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Details

Stereochemistry ACHIRAL
Molecular Formula C19H14N2O2S
Molecular Weight 334.392
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TIDEGLUSIB

SMILES

O=C1SN(C(=O)N1CC2=CC=CC=C2)C3=CC=CC4=CC=CC=C34

InChI

InChIKey=PMJIHLSCWIDGMD-UHFFFAOYSA-N
InChI=1S/C19H14N2O2S/c22-18-20(13-14-7-2-1-3-8-14)19(23)24-21(18)17-12-6-10-15-9-4-5-11-16(15)17/h1-12H,13H2

HIDE SMILES / InChI
Molecular Formula C19H14N2O2S
Molecular Weight 334.392
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

Tideglusib (NP031112, NP-12, Nypta, Noscira SA, Madrid, Spain), a drug, which belongs to the thiadiazolidinone family, is a GSK-3β inhibitor. Tideglusib was in phase II clinical trials for the treatment of Alzheimer disease (AD) and progressive supranuclear palsy. Participants showed no benefit on either of the primary outcome measures or exploratory endpoints and further development in the drug was halted for these two disease. However, Tideglusib is on phase II clinical trial to determine whether drug is safe and efficacious in the treatment of adolescents and adults with congenital and juvenile-onset Myotonic Dystrophy.

Originator

Approval Year

Unknown
149124
Targets

Targets

Primary TargetPharmacologyConditionPotency
Glycogen synthase kinase-3 beta
52
Target ID: P49841
Gene ID: 2932.0
Gene Symbol: GSK3B
Target Organism: Homo sapiens (Human)
Inhibitor
8504
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Phase II
1147
Unknown

Approved Use

Unknown
Primary
Phase II
1147
Unknown

Approved Use

Unknown
Primary
Phase II
1147
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
513.54 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/32942085/
400 mg 1 times / day multiple, oral
dose: 400 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TIDEGLUSIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1170.95 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/32942085/
1000 mg 1 times / day multiple, oral
dose: 1000 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TIDEGLUSIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
1365.54 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/32942085/
400 mg 1 times / day multiple, oral
dose: 400 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TIDEGLUSIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
3398.68 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/32942085/
1000 mg 1 times / day multiple, oral
dose: 1000 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TIDEGLUSIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
2.05 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/32942085/
400 mg 1 times / day multiple, oral
dose: 400 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TIDEGLUSIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1.7 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/32942085/
1000 mg 1 times / day multiple, oral
dose: 1000 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TIDEGLUSIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Sourcing

Sourcing

Vendor/AggregatorIDURL
1PlusChem LLC
1P0036M4
https://www.1pchem.com/search?query=1P0036M4
AChemBlock
O32866
http://www.achemblock.com/catalogsearch/result/?q=O32866
AK Scientific
X5395
https://aksci.com/item_detail.php?cat=X5395
Angene
AGN-PC-006L53
http://www.angenechemical.com/productshow/AGN-PC-006L53.html
AOBIOUS INC
AOB5562
http://aobious.com/aobious/search?search_query=AOB5562
ApexBio Technology
B1539
https://www.apexbt.com/catalogsearch/result/?q=B1539
AstaTech
40613
http://astatechinc.com/CPSResult.php?CRNO=40613
BLD Pharm
BD306015
http://www.bldpharm.com/search/Search.html?keyword=BD306015
BOC Sciences
865854-05-3
http://www.bocsci.com/description.asp?cas=865854-05-3
Cayman Chemical
16727
http://www.caymanchem.com/app/template/Product.vm/catalog/16727
Chem Scene
CS-0613
http://www.chemscene.com/goproductList/searchProductList?productObj=CS-0613
ChemShuttle
104792
https://www.chemshuttle.com/catalogsearch/result/?q=104792
Debye Scientific
DA-41071
https://www.debyesci.com/index.php?id=product&ext[cno]=DA-41071
eMolecules
44786343
https://orderbb.emolecules.com/search/#?query=44786343
eNovation Chemicals
D480521
https://www.enovationchem.com/Products.asp?SEARCHTEXT=D480521&searchbtn.x=0&searchbtn.y=0
Excenen
EX-A600
http://www.excenen.com/searchresultlist.php?id=EX-A600
KeyOrganics
AS-56156
http://www.keyorganicsinc.com/bionet/catalogsearch/result?q=AS-56156
Lab Network
LN01314805
https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01314805
Matrix Scientific
145196
http://www.matrixscientific.com/145196.html
mcule
MCULE-3900652558
https://mcule.com/MCULE-3900652558/
MedChem Express
HY-14872
https://www.medchemexpress.com/search.html?q=HY-14872&ft=&fa=&fp=
Molnova
M16292
https://www.molnova.com/en/serch-list.html?keywords=M16292
MolPort
MolPort-028-599-952
https://www.molport.com/shop/molecule-link/MolPort-028-599-952
MuseChem
I005208
https://www.musechem.com/product/I005208.html
Selleck Chemicals
S2823
http://www.selleckchem.com/search.html?searchDTO.searchParam=S2823
ShangHai Biochempartner
BCP000647
http://www.biochempartner.com/search_BCP000647
ShangHai Biochempartner
BCP06016
http://www.biochempartner.com/search_BCP06016
TargetMol
T3067
https://www.targetmol.com/search?keyword=T3067
Wonderchem
WC-009UNT
http://www.wonder-chem.com/search.html?text=WC-009UNT
PubMed

