T0070907 - Moligand™, 10mM in DMSO , Antagonist of Peroxisome proliferator-activated receptor-γ, CAS No.313516-66-4, Antagonist of Peroxisome proliferator-activated receptor-γ

CAS: 313516-66-4 Cat. No.: T408157 Formula: C₁₂H₈ClN₃O₃ Peso molecolare: 277.66 Numero EC: 631-142-7 PubChem CID: 2777391

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

Benzamide, 2-chloro-5-nitro-N-4-pyridinyl-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

Information

T0070907 is a potent and selectivePPARγinhibitor withIC50of 1 nM in a cell-free assay, with a >800-fold selectivity over PPARα and PPARδ. T0070907 significantly decreases the levels ofDNA-PKcsandRAD51proteins in ME-180 and SiHa cells.
In vitro

T0070907 is a potent and selective PPARγ antagonist. With an apparent binding affinity (concentration at 50% inhibition of [³H] rosiglitazone binding or IC50) of 1 nM, T0070907 covalently modifies PPARγ on cysteine 313 in helix 3 of human PPARγ2. T0070907 blocks PPARγ function in both cell-based reporter gene and adipocyte differentiation assays. Consistent with its role as an antagonist of PPARγ, T0070907 blocks agonist-induced recruitment of coactivator-derived peptides to PPARγ in a homogeneous time-resolved fluorescence-based assay and promotes recruitment of the transcriptional corepressor NCoR to PPARγ in both glutathione S-transferase pull-down assays and a PPARγ/retinoid X receptor (RXR) α-dependent gel shift assay. Studies with mutant receptors suggest that T0070907 modulates the interaction of PPARγ with these cofactor proteins by affecting the conformation of helix 12 of the PPARγ ligand-binding domain. Interestingly, whereas the T0070907-induced NCoR recruitment to PPARγ/RXRα heterodimer can be almost completely reversed by the simultaneous treatment with RXRα agonist LGD1069, T0070907 treatment has only modest effects on LGD1069-induced coactivator recruitment to the PPARγ/RXRα heterodimer. T0070907 treatment inhibits proliferation, invasion and migration but does not significantly affect apoptosis. Molecular inhibition using a dominant negative (Δ462) receptor yields similar results. T007 also mediates a dose-dependent decrease in phosphorylation of PPARγ, and its ability to bind to DNA, and may directly affect mitogen-activated protein kinase signaling.

In vivo

Lipopolysaccharide preconditioning significantly attenuates the development of renal dysfunction, hepatocellular injury, and circulatory failure as well as the increase in the plasma levels of interleukin-1 [beta] caused by severe endotoxemia. T0070907 can attenuate all of these beneficial effects afforded by preconditioning with lipopolysaccharide
Cell Data

cell lines：LNCaP and LAPC4

Concentrations：20 μM and higher concentrations

Incubation Time：48 h

Powder Purity:≥99%

Specifications

Sinonimi

Benzamide, 2-chloro-5-nitro-N-4-pyridinyl-

Specifiche e purezza

Moligand™, 10mM in DMSO

Meccanismi biochimici e fisiologici

T0070907 is a potent and selective PPARγ inhibitor with IC50 of 1 nM in a cell-free assay, with a >800-fold selectivity over PPARα and PPARδ. T0070907 significantly decreases the levels of DNA-PKcs and RAD51 proteins in ME-180 and SiHa cells.

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Grado

Moligand™

Tipo di azione

ANTAGONIST

Meccanismo d'azione

Antagonist of Peroxisome proliferator-activated receptor-γ

Nomi e identificatori

• Isomeri SMILES: C1=CC(=C(C=C1[N+](=O)[O-])C(=O)NC2=CC=NC=C2)Cl
• WGK Germania: 3
• PubChem CID: 2777391
• Peso molecolare: 277.66

Obiettivi associati (umani)

PPARG Tclin Peroxisome proliferator-activated receptor gamma (1 Activities)

Discover Target: PPARG

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Proprietà chimiche e fisiche

• Solubilità: Solubility (25°C) In vitro

Riferimenti

1. Jinmiao Tian, Lichao Zhang, Xiaoqin La, Xiaxia Fan, Aiping Li, Changxin Wu, Yuxuan An, Shuning Yan, Xiushan Dong, Haitao Wu, Zhuoyu Li.  (2023)  Tumor-secreted GRP78 induces M2 polarization of macrophages by promoting lipid catabolism.  CELLULAR SIGNALLING,      [PMID:37207940] [10.1016/j.cellsig.2023.110719]

2. Meng-Ke Song, Meng-Qi Wang, Yu-Qing Ruan, Can Cui, Wen-Gang Chen, Opeyemi Joshua Olatunji, Yan Li, Jian Zuo.  (2025)  Qing-Luo-Yin Eases T Cells-Mediated Angiogenesis in Adjuvant-Induced Arthritis Rats by Activating PPARγ.  Journal of Inflammation Research,      [PMID:40093952] [10.2147/JIR.S508316]

3. Qing-qing Fang, Yang-jun Gu, Yong Wang, Zheng-cai Wang, Xiao-ying Lin, Kai Guo, Ze-ming Zhuang, Xin-cao Zhong, Li-yun Zhang, Jian Chen, Wei-qiang Tan.  (2025)  The therapeutic potential of Rosiglitazone in modulating scar formation through PPAR-γ pathway.  EUROPEAN JOURNAL OF PHARMACOLOGY,      [PMID:40054722] [10.1016/j.ejphar.2025.177445]

4. Yan Jin, Fang Lu, Xi Miaocui, Liu Ziqi, Zhang Shihan, Zhang Yuning, Zhang Yuwei, Xue Ting, Li Jiahang, Huang Yue, Chang Runfeng, Qian Qiuhui, Wang Zejun, Teng Miaomiao, Wang Huili.  (2026)  Ethylhexyl Diphenyl Phosphate Mediates Oxidative Stress and Energy Metabolism Abnormalities by Affecting Glycolipid Metabolism in Zebrafish during Early Development: Key Regulatory Role of the Peroxisome Proliferator-Activated Receptor Signaling Pathway.  ENVIRONMENTAL SCIENCE & TECHNOLOGY,  60  (30): (20740-20756).  [PMID:42482340] [10.1021/acs.est.5c06517]

Domande frequenti

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 313516-66-4, the molecular formula is C12H8ClN3O3, and the molecular weight is 277.66 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.