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T0070907

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T0070907 Basic information

Product Name:
T0070907
Synonyms:
  • 2-CHLORO-5-NITRO-N-4-PYRIDINYLBENZAMIDE
  • 2-CHLORO-5-NITRO-N-(4-PYRIDYL)BENZAMIDE
  • T 0070907
  • N1-(4-PYRIDYL)-2-CHLORO-5-NITROBENZAMIDE
  • BenzaMide, 2-chloro-5-nitro-N-4-pyridinyl-
  • T0070907 - CAS 313516-66-4 - Calbiochem
  • CS-2314
  • T0070907 (T-0070907
CAS:
313516-66-4
MF:
C12H8ClN3O3
MW:
277.66
Product Categories:
  • PPARγ antagonist
  • Inhibitor
  • Inhibitors
  • Intracellular receptor
Mol File:
313516-66-4.mol
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T0070907 Chemical Properties

Melting point:
>184°C (dec.)
Density 
1.498
storage temp. 
2-8°C
solubility 
DMSO: >10mg/mL
form 
White solid
color 
white
Water Solubility 
Soluble in DMSO at 10mg/ml. Insoluble in water.
Sensitive 
Light Sensitive
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Safety Information

Hazard Codes 
Xn
Risk Statements 
22-36
Safety Statements 
26
WGK Germany 
2
HS Code 
29333990
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T0070907 Usage And Synthesis

Description

The peroxisome proliferator-activated receptor-γ (PPARγ) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones (TZDs). TZDs are a group of structurally related synthetic PPARγ receptor agonists with antidiabetic actions in vivo. There are many PPARγ agonists, including 15-deoxy-Δ12,14-prostaglandin J2 and azelaoyl PAF, which are naturally derived. However, only a few antagonists have been reported. T0070907 is a potent and selective antagonist of the human PPARγ with an apparent IC50 of 1 nM for the binding inhibition of rosiglitazone, a reference TZD. T0070907 covalently binds to Cys313 of PPARγ, inducing conformational changes that block the recruitment of transcriptional cofactors to the PPARγ/RXR heterodimer.

Chemical Properties

Off-White Solid

Uses

A cell-permeable chloro-nitro-benzamido compound that acts as a potent, specific, irreversible, and high-affinity antagonist of PPAR with a Ki of 1 nM. Displays >800-fold greater selectivity for PPAR over PPARa and PPARd (Ki = 0.85 and 1.8 ,

Uses

T0070907 has been used to reduce peroxisome proliferator-activated receptor gamma (PPAR-γ) expression in lipopolysaccharide (LPS)-induced leukemia RAW264.7 cell line. It also has been used to evaluate the involvement of wogonin in alleviating EtOH (ethanol)-induced inflammation in RAW264.7 cell line.

Definition

ChEBI: 2-chloro-5-nitro-N-pyridin-4-ylbenzamide is a carbonyl compound and an organohalogen compound.

General Description

T0070907 has antimicrotubule, antitumor and radiosensitizing properties. It decreases tubulin protein levels, which is associated with cell cycle arrest, apoptosis and also reduces metastasis of colorectal carcinoma cells. T0070907 is used as a therapeutic target in breast cancer. It stimulates proteasome-dependent degradation of tubulin.

Biological Activity

Potent and selective PPAR γ antagonist (IC 50 = 1 nM). Displays > 800-fold selectivity for PPAR γ over PPAR α and PPAR δ . In vitro, blocks transcriptional activity of PPAR γ and inhibits rosiglitazone-induced adipogenesis.

Biochem/physiol Actions

T0070907 is very similar in structure and activity to the PPAR-γ antagonist GW9662. T0070907 is more potent and has higher selectivity for PPAR-γ over all other subtypes (about 800-fold) whereas GW9662 has been reported to have some PPAR-α agonist activity.

storage

Store at RT

References

[1] lee g, elwood f, mcnally j, weiszmann j, lindstrom m, amaral k, nakamura m, miao s, cao p, learned rm, chen jl, li y. t0070907, a selective ligand for peroxisome proliferator-activated receptor gamma, functions as an antagonist of biochemical and cellular activities. j biol chem. 2002 may 31;277(22):19649-57.

T0070907Supplier

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