CS-2314
T0070907
CAS: 313516-66-4
Molecular Formula: C12H8ClN3O3
CS-2314 - Names and Identifiers
CS-2314 - Physico-chemical Properties
| Molecular Formula | C12H8ClN3O3 |
| Molar Mass | 277.66 |
| Density | 1.498 |
| Melting Point | >184°C (dec.) |
| Water Solubility | Soluble in DMSO at 10mg/ml. Insoluble in water. |
| Solubility | DMSO: >10mg/mL |
| Appearance | White solid |
| Color | white |
| Storage Condition | 2-8°C |
| Sensitive | Light Sensitive |
| In vitro study | T0070907 is a potent and selective PPAR gamma inhibitor. Has obvious affinity, IC50 is 1 nM. T0070907 is covalently bound to the cysteine helix 3 at position 313 of PPAR gamma. T0070907 blocks PPARγ function during cell-based reporter gene and adipocyte differentiation. Consistent with its PPAR gamma antagonist function, t0070907 blocks the accumulation of agonist-induced co-activators towards PPAR gamma in a homogeneous time-resolved fluorescence assay and is capable of functioning in the glutathione S-transferase Pull-down assay and PPAR gamma/retinoic acid X receptor (RXR) enhanced enrichment of the transcriptional co-repressor NcoR towards PPAR gamma in an alpha-dependent gel shift assay. Receptor mutant studies show that T0070907 modulates the interaction of PPARγ with these cofactors by affecting the structure of the 12th Helical region of ligand binding in PPARγ. Interestingly, the enrichment of NCoR induced by T0070907 at the PPAR gamma/rxrα heterodimer was completely reversed by the rxrα agonist LGD1069, t0070907 treatment had only a slight effect on lgd1069-induced co-activator enrichment at the PPARγ/rxrα heterodimer. T0070907 treatment inhibited cell proliferation, invasion and migration but did not significantly affect apoptosis. Similar results were obtained using the dominant negative (Δ462) receptor to study molecular inhibition. T007 can also reduce the level of PPARγ phosphorylation as well as DNA binding capacity and may directly affect the mitogen-activated protein kinase signaling pathway. |
| In vivo study | Lipopolysaccharide pretreatment can significantly improve renal insufficiency, reduce liver cell injury and circulatory failure, and reduce the increase of interleukin-1 in plasma caused by severe endotoxemia. T0070907 can attenuate all of the beneficial effects of lipopolysaccharide pretreatment described above. |
CS-2314 - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | R22 - Harmful if swallowed R36 - Irritating to the eyes |
| Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| WGK Germany | 2 |
| HS Code | 29333990 |
CS-2314 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.602 ml | 18.008 ml | 36.015 ml |
| 5 mM | 0.72 ml | 3.602 ml | 7.203 ml |
| 10 mM | 0.36 ml | 1.801 ml | 3.602 ml |
| 5 mM | 0.072 ml | 0.36 ml | 0.72 ml |
Last Update：2024-01-02 23:10:35
CS-2314 - Reference Information
| biological activity | T0070907 is an effective, selective PPARγ inhibitor. IC50 is 1 nM in cell-free test, which is more than 800 times higher than the selectivity of PPARα and PPARδ. T0070907 can significantly reduce the expression level of DNA-PKcs and RAD51 protein in ME-180 and SiHa cells. |
| target | TargetValue PPARγ (Cell-free say) 1 nM |
| Target | Value |
| PPARγ (Cell-free assay) | 1 nM |
| in vitro study | T0070907 is a strong and selective PPARγ inhibitor. It has obvious affinity, IC50 is 1 nM. T0070907 are covalently bound to cysteine helix 3 at PPARγ 313. T0070907 blocks the function of PPARγ in cell-based reporter genes and adipocyte differentiation. Consistent with its PPARγ antagonist function, T0070907 blocked agonist-induced co-activators from enriching toward PPARγ in homogeneous time-resolved fluorescence analysis and promoted transcription-assisted repressor NcoR from enriching toward PPARγ in glutathione S-transferase Pull-down experiments and PPARγ/retinoic acid X receptor (RXR)α-dependent gel shift analysis. Receptor mutant studies have shown that T0070907 regulate the interaction of PPARγ with these cofactors by affecting the structure of the 12th helix region of ligand binding in PPARγ. Interestingly, the enrichment of T0070907-induced NCoR at PPARγ/RXRα heterodimer can be completely reversed by RXRα agonist LGD1069. T0070907 treatment has only slight effect on the enrichment of LGD1069-induced coactivators at PPARγ/RXRα heterodimer. T0070907 treatment inhibited cell proliferation, invasion and migration but did not significantly affect cell apoptosis. The study of molecular inhibition using dominant inactivation (Δ462) receptors yielded similar results. T007 can also reduce PPARγ phosphorylation level and DNA binding ability and may directly affect the signaling pathway of mitogen-activated protein kinase. |
| in vivo study | lipopolysaccharide pretreatment can obviously improve renal insufficiency, reduce liver cell injury and circulatory failure, and reduce the increase of interleukin -1 in plasma caused by severe endotoxemia. T0070907 can weaken the beneficial effects brought by all the above lipopolysaccharide pretreatment. |
| use | A cell-permeable chloro-nitro-benzamido compound that acts as a potent, specific, irreversible, and high-affinity antagonist of PPARγ with a Ki of 1 nM. Displays >800-fold greater selectivity for PPAR γ over PPARα and PPARδ (Ki = 0.85 μM and 1.8 μM, respectively). Blocks hormone- and agonist-induced adipogenesis in 3T3-L1 cells. It suppresses interactions between PPARγ and coactivator-derived pepti des, while promotes the recruitment of corepressor-derived peptides. Shown to modulate the interaction of PPARγ2 with the cofactor proteins through covalent binding to Cys313 in its ligand-binding dom ain. |
Last Update：2024-04-09 01:59:59
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Product Name: T0070907 Visit Supplier Webpage Request for quotationCAS: 313516-66-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Featured ProductsSpot supply
Product Name: T0070907 Visit Supplier Webpage Request for quotationCAS: 313516-66-4
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Multiple SpecificationsSpot supply
Product Name: T0070907 Request for quotationCAS: 313516-66-4
Tel: 400-968-2212
Email: 3623107365@qq.com
Mobile: 18916960931
QQ: 3623107365
Wechat: 18916960931
Spot supply
Product Name: T0070907 Visit Supplier Webpage Request for quotationCAS: 313516-66-4
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Multiple SpecificationsSpot supply
Product Name: T0070907 Visit Supplier Webpage Request for quotationCAS: 313516-66-4
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: T0070907 Visit Supplier Webpage Request for quotationCAS: 313516-66-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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