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AB141125

GW 9662, PPARgamma antagonist

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(11 Publications)

MW 276.67 Da, Purity >99%. Selective PPARγ antagonist (IC50 values are 3.3, 32, >1000 nM for PPARγ, PPARα and PPARδ respectively). Apoptotic and antimetastatic activity in vitro.

View Alternative Names

(R)-limonene 6-monooxygenase, (S)-limonene 6-monooxygenase, (S)-limonene 7-monooxygenase, ACLS, AHR_HUMAN, AI838772, AIS, ANDR_HUMAN, AR, AR8, AW493413, Ah receptor, Androgen nuclear receptor variant 2, Androgen receptor, Androgen receptor (dihydrotestosterone receptor; testicular feminization; spinal and bulbar muscular atrophy; Kennedy disease), Aromatic hydrocarbon receptor, Aryl hydrocarbon receptor, Aryl hydrocarbon receptor precursor, Atherosclerosis, susceptibility to, included, BXR, C-mpl ligand, CP2C9_HUMAN, CPC12, CPC8, CPC9, CPCJ, CYP2C, CYP2C10, CYPIIC9, Class E basic helix-loop-helix protein 76, Cytochrome P-450MP, Cytochrome P450 2C9, Cytochrome P450 MP-4, Cytochrome P450 MP-8, Cytochrome P450 PB-1, Cytochrome P450, family 2, subfamily C, polypeptide 9, DHTR, DKFZp686N23123, DNA binding protein, Dihydro testosterone receptor, Dihydrotestosterone receptor (DHTR), ER, ER-alpha, ER-beta, ERR a, ERR-alpha, ERR1 protein, ERR1_HUMAN, ER[a], ER[b], ESR, ESR B, ESR BETA, ESR1_HUMAN, ESRA, ESRL 1, ESRR A, ESTR B, Era, Erb, Erb2, Estr, Estra, Estradiol Receptor alpha, Estradiol Receptor beta, Estradiol receptor, Estrogen Receptor 1, Estrogen Receptor 2, Estrogen receptor, Estrogen receptor 1 (alpha), Estrogen receptor 2 (ER beta), Estrogen receptor 2 ER beta, Estrogen receptor alpha, Estrogen receptor beta 4, Estrogen receptor related 1, Estrogen receptor-like 1, Estrogen resistance, included, Estrogen-related receptor alpha, Estrra, FLJ11090, GCPS, GLI Kruppel family member GLI 3, GLI Kruppel family member GLI3 (Greig cephalopolysyndactyly syndrome), GLI family zinc finger 3, GLI3 C-terminally truncated form, GLI3 form of 190 kDa, GLI3 form of 83 kDa, GLI3 full length protein, GLI3-190, GLI3-83, GLI3FL, GLI3_HUMAN, Glioma associated oncogene family zinc finger 3, HDL cholesterol, augmented response of, to hormone replacement, included, HGNC:348, HUMARA, HYSP1, KD, Kennedy disease (KD), MGC104252, MGC112732, MGC149605, MGC88320, MGDF, MKCSF, MPL ligand, MPLLG, Megakaryocyte colony-stimulating factor, Megakaryocyte growth