Compounds > chiglitazar
Page last updated: 2024-11-13

chiglitazar

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

chiglitazar: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID71402018
CHEMBL ID4650349
SCHEMBL ID22607975
MeSH IDM0504924

Synonyms (24)

Synonym
chiglitazar
cs 038
e6ejv1j6y0 ,
unii-e6ejv1j6y0
743438-45-1
l-tyrosine, o-[2-(9h-carbazol-9-yl)ethyl]-n-[2-(4-fluorobenzoyl)phenyl]-
DTXSID00225352
CS-038 ,
cs038
CS-0025471
HY-106266
o-(2-(9h-carbazol-9-yl)ethyl)-n-(2-(4-fluorobenzoyl)phenyl)-l-tyrosine
l-tyrosine, o-(2-(9h-carbazol-9-yl)ethyl)-n-(2-(4-fluorobenzoyl)phenyl)-
carfloglitazar, (s)-
(2s)-3-(4-(2-carbazol-9-ylethoxy)phenyl)-2-(2-(4-fluorobenzoyl)anilino)propanoic acid
bilessglu
gtpl12287
MS-30324
SCHEMBL22607975
(2s)-3-[4-(2-carbazol-9-ylethoxy)phenyl]-2-[2-(4-fluorobenzoyl)anilino]propanoic acid
CHEMBL4650349
GLXC-26864
3-[4-(2-carbazol-9-ylethoxy)phenyl]-2-[2-(4-fluorobenzoyl)anilino]propanoic acid
AKOS040741545

Research Excerpts

Overview

Chiglitazar is a dual alpha/gamma peroxisome proliferator-activated receptor (PPAR) agonist.

ExcerptReferenceRelevance
"2. Chiglitazar is a PPARalpha/gamma dual agonist."( The PPARalpha/gamma dual agonist chiglitazar improves insulin resistance and dyslipidemia in MSG obese rats.
Chen, YT; Li, PP; Liu, Q; Lu, XP; Ning, ZQ; Shan, S; Shen, ZF; Sun, SJ; Xie, MZ, 2006)		1.13
"Chiglitazar is a dual alpha/gamma peroxisome proliferator-activated receptor (PPAR) agonist. "( Determination of chiglitazar, a dual alpha/gamma peroxisome proliferator-activated receptor (PPAR) agonist, in human plasma by liquid chromatography-tandem mass spectrometry.
Chen, WL; Chu, NN; Li, XN; Xu, HR, 2007)		2.12

Treatment

ExcerptReferenceRelevance
"Treatment with chiglitazar blocked the ubiquitination of PPARα and increased its expression, resulting in the inhibition of glucose metabolism and apoptosis of AML cells."( Therapeutic inhibition of PPARα-HIF1α-PGK1 signaling targets leukemia stem and progenitor cells in acute myeloid leukemia.
Deng, M; Fang, Z; Huang, Y; Jiang, Y; Lai, Q; Luo, Y; Pan, G; Qin, D; Tan, J; Tang, Y; Xie, C; Xu, B; Zha, J; Zhao, H; Zhong, M; Zhou, H; Zhou, Y, 2023)		1.25

Pharmacokinetics

ExcerptReferenceRelevance
"To develop and validate a novel precolumn derivatization method for the quantitative determination and pharmacokinetic application of acetylshikonin in macaque monkeys by liquid chromatography-electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS)."( Quantitative determination of acetylshikonin in macaque monkey blood by LC-ESI-MS/MS after precolumn derivatization with 2-mercaptoethanol and its application in pharmacokinetic study.
Dou, GF; Du, A; Gu, RL; Meng, ZY; Sun, DX; Tian, HF; Wu, ZN; Yuan, D, 2008)		0.35
" After the administration of acetylshikonin (80 mg/kg, po) in macaque monkeys, the pharmacokinetic parameters were obtained through the non-compartmental analysis, where the area under the concentration-time curve to the last measurable concentration, the terminal elimination halflife, and the mean residual time were 615."( Quantitative determination of acetylshikonin in macaque monkey blood by LC-ESI-MS/MS after precolumn derivatization with 2-mercaptoethanol and its application in pharmacokinetic study.
Dou, GF; Du, A; Gu, RL; Meng, ZY; Sun, DX; Tian, HF; Wu, ZN; Yuan, D, 2008)		0.35
"The method was validated and applied to the quantitative determination and pharmacokinetic study of acetylshikonin in the blood samples of macaque monkeys."( Quantitative determination of acetylshikonin in macaque monkey blood by LC-ESI-MS/MS after precolumn derivatization with 2-mercaptoethanol and its application in pharmacokinetic study.
Dou, GF; Du, A; Gu, RL; Meng, ZY; Sun, DX; Tian, HF; Wu, ZN; Yuan, D, 2008)		0.35
" The validated LC-MS/MS method was successfully applied to the preliminary pharmacokinetic study in rats."( Quantitative determination of beta,beta-dimethylacrylshikonin (DASK) in rat whole blood by liquid chromatography-tandem mass spectrometry with pre-column derivation and its pharmacokinetic application.
Dou, G; Meng, Z; Sun, D; Tian, H; Yuan, D, 2009)		0.35
" The findings showed that the CYP3A4 inhibitor itraconazole had no apparent pharmacokinetic drug interaction with chiglitazar, whereas rifampicin did."( Pharmacokinetic Interaction of Chiglitazar with CYP3A4 Inducer or Inhibitor: An Open-Label, Sequential Crossover, Self-Control, 3-Period Study in Healthy Chinese Volunteers.
Chen, H; Chen, W; Li, H; Li, J; Li, X; Liu, C; Sheng, L; Wu, Y; Xu, H; Yang, M; Yuan, F, 2023)		1.41

