T0070907

Bezeichnung:T0070907

CAS-Nr313516-66-4

Englisch Name:T0070907

CBNumberCB4771443

SummenformelC12H8ClN3O3

Molgewicht277.66

MOL-Datei313516-66-4.mol

T0070907 physikalisch-chemischer Eigenschaften

Schmelzpunkt	>184°C (dec.)
Dichte	1.498
storage temp.	2-8°C
Löslichkeit	DMSO: >10mg/mL
Aggregatzustand	White solid
Farbe	white
Wasserlöslichkeit	Soluble in DMSO at 10mg/ml. Insoluble in water.
Sensitive	Light Sensitive

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	22-36
S-Sätze:	26
WGK Germany	2
HS Code	29333990

Gefahreninformationscode (GHS)

T0070907 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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.
Chemische Eigenschaften
Off-White Solid
Verwenden
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 ,
Verwenden
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.
Allgemeine Beschreibung
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.
Biologische Aktivität
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.
Lager
Store at RT
Einzelnachweise
[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.

T0070907 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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