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863513-91-1 (Cebranopadol)

1

Identification

Cebranopadol Cebranopadol
Name Cebranopadol
Formula C24H27FN2O
MW 378.48
CAS No. 863513-91-1
EINECS
Smiles CN(C)[[email protected]]1(C2=CC=CC=C2)CC[[email protected]]3(C(N4)=C(CCO3)C5=C4C=CC(F)=C5)CC1
Synonyms GRT-6005;GRT 6005;GRT6005; (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
InChI InChI=1S/C24H27FN2O/c1-27(2)23(17-6-4-3-5-7-17)11-13-24(14-12-23)22-19(10-15-28-24)20-16-18(25)8-9-21(20)26-22/h3-9,16,26H,10-15H2,1-2H3/t23-,24-
2

Introduction

Cebranopadol(GRT-6005) is a novel first in class compounds with potent agonist activity on ORL-1 (opioid receptor like -1) and the well established mu opioid receptor. IC50 Value: Target:ORL-1 Cebranopadol and GRT 6006 are novel first-in-class compounds with unique pharmacological and pharmacokinetic profiles that may enhance their effect in certain pain conditions.

Background Information

Cebranopadol(GRT-6005) is a novel first in class compounds with potent agonist activity on ORL-1 (opioid receptor like -1) and the well established mu opioid receptor. IC50 Value: Target:ORL-1 Cebranopadol and GRT 6006 are novel first-in-class compounds with unique pharmacological and pharmacokinetic profiles that may enhance their effect in certain pain conditions. The unique mode of action of these compounds builds on the ORL-1 receptor and, supported by the established mu opioid receptor, is particularly suitable for the treatment of moderate to severe chronic pain [1]. in vitro: in vivo: Clinical trial: 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. ......by MedChemexpress Co., Ltd.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance:Light yellow to yellow solid EBNumber:EB000017153

Storage condition

Solubility

DMSO by MedChemexpress Co., Ltd.
5

Mechanism and Indication

6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Cebranopadol Grunenthal GmbH Cancer pain 2013/11/30 2016/4/30 Phase 3 Clinical
Cebranopadol Grunenthal GmbH Pain 2011/5/31 2011/12/31 Phase 2 Clinical
Cebranopadol Grunenthal GmbH Neuropathic pain 2011/5/31 2012/1/31 Phase 2 Clinical
Cebranopadol Grunenthal GmbH Diabetic neuropathy 2009/4/30 2010/5/1 Phase 2 Clinical
Cebranopadol Grunenthal GmbH Pain 2009/3/31 2009/10/31 Phase 2 Clinical
Cebranopadol - Phase 3
7

Safety Data of Cebranopadol

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
Aladdin 50mg/RMB13531() China
Apexbio Technology LLC 5mg/USD261() USA
CHEMSCENE, LLC USA
DC Chemicals 100mg/USD1100(In stock) China
MedChemexpress Co., Ltd. 5mg/USD260(In stock);10mg/USD336(In stock);50mg/USD906(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD260(In stock);10mg/USD336(In stock);50mg/USD906(In stock);200mg/USD2056(In stock) China
10

Related Products

Other Forms of 863513-91-1

Name CAS No Formula MW
Spiro[cyclohexane-1,1'(3'H)-pyrano[3,4-b]indol]-4-amine, 6'-fluoro-4',9'-dihydro-N,N-dimethyl-4-phenyl-, cis- (9CI) 863513-93-3 C24H27FN2O 378.48

Recommended Compounds in Opioid Receptor

Name CAS No Formula MW
Eluxadoline 864821-90-9 C32H35N5O5 569.65
Sufentanil (citrate) 60561-17-3 C28H38N2O9S 578.67
Buprenorphine (hydrochloride) 53152-21-9 C29H42ClNO4 504.1
Oxymorphone 76-41-5 C17H19NO4 301.34
TRV 130 1401028-24-7 C22H30N2O2S 386.55
Loperamide (hydrochloride) 34552-83-5 C29H34Cl2N2O2 513.5
Trimebutine 39133-31-8 C22H29NO5 387.47
Meptazinol (hydrochloride) 59263-76-2 C15H24ClNO 269.81
Alvimopan (dihydrate) 170098-38-1 C25H36N2O6 460.56
LY2795050 1346133-08-1 C23H22ClN3O2 407.89
Spiro[cyclohexane-1,1'(3'H)-pyrano[3,4-b]indol]-4-amine, 6'-fluoro-4',9'-dihydro-N,N-dimethyl-4-phenyl-, cis- (9CI) 863513-93-3 C24H27FN2O 378.48
Matrine 519-02-8 C15H24N2O 248.36
Naloxone (hydrochloride) 357-08-4 C19H22ClNO4 363.84
Sufentanil 56030-54-7 C22H30N2O2S 386.55
Methylnaltrexone (Bromide) 73232-52-7 C21H26BrNO4 436.34
Tapentadol 175591-23-8 C14H23NO 221.34
Tapentadol (hydrochloride) 175591-09-0 C14H24ClNO 257.8
Naltrexone 16590-41-3 C20H23NO4 341.4
Naltrexone (Hydrochloride) 16676-29-2 C20H24ClNO4 377.86
Alvimopan (monohydrate) 1383577-62-5 C25H34N2O5 442.55

Recommended Compounds in Same Indication

Name CAS No Formula MW
Tropisetron 89565-68-4 C17H20N2O2 284.35
Capsaicin 404-86-4 C18H27NO3 305.41
Etodolac 41340-25-4 C17H21NO3 287.35
Sufentanil 56030-54-7 C22H30N2O2S 386.55
PH-797804 586379-66-0 C22H19BrF2N2O3 477.3
TRO 19622 22033-87-0 C27H45NO 399.65
Gabapentin (hydrochloride) 60142-95-2 C9H18ClNO2 207.7
ADL-5859 850173-95-4 C24H29ClN2O3 428.95
Gabapentin 60142-96-3 C9H17NO2 171.24
Sufentanil (citrate) 60561-17-3 C28H38N2O9S 578.67
Nepafenac 78281-72-8 C15H14N2O2 254.28
Celecoxib 169590-42-5 C17H14F3N3O2S 381.37
Atomoxetine (hydrochloride) 82248-59-7 C17H22ClNO 291.82
Diazepam 439-14-5 C16H13ClN2O 284.74
Naloxone (hydrochloride) 357-08-4 C19H22ClNO4 363.84
Ranirestat 147254-64-6 C17H11BrFN3O4 420.19
Etoricoxib 202409-33-4 C18H15ClN2O2S 358.84
Pregabalin 148553-50-8 C8H17NO2 159.23
Rofecoxib 162011-90-7 C17H14O4S 314.36
Tapentadol (hydrochloride) 175591-09-0 C14H24ClNO 257.8
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Route of Synthesis

12

References

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More Information

Cebranopadol

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