Dosage Studied

ExcerptRelevanceReference
" A single-center, open-label, sequential crossover, and self-control study was carried out in 24 healthy subjects to determine the pharmacokinetics of chiglitazar dosed with and without CYP3A4 inhibitors and inducers."( Pharmacokinetic Interaction of Chiglitazar with CYP3A4 Inducer or Inhibitor: An Open-Label, Sequential Crossover, Self-Control, 3-Period Study in Healthy Chinese Volunteers.
Chen, H; Chen, W; Li, H; Li, J; Li, X; Liu, C; Sheng, L; Wu, Y; Xu, H; Yang, M; Yuan, F, 2023)		1.4
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (14)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (28.57)29.6817
2010's0 (0.00)24.3611
2020's10 (71.43)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 31.96

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index31.96 (24.57)
Research Supply Index3.04 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index37.86 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (31.96)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials5 (33.33%)5.53%
Reviews1 (6.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other9 (60.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
mercaptoethanol
Mercaptoethanol: A water-soluble thiol derived from hydrogen sulfide and ethanol. It is used as a reducing agent for disulfide bonds and to protect sulfhydryl groups from oxidation.		2.0410alkanethiol;
primary alcohol		geroprotector
pioglitazone
Pioglitazone: A thiazolidinedione and PPAR GAMMA agonist that is used in the treatment of TYPE 2 DIABETES MELLITUS.. pioglitazone : A member of the class of thiazolidenediones that is 1,3-thiazolidine-2,4-dione substituted by a benzyl group at position 5 which in turn is substituted by a 2-(5-ethylpyridin-2-yl)ethoxy group at position 4 of the phenyl ring. It exhibits hypoglycemic activity.		2.0310aromatic ether;
pyridines;
thiazolidinediones		antidepressant;
cardioprotective agent;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
geroprotector;
hypoglycemic agent;
insulin-sensitizing drug;
PPARgamma agonist;
xenobiotic
pirinixic acid
pirinixic acid: structure		2.0310aryl sulfide;
organochlorine compound;
pyrimidines
rosiglitazone
[no description available]		2.0310aminopyridine;
thiazolidinediones		EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
insulin-sensitizing drug
acetylshikonin
acetylshikonin: from roots of Boraginacea; RN given refers to cpd without isomeric designation		2.0410
naphthoquinones
Naphthoquinones: Naphthalene rings which contain two ketone moieties in any position. They can be substituted in any position except at the ketone groups.		2.0510
sitagliptin phosphate
Sitagliptin Phosphate: A pyrazine-derived DIPEPTIDYL-PEPTIDASE IV INHIBITOR and HYPOGLYCEMIC AGENT that increases the levels of the INCRETIN hormones GLUCAGON-LIKE PEPTIDE-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). It is used in the treatment of TYPE 2 DIABETES.		6.7633
sodium glutamate
Sodium Glutamate: One of the FLAVORING AGENTS used to impart a meat-like flavor.. monosodium glutamate : An organic sodium salt that is the monosodium salt of glutamic acid.		2.0310monosodium glutamateflavouring agent
abt-199
venetoclax: A BCL-2 inhibitor with antineoplastic activity that is used in the treatment of CHRONIC LYMPHOCYTIC LEUKEMIA associated with chromosome 17p deletion; structure in first source.. venetoclax : A member of the class of pyrrolopyridines that is a potent inhibitor of the antiapoptotic protein B-cell lymphoma 2. It is used for treamtment of chronic lymphocytic leukemia with 17p deletion.		2.610aromatic ether;
C-nitro compound;
monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
N-sulfonylcarboxamide;
oxanes;
pyrrolopyridine		antineoplastic agent;
apoptosis inducer;
B-cell lymphoma 2 inhibitor
rifampin
Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)		2.610cyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion		angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor
beta, beta-dimethylacrylshikonin
beta, beta-dimethylacrylshikonin: RN given refers to unspecified stereoisomer; structure given in first source		2.0510
ConditionIndicatedRelationship StrengthStudiesTrials
Diabetes Mellitus, Adult-Onset
[description not available]		0965
Diabetes Mellitus, Type 2
A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.		11165
Insulin Sensitivity
[description not available]		05.732
Insulin Resistance
Diminished effectiveness of INSULIN in lowering blood sugar levels: requiring the use of 200 units or more of insulin per day to prevent HYPERGLYCEMIA or KETOSIS.		05.732
Acute Myelogenous Leukemia
[description not available]		04.2190
Leukemia, Myeloid, Acute
Clonal expansion of myeloid blasts in bone marrow, blood, and other tissue. Myeloid leukemias develop from changes in cells that normally produce NEUTROPHILS; BASOPHILS; EOSINOPHILS; and MONOCYTES.		04.2190
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.5120
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		02.0410
Dyslipidemia
[description not available]		07.0310
Obesity
A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).		02.0310
Dyslipidemias
Abnormalities in the serum levels of LIPIDS, including overproduction or deficiency. Abnormal serum lipid profiles may include high total CHOLESTEROL, high TRIGLYCERIDES, low HIGH DENSITY LIPOPROTEIN CHOLESTEROL, and elevated LOW DENSITY LIPOPROTEIN CHOLESTEROL.		02.0310