General
Preferred name
ROSIGLITAZONE
Synonyms
ROSIGLITAZONE MALEATE ()
BRL-49653 HCl ()
Rosiglitazone HCl ()
BRL49653 ()
BRL 49653C ()
BRL 49653 ()
Rosiglitazone Hydrochloride ()
Rosiglitazone (BRL-49653) ()
Rosiglitazone XR ()
Rosiglitazone (maleate) ()
Rosiglitazone (hydrochloride) ()
BRL 49653 (hydrochloride) ()
BRL-49653C ()
Rosiglitazone potassium salt ()
Rosiglitazone (BRL-49653) maleate ()
Rosiglitazone (BRL 49653) ()
Rosiglitazone (BRL-49653) HCl ()
Rosiglitazone (potassium salt) ()
Rosiglitazone-d3 ()
Avandia ()
Rosiglitazone maleate component of avandaryl ()
BRL-49653-C ()
Rosiglitazone maleate component of avandamet ()
NSC-717764 ()
Rosiglitzazone maleate ()
ROSVEL ()
Venvia ()
Avandaryl ()
REZULT ()
NSC-758698 ()
TDZ-01 ()
Nyracta ()
ROSIGLITAZONA ()
ROSIGLIZOLE ()
Avandamet ()
BRL-49653 ()
GAUDIL ()
NYRACTA ()
VENVIA ()
P&D ID
PD010041
CAS
155141-29-0
1217260-35-9
122320-73-4
302543-62-0
316371-84-3
1132641-22-5
Tags
available
drug
Approved by
FDA
First approval
1999
Drug indication
HIV infection
diabetes mellitus
Type 2 diabetes
Type-2 diabetes
Alzheimer disease
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withdrawn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)
DESCRIPTION
Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARĀ¦Ć, with EC50s of 30 nM, 100 nM and 60 nM for PPARĀ¦Ć1, PPARĀ¦Ć2, and PPARĀ¦Ć, respectively, and a Kd of appr 40 nM for PPARĀ¦Ć; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).
PRICE
29
PRICE
29
DESCRIPTION
Rosiglitazone (BRL 49653) is an orally active selective PPARĀ¦Ć agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone is an TRPC5 activator (EC50: 30 Ā¦ĆM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer[1][2][4][7].
DESCRIPTION
Rosiglitazone (BRL49653) is a PPAR?? agonist, TRPC5 activator, and TRPM3 inhibitor with oral activity. Rosiglitazone is also a hypoglycemic agent and a thiazolidinedione insulin sensitizer.
PRICE
29
DESCRIPTION
Rosiglitazone (BRL 49653) hydrochloride is an orally active selective PPARĀ¦Ć agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone hydrochloride is a TRPC5 activator (EC50: 30 Ā¦ĆM) and TRPM3 inhibitor. Rosiglitazone hydrochloride can be used in the research of obesity and diabetes, senescence, ovarian cancer[1][2][4][7].
DESCRIPTION
Rosiglitazone is used to maintain glycemic control in type 2 diabetes.
(Enamine Bioactive Compounds)
DESCRIPTION
Rosiglitazone maleate (BRL 49653) is the maleate salt of rosiglitazone, an orally-active thiazolidinedione with antidiabetic properties and potential antineoplastic activity.
(TargetMol Bioactive Compound Library)
DESCRIPTION
Pregnane X receptor agonist; antibiotic
(Tocris Bioactive Compound Library)
DESCRIPTION
Potent and selective PPARgamma agonist; antidiabetic agent.
(Tocriscreen Plus)
DESCRIPTION
Rosiglitazone is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Rosiglitazone (BRL49653) is a PPARĪ³ agonist, TRPC5 activator, and TRPM3 inhibitor with oral activity. Rosiglitazone is also a hypoglycemic agent and a thiazolidinedione insulin sensitizer.
(TargetMol Bioactive Compound Library)
DESCRIPTION
Rosiglitazone is an agonist of peroxisome proliferator-activated receptor Ī³ (PPARĪ³) that binds to PPARĪ³ and sensitizes its response to insulin. It has been indicated for the treatment of type 2 diabetes, however, its application was restricted for increasing the risk of heart failure.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Rosiglitazone HCl is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Rosiglitazone hydrochloride (BRL-49653 HCl) is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
10
Organisms
1
Compound Sets
39
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
CeMM library of unique drugs (CLOUD)
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
DrugMatrix
Enamine Bioactive Compounds
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
NCATS Inxight Approved Drugs
NIH Clinical Collections (NCC)
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
NURSA ligand set
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
The Spectrum Collection
Tocris Bioactive Compound Library
Tocriscreen Plus
Withdrawn 2.0
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
98
Molecular Weight
357.11
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
1
Rotatable Bonds
7
Ring Count
3
Aromatic Ring Count
2
cLogP
2.49
TPSA
71.53
Fraction CSP3
0.28
Chiral centers
1.0
Largest ring
6.0
QED
0.82
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
Peroxisome proliferator-activated receptor gamma
PPAR? agonist
Ferroptosis
PPAR
TRP Channel
Autophagy,Ferroptosis,PPAR,TRP Channel
PPARĪ³
Target Type
Nuclear Receptors
MOA
peroxisome proliferator-activated receptor agonist
Agonist
Insulin Sensitizers
PPARgamma Agonists
Primary Target
PPAR?
Member status
member
ATC
A10BG02
Toxicity type
cardiovascular
Pathway
Apoptosis
Autophagy
DNA Damage/DNA Repair
Membrane Transporter/Ion Channel
Metabolism
Cell Cycle/DNA Damage
Metabolic Enzyme/Protease
Neuronal Signaling
Vitamin D Related/Nuclear Receptor
Recommended Cell Concentration
1 uM
Source data
