T0070907 Property

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

Safety

Hazard Codes 

Xn

Risk Statements 

22-36

Safety Statements 

26

WGK Germany 

2

HS Code 

29333990

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P405Store locked up.

T0070907 Chemical Properties,Usage,Production

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-Δ^12,14-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.