and development factor, Megakaryocyte stimulating factor, Microsomal monooxygenase, Myeloproliferative leukemia virus oncogene ligand, Myocardial infarction, susceptibility to, included, NF-E2-related factor 2, NF2L2_HUMAN, NR1B1, NR1C3, NR1I2_HUMAN, NR3A1, NR3A2, NR3B1, NR3C4, NRF2, Nfe2l2, Nuclear factor, Nuclear factor (erythroid derived 2) like 2, Nuclear factor erythroid 2-related factor 2, Nuclear factor erythroid derived 2 like 2, Nuclear mitotic apparatus protein retinoic acid receptor alpha fusion protein, Nuclear receptor subfamily 1 group B member 1, Nuclear receptor subfamily 1 group C member 3, Nuclear receptor subfamily 1 group I member 2, Nuclear receptor subfamily 3 group A member 1, Nuclear receptor subfamily 3 group A member 2, Nuclear receptor subfamily 3 group B member 1, Nuclear receptor subfamily 3 group C member 4, Nuclear receptor subfamily 3 group C member 4 (NR3C4), Nucleophosmin retinoic acid receptor alpha fusion protein NPM RAR long form, ONR 1, OTTHUMP00000017718, OTTHUMP00000017719, OTTHUMP00000020135, OTTHUMP00000215173, OTTHUMP00000215174, OTTHUMP00000215175, Oncogene GLI3, Orphan nuclear receptor PAR 1, Orphan nuclear receptor PXR, P450 MP, P450 PB 1, P450C2C, P450IIC19, P450IIC9, PAP A, PAPB, PAR, PAR q, PPAR-gamma, PPARG2, PPARG_HUMAN, PPD IV, PRR, Peroxisome proliferator activated receptor gamma 2, Peroxisome proliferator-activated receptor gamma, Pregnane X receptor, RAR, RAR-alpha, RARA_HUMAN, RARalpha1, RNESTROR, RP24-311F12.2, Retinoic acid nuclear receptor alpha variant 1, Retinoic acid nuclear receptor alpha variant 2, Retinoic acid receptor alpha, Retinoic acid receptor alpha polypeptide, S-mephenytoin 4-hydroxylase, SBMA, SCAN1, SMAX1, SXR, Spinal and bulbar muscular atrophy, Spinal and bulbar muscular atrophy (SBMA), Steroid and xenobiotic receptor, Steroid hormone receptor ERR1, TFM, THCYT1, TYDP, TYDP1_HUMAN, Testicular Feminization (TFM), Thrombopoietin, Thrombopoietin nirs variant 1, Transcriptional activator GLI3, Transcriptional repressor GLI3R, Tyr-DNA phosphodiesterase 1, Tyrosyl-DNA phosphodiesterase 1, Xenobiotic monooxygenase, Zinc finger protein GLI 3, androgen receptor splice variant 4b, bHLHe76, cytochrome P-450 S-mephenytoin 4-hydroxylase, erythroid derived 2, estrogen receptor related receptor alpha, flavoprotein-linked monooxygenase, hERR1, like 2, nuclear factor erythroid 2 like 2, pregnane X nuclear receptor variant 2

