General
Preferred name
TROGLITAZONE
Synonyms
CS-045 ()
Romozin ()
Rezulin ()
Romglizone ()
Noscal ()
Prelay ()
Rezulin, Romglizone, Prelay, Romozin ()
Troglitazone (CS-045) ()
GR-92132X ()
Gr92132X ()
Troglitazona ()
CI-991 ()
Troglitazone-d4 ()
P&D ID
PD009121
CAS
97322-87-7
2749370-85-0
Tags
available
drug
Approved by
FDA
First approval
1997
Drug indication
diabetes mellitus
Diabetic complication
Drug Status
approved
withdrawn
investigational
Max Phase
4.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
MOA
Troglitazone is a thiazolidinedione antidiabetic agent that lowers blood glucose by improving target cell response to insulin. It has a unique mechanism of action that is dependent on the presence of insulin for activity. Troglitazone decreases hepatic glucose output and increases insulin dependent glucose disposal in skeletal muscle. Its mechanism of action is thought to involve binding to nuclear receptors (PPAR) that regulate the transcription of a number of insulin responsive genes critical for the control of glucose and lipid metabolism. Troglitazone is a ligand to both PPARα and PPARγ, with a highter affinity for PPARγ. The drug also contains an α-tocopheroyl moiety, potentially giving it vitamin E-like activity. Troglitazone has been shown to reduce inflammation, and is associated with a decrase in nuclear factor kappa-B (NF-κB) and a concomitant increase in its inhibitor (IκB). Unlike sulfonylureas, troglitazone is not an insulin secretagogue.
DESCRIPTION
Troglitazone is an antidiabetic and anti-inflammatory drug.
(GtoPdb)
DESCRIPTION
Troglitazone is an orally active PPAR¦Ã agonist, with EC50s of 550 nM and 780 nM for human and murine?PPAR¦Ã receptor, respectively. Troglitazone has anticancer activity, prevents and inhibits the development of type 2 diabetes.
PRICE
82
DESCRIPTION
Troglitazone (Romglizone) is a PPAR?? agonist with anti-inflammatory and anti-tumor activity.
DESCRIPTION
Potent and selective RXRalpha agonist
(Tocris Bioactive Compound Library)
DESCRIPTION
Selective PPARgamma agonist; antidiabetic agent
(Tocriscreen Plus)
DESCRIPTION
Troglitazone, PPARγ agonist, is an anti-diabetic thiazolidinedione (TZD) with anti-inflammatory and anti-tumor activity, which was approved for the treatment of insulin resistance and hyperglycemia in Type II diabetes, but was withdrawn from the market due to hepatotoxicity. It binds to the PPARγ ligand-binding domain (LBD) but fails to induce interaction of the PPARγ LBD with the transcriptional coactivators SRC-1, TIF2, AIB1, p300, or TRAP220. It also induces cell cycle arrest and apoptosis in several cancer cell lines. It displays no activity at PPARα or PPARδ receptors and displays anti-invasive effect on human breast cancer cells. It also inhibits cell growth of hematopoietic cell lines and inhibits lamellipodia formation and actin polymerization.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Troglitazone (Romglizone) is a PPARγ agonist with anti-inflammatory and anti-tumor activity.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
12
Organisms
5
Compound Sets
30
AdooQ Bioactive Compound Library
BOC Sciences Bioactive Compounds
ChEMBL Approved Drugs
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CZ-OPENSCREEN Bioactive Library
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
DrugMatrix
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
NURSA ligand set
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
Withdrawn 2.0
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
39
Molecular Weight
441.16
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
2
Rotatable Bonds
5
Ring Count
4
Aromatic Ring Count
2
cLogP
4.37
TPSA
84.86
Fraction CSP3
0.42
Chiral centers
2.0
Largest ring
6.0
QED
0.72
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
Nuclear Receptors
Pathway
Apoptosis
Autophagy
DNA Damage/DNA Repair
Metabolism
Cell Cycle/DNA Damage
Metabolic Enzyme/Protease
Vitamin D Related/Nuclear Receptor
Primary Target
PPAR?
MOA
Agonist
Insulin Sensitizers
PPARgamma Agonists
CCL2 Expression Inhibitors
EGR1 Expression Enhancers
Member status
member
ATC
A10BG01
Toxicity type
hepatic
Target
Ferroptosis
PPAR
Apoptosis related,Autophagy,Ferroptosis,PPAR
PPARγ
Therapeutic Class
Antiinflammatory Agents
Source data
