol

Time：2016-11-01

CAS#: 863513-91-1

Description: Cebranopadol, also known as GRT-6005, is a Opioid Receptor Agonist with agonistic activity at nociceptin/orphanin FQ and opioid receptors. Cebranopadol displays analgesic, antiallodynic and antihyperalgesic properties in several rat models of acute nociceptive, inflammatory, cancer and neuropathic pain. In contrast to classical opioids, it has a higher analgesic potency in models of neuropathic pain than in acute nociceptive pain. Even at higher analgesic doses, cebranopadol does not induce motor coordination deficits or respiratory depression in rats.

Synonym: GRT-6005; GRT 6005; GRT6005; Cebranopadol

IUPAC/Chemical Name: (1r,4r)-6′-fluoro-N,N-dimethyl-4-phenyl-4′,9′-dihydro-3’H-spiro[cyclohexane-1,1′-pyrano[3,4-b]indol]-4-amine

PRICE AND AVAILABILITY

Size Price

10mg Not available

100mg Not available

1g Ask price

10g Ask price

Cebranopadol, purity > 98%, is not in stock, may be available through custom synthesis. Minimum 1 gram order is requested. Current shipping out time is about 2 months after order is received.

THEORETICAL ANALYSIS

Name: Cebranopadol
CAS#: 863513-91-1
Chemical Formula: C24H27FN2O
Exact Mass: 378.2107
Molecular Weight: 378.4914
Elemental Analysis: C, 76.16; H, 7.19; F, 5.02; N, 7.40; O, 4.23

TECHNICAL DATA

Appearance:

Solid powder

Purity:

>98% (or refer to the Certificate of Analysis)

Shipping Condition:

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:

Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:

Soluble in DMSO, not in water

Shelf Life:

>2 years if stored properly

Drug Formulation:

This drug may be formulated in DMSO

Stock Solution Storage:

0 – 4 C for short term (days to weeks), or -20 C for long term (months).

ADDITIONAL INFORMATION

Related CAS#
863513-92-2 (Cebranopadol Hemicitrate)
863513-91-1 (Cebranopadol)

REFERENCES

1: Bird MF, Lambert DG. Simultaneous targeting of multiple opioid receptor types. Curr Opin Support Palliat Care. 2015 Jun;9(2):98-102. doi: 10.1097/SPC.0000000000000129. Review. PubMed PMID: 25872121.

2: Sałat K, Jakubowska A, Kulig K. Cebranopadol : a first-in-class potent analgesic agent with agonistic activity at nociceptin/orphanin FQ and opioid receptors. Expert Opin Investig Drugs. 2015 Jun;24(6):837-44. doi: 10.1517/13543784.2015.1036985. Epub 2015 Apr 12. Review. PubMed PMID: 25865744.

3: Lambert DG, Bird MF, Rowbotham DJ. Cebranopadol: a first in-class example of a nociceptin/orphanin FQ receptor and opioid receptor agonist. Br J Anaesth. 2015 Mar;114(3):364-6. doi: 10.1093/bja/aeu332. Epub 2014 Sep 23. PubMed PMID: 25248647.

4: Schunk S, Linz K, Hinze C, Frormann S, Oberbörsch S, Sundermann B, Zemolka S, Englberger W, Germann T, Christoph T, Kögel BY, Schröder W, Harlfinger S, Saunders D, Kless A, Schick H, Sonnenschein H. Discovery of a Potent Analgesic NOP and Opioid Receptor Agonist: Cebranopadol. ACS Med Chem Lett. 2014 Jun 24;5(8):857-62. doi: 10.1021/ml500117c. eCollection 2014 Aug 14. PubMed PMID: 25147603; PubMed Central PMCID: PMC4137374.

5: Linz K, Christoph T, Tzschentke TM, Koch T, Schiene K, Gautrois M, Schröder W, Kögel BY, Beier H, Englberger W, Schunk S, De Vry J, Jahnel U, Frosch S. Cebranopadol: a novel potent analgesic nociceptin/orphanin FQ peptide and opioid receptor agonist. J Pharmacol Exp Ther. 2014 Jun;349(3):535-48. doi: 10.1124/jpet.114.213694. Epub 2014 Apr 8. PubMed PMID: 24713140.

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