1 Images
Chemical Structure - GW 9662, PPARgamma antagonist (AB141125)
  • Chemical Structure

Lab

Chemical Structure - GW 9662, PPARgamma antagonist (AB141125)

2D chemical structure image of ab141125, GW 9662, PPARgamma antagonist

Key facts

CAS number

22978-25-2

Purity

>99%

Form

Solid

form

Molecular weight

276.67 Da

Molecular formula

C<sub>1</sub><sub>3</sub>H<sub>9</sub>ClN<sub>2</sub>O<sub>3</sub>

PubChem

644213

Nature

Synthetic

Solubility

Soluble in ethanol to 50 mM

Biochemical name

2-Chloro-5-nitro-N-phenylbenzamide

Biological description

Selective PPARγ antagonist (IC50 values are 3.3, 32, >1000 nM for PPARγ, PPARα and PPARδ respectively). Apoptotic and antimetastatic activity in vitro.

Canonical smiles

C1=CC=C(C=C1)NC(=O)C2=C(C=CC(=C2)[N+](=O)[O-])Cl

InChi

InChI=1S/C13H9ClN2O3/c14-12-7-6-10(16(18)19)8-11(12)13(17)15-9-4-2-1-3-5-9/h1-8H,(H,15,17)

InChiKey

DNTSIBUQMRRYIU-UHFFFAOYSA-N

IUPAC Name

2-chloro-5-nitro-N-phenylbenzamide

Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
+4°C
Appropriate long-term storage conditions
+4°C
Storage information
The product can be stored for up to 12 months

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

Thyroid peroxidase (TPO) Estrogen Receptor (ER) Aryl hydrocarbon Receptor (AhR) Peroxisome proliferator-activated receptor gamma (PPAR gamma) GLI family zinc finger 3 (Gli3) Tyrosyl-DNA phosphodiesterase 1 (TDP1) Cytochrome P450 2C9 (CYP2C9) Androgen Receptor (AR) Retinoic Acid Receptor alpha (RAR alpha) and Pregnane X Receptor (PXR) represent a range of important biological targets. These proteins exhibit varying functions including hormonal regulation enzymatic activity and transcriptional activation. For instance TPO with a mass of approximately 103 kDa is expressed mainly in the thyroid gland and functions in thyroid hormone synthesis. Meanwhile Cytochrome P450 proteins like CYP2C9 are involved in drug metabolism and are expressed in the liver. Some proteins like ER and AR serve as nuclear hormone receptors playing key roles in gene transcription following ligand binding.
Biological function summary

These targets constitute essential components in cellular and physiological contexts. Estrogen and Androgen receptors enable hormone-driven transcription modulation integral to reproductive tissue function. PPAR gamma acts within adipose tissue regulating fatty acid storage and glucose metabolism and often intersecting with metabolic diseases. CYP2C9 and related enzymes metabolize xenobiotics and endogenous compounds influencing drug clearance rates. PXR can heterodimerize with Retinoid X Receptor to regulate genes responsible for detoxifying cells from foreign substances.

Pathways

These targets integrate into critical biological circuits. Estrogen Receptor and Androgen Receptor partake in steroid hormone signaling pathways important for the development and maintenance of secondary sexual characteristics. Similarly PPAR gamma aligns with the metabolic signaling pathway interacting with proteins involved in lipid metabolism and insulin sensitivity. Cytochrome P450 family members like CYP2C9 impact pathways related to drug metabolism working closely with other CYP enzymes to metabolize substrates including medications and hormones.

These proteins hold associations with various health conditions. Dysregulation of Estrogen Receptor or Androgen Receptor functions can contribute to hormone-sensitive cancers such as breast and prostate cancer respectively interacting with co-regulators like steroid receptor coactivators. PPAR gamma mutations link to metabolic disorders including type 2 diabetes and obesity due to its role in regulating insulin sensitivity. Changes in CYP2C9 activity can influence drug efficacy and lead to adverse drug reactions relevant in personalized medicine approaches with connections to other CYP family members concerning drug-drug interactions.

Product protocols

Publications (11)

Recent publications for all applications. Explore the full list and refine your search

Environmental science and pollution research international 32:6273-6284 PubMed39992522

2025

The anti-inflammatory effect of the amniotic PPARγ pathways is not dysregulated by the alternative plasticizer DINCH and its metabolite MINCH in human fetal membranes.

Applications

Unspecified application

Species

Unspecified reactive species

Coline Charnay,Audrey Antoine,Corinne Belville,Denis Gallot,Régine Minet-Quinard,Vincent Sapin,Loïc Blanchon

BMC pulmonary medicine 23:359 PubMed37740176

2023

PEDF inhibits LPS-induced acute lung injury in rats and promotes lung epithelial cell survival by upregulating PPAR-γ.

Applications

Unspecified application

Species

Unspecified reactive species

Lei Xu,Yifei Chen,Shoujie Feng,Zeyan Liu,Ying Ye,Ranran Zhou,Lijun Liu

Respiratory research 23:100 PubMed35459189

2022

PEDF is an antifibrosis factor that inhibits the activation of fibroblasts in a bleomycin-induced pulmonary fibrosis rat model.