PubMed

TitleDatePubMed
Treatment of Alzheimer's disease with the GSK-3 inhibitor tideglusib: a pilot study.
2013
Evidence for irreversible inhibition of glycogen synthase kinase-3β by tideglusib.
2012-01-06
Exploring the binding sites of glycogen synthase kinase 3. Identification and characterization of allosteric modulation cavities.
2011-12-22
Switching reversibility to irreversibility in glycogen synthase kinase 3 inhibitors: clues for specific design of new compounds.
2011-06-23
Glycogen synthase kinase 3 inhibitors in the next horizon for Alzheimer's disease treatment.
2011
Patents

Patents

20050222220
1

Sample Use Guides

In Vivo Use Guide
1000 mg of tideglusib as a powder for oral suspension once every other day in an overnight fasted state for 26 weeks/extension
Route of Administration: Oral
In Vitro Use Guide
Tideglusib is an irreversible inhibitor of GSK-3β. The interaction of tideglusib with GSK-3β, binding studies with radioactive compound were performed. [35S]tideglusib (207 Bq/nmol) at 55 μM was incubated with 5 μM GSK-3β for 1 h at 25 °C in 315 μl of 50 mM Tris-HCl, pH 7.5, containing 150 mM NaCl and 0.1 mM EGTA.
Substance Class Chemical
Created
by admin
on Mon Mar 31 18:46:10 GMT 2025
Edited
by admin
on Mon Mar 31 18:46:10 GMT 2025
Record UNII
Q747Y6TT42
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
TIDEGLUSIB
INN   WHO-DD  
INN  
Official Name English
NP-031112
Preferred Name English
4-BENZYL-2-(A-NAPHTHYL)-1,2,4-THIADIAZOLIDINE-3,5-DIONE
Common Name English
NP-12
Code English
4-BENZYL-2-(A-NAPHTYL)-1,2,4-THIADIAZOLIDINE-3,5-DIONE
Common Name English
4-BENZYL-2-(NAPHTHALEN-1-YL)-1,2,4-THIADIAZOLIDINE-3,5-DIONE
Systematic Name English
tideglusib [INN]
Common Name English
NP031112
Code English
Tideglusib [WHO-DD]
Common Name English
Classification Tree Code System Code
EU-Orphan Drug EU/3/15/1452
Created by admin on Mon Mar 31 18:46:10 GMT 2025 , Edited by admin on Mon Mar 31 18:46:10 GMT 2025
FDA ORPHAN DRUG 290109
Created by admin on Mon Mar 31 18:46:10 GMT 2025 , Edited by admin on Mon Mar 31 18:46:10 GMT 2025
FDA ORPHAN DRUG 577417
Created by admin on Mon Mar 31 18:46:10 GMT 2025 , Edited by admin on Mon Mar 31 18:46:10 GMT 2025
NCI_THESAURUS C471
Created by admin on Mon Mar 31 18:46:10 GMT 2025 , Edited by admin on Mon Mar 31 18:46:10 GMT 2025
Code System Code Type Description
PUBCHEM
11313622
Created by admin on Mon Mar 31 18:46:10 GMT 2025 , Edited by admin on Mon Mar 31 18:46:10 GMT 2025
PRIMARY
DRUG BANK
DB12129
Created by admin on Mon Mar 31 18:46:10 GMT 2025 , Edited by admin on Mon Mar 31 18:46:10 GMT 2025
PRIMARY
EPA CompTox
DTXSID90235682
Created by admin on Mon Mar 31 18:46:10 GMT 2025 , Edited by admin on Mon Mar 31 18:46:10 GMT 2025
PRIMARY
SMS_ID
100000177254
Created by admin on Mon Mar 31 18:46:10 GMT 2025 , Edited by admin on Mon Mar 31 18:46:10 GMT 2025
PRIMARY
NCI_THESAURUS
C97364
Created by admin on Mon Mar 31 18:46:10 GMT 2025 , Edited by admin on Mon Mar 31 18:46:10 GMT 2025
PRIMARY
ChEMBL
CHEMBL3545157
Created by admin on Mon Mar 31 18:46:10 GMT 2025 , Edited by admin on Mon Mar 31 18:46:10 GMT 2025
PRIMARY
INN
9223
Created by admin on Mon Mar 31 18:46:10 GMT 2025 , Edited by admin on Mon Mar 31 18:46:10 GMT 2025
PRIMARY
FDA UNII
Q747Y6TT42
Created by admin on Mon Mar 31 18:46:10 GMT 2025 , Edited by admin on Mon Mar 31 18:46:10 GMT 2025
PRIMARY
CAS
865854-05-3
Created by admin on Mon Mar 31 18:46:10 GMT 2025 , Edited by admin on Mon Mar 31 18:46:10 GMT 2025
PRIMARY
WIKIPEDIA
Tideglusib
Created by admin on Mon Mar 31 18:46:10 GMT 2025 , Edited by admin on Mon Mar 31 18:46:10 GMT 2025
PRIMARY
CHEBI
147398
Created by admin on Mon Mar 31 18:46:10 GMT 2025 , Edited by admin on Mon Mar 31 18:46:10 GMT 2025
PRIMARY
Related Record Type Details
GLYCOGEN SYNTHASE KINASE-3 BETA
TARGET -> INHIBITOR
IRREVERSIBLE INHIBITOR
Related Record Type Details
Structure of TIDEGLUSIB
ACTIVE MOIETY
NIH
NCATS
PRIVACY NOTICE
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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