Applications

Unspecified application

Species

Unspecified reactive species

Xichun Qin,Caili Jia,Jingtian Liang,Jiali Chen,Xiucheng Liu,Zhixiang Chao,Hao Qin,Yanliang Yuan,Zhiwei Liu,Zhongming Zhang,Hongyan Dong,Hao Zhang

International journal of molecular medicine 49: PubMed34935055

2021

Sildenafil protects against pulmonary hypertension induced by hypoxia in neonatal rats via activation of PPARγ‑mediated downregulation of TRPC.

Applications

Unspecified application

Species

Unspecified reactive species

Wanjie Huang,Na Liu,Xin Tong,Yanna Du

Environmental health perspectives 127:27003 PubMed30810372

2019

The Role of Peroxisome Proliferator–Activated Receptor Gamma (PPARγ) in Mono(2-ethylhexyl) Phthalate (MEHP)-Mediated Cytotrophoblast Differentiation.

Applications

Unspecified application

Species

Unspecified reactive species

Hussein Shoaito,Julia Petit,Audrey Chissey,Nicolas Auzeil,Jean Guibourdenche,Sophie Gil,Olivier Laprévote,Thierry Fournier,Séverine A Degrelle

Medical science monitor : international medical jo 24:803-811 PubMed29417935

2018

Hydroxysafflor-Yellow A Induces Human Gastric Carcinoma BGC-823 Cell Apoptosis by Activating Peroxisome Proliferator-Activated Receptor Gamma (PPARγ).

Applications

Unspecified application

Species

Unspecified reactive species

Li Liu,Na Si,YiCong Ma,DongYu Ge,Xue Yu,AngRan Fan,Xu Wang,JingHong Hu,Peng Wei,Long Ma,ZiWei Chen,Qian Zhang,CuiLing Feng

Journal of neuroinflammation 15:19 PubMed29338785

2018

Benefits of VCE-003.2, a cannabigerol quinone derivative, against inflammation-driven neuronal deterioration in experimental Parkinson's disease: possible involvement of different binding sites at the PPARγ receptor.

Applications

Unspecified application

Species

Unspecified reactive species

Concepción García,María Gómez-Cañas,Sonia Burgaz,Belén Palomares,Yolanda Gómez-Gálvez,Cristina Palomo-Garo,Sara Campo,Joel Ferrer-Hernández,Carolina Pavicic,Carmen Navarrete,M Luz Bellido,Moisés García-Arencibia,M Ruth Pazos,Eduardo Muñoz,Javier Fernández-Ruiz

PPAR research 2017:6139107 PubMed29225614

2017

New Transcriptional Reporters to Quantify and Monitor PPAR Activity.

Applications

Unspecified application

Species

Unspecified reactive species

Séverine A Degrelle,Hussein Shoaito,Thierry Fournier

American journal of translational research 8:3460-70 PubMed27648136

2016

Peroxisome proliferator-activated receptor-γ agonist troglitazone suppresses transforming growth factor-β1 signalling through miR-92b upregulation-inhibited Axl expression in human keloid fibroblasts in vitro.

Applications

Unspecified application

Species

Unspecified reactive species

Hua-Yu Zhu,Wen-Dong Bai,Jun Li,Ke Tao,Hong-Tao Wang,Xue-Kang Yang,Jia-Qi Liu,Yun-Chuan Wang,Ting He,Song-Tao Xie,Da-Hai Hu

American journal of cancer research 6:1358-70 PubMed27429849

2016

Peroxisome proliferator-activated receptor-γ agonist inhibits collagen synthesis in human keloid fibroblasts by suppression of early growth response-1 expression through upregulation of miR-543 expression.

Applications

Unspecified application

Species

Unspecified reactive species

Hua-Yu Zhu,Wen-Dong Bai,Hong-Tao Wang,Song-Tao Xie,Ke Tao,Lin-Lin Su,Jia-Qi Liu,Xue-Kang Yang,Jun Li,Yun-Chuan Wang,Ting He,Jun-Tao Han,Da-Hai Hu
View all publications

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