T0070907

Modify Date: 2024-01-09 19:04:57

T0070907 Structure
T0070907 structure
Common Name T0070907
CAS Number 313516-66-4 Molecular Weight 277.663
Density 1.5±0.1 g/cm3 Boiling Point 381.7±37.0 °C at 760 mmHg
Molecular Formula C12H8ClN3O3 Melting Point N/A
MSDS USA Flash Point 184.6±26.5 °C
Symbol GHS07
GHS07
Signal Word Warning

 Use of T0070907


T0070907 is a potent PPARγ antagonist with a Ki of 1 nM.

 Names

Name 2-chloro-5-nitro-N-pyridin-4-ylbenzamide
Synonym More Synonyms

 T0070907 Biological Activity

Description T0070907 is a potent PPARγ antagonist with a Ki of 1 nM.
Related Catalog
Target

PPARγ:1 nM (Ki)

PPARδ:1.8 μM (Ki)

PPARα:0.85 μM (Ki)

In Vitro T0070907 (50 μM) pre-treatment impairs repair of IR-induced DNA DSBs in both ME-180 and SiHa cells treated with irradiated (4 Gy). T0070907 (0-50 μM) significantly decreases the levels of DNA-PKcs and RAD51 proteins in ME-180 and SiHa cells[1]. T0070907 (50 μM) treatment reduces the levels of α- and β-tubulin protein in a time-dependent manner, decreases the synthesis of DNA, and prevents the radiation-induced alterations in the cell cycle regulatory proteins of ME180 and SiHa cells[2]. T0070907 (10 µM) has cytotoxicity in an adipocyte-specific and PPARγ-independent manner. T0070907 increases oxidative stress in immature adipocytes[3]. T0070907 (1 μM) blocks the induction of adipogenesis by various treatments of the adipogenic cell line 3T3-L1. T0070907 covalently modifies PPAR on cysteine 313 in helix 3 of human PPAR 2[4].
Kinase Assay To determine the binding affinity of T0070907 to the PPARs, scintillation proximity assay (SPA) is performed with the following modifications. A 90 μL reaction contains SPA buffer (10 mM K2HPO4, 10 mM KH2PO4, 2 mM EDTA, 50 mM NaCl, 1 mM dithiothreitol, 2 mM CHAPS, 10% (v/v) glycerol, pH 7.1), 50 ng of GST-PPAR (or 150 ng of GST-PPAR), 5 nM 3H-labeled radioligands, and 5 μL of T0070907 in Me2SO. After incubation for 1 h at room temperature, 10 μL of polylysine-coated SPA beads (at 20 mg/mL in SPA buffer) are added, and the mixture is incubated for 1 h before reading in Packard Topcount. [3H]Rosiglitazone is used for PPAR, and [3H]GW2433 is used for PPAR and PPAR.
References

[1]. An Z, et al. T0070907 inhibits repair of radiation-induced DNA damage by targeting RAD51. Toxicol In Vitro. 2016 Dec;37:1-8

[2]. An Z, et al. T0070907, a PPAR γ inhibitor, induced G2/M arrest enhances the effect of radiation in human cervical cancer cells through mitotic catastrophe. Reprod Sci. 2014 Nov;21(11):1352-61.

[3]. Kawahara A, et al. Peroxisome proliferator-activated receptor γ (PPARγ)-independent specific cytotoxicity against immature adipocytes induced by PPARγ antagonist T0070907. Biol Pharm Bull. 2013;36(9):1428-34

[4]. Lee G, et al. 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. Epub 2002 Mar 4

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Boiling Point 381.7±37.0 °C at 760 mmHg
Molecular Formula C12H8ClN3O3
Molecular Weight 277.663
Flash Point 184.6±26.5 °C
Exact Mass 277.025421
PSA 87.81000
LogP 2.25
Appearance of Characters white
Vapour Pressure 0.0±0.9 mmHg at 25°C
Index of Refraction 1.684
Storage condition Store at RT
Water Solubility DMSO: >10mg/mL | Soluble in DMSO at 10mg/ml. Insoluble in water.

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302-H319
Precautionary Statements P305 + P351 + P338
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes Xn
Risk Phrases 22-36
Safety Phrases 26
RIDADR NONH for all modes of transport
HS Code 2933399090

 Synthetic Route

~%

T0070907 Structure

T0070907

CAS#:313516-66-4

Literature: US2003/134859 A1, ;

 Precursor & DownStream

Precursor  2

DownStream  0

 Customs

HS Code 2933399090
Summary 2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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 Synonyms

2-Chloro-5-nitro-N-4-pyridinyl-benzamide Benzamide,2-chloro-5-nitro-N-4-pyridinyl
Benzamide,2-chloro-5-nitro-N-4-pyridinyl
2-chloro-5-nitro-N-pyridin-4-yl-benzamide
Benzamide, 2-chloro-5-nitro-N-4-pyridinyl-
2-Chloro-5-nitro-N-(4-pyridinyl)benzamide
2-Chloro-5-nitro-N-4-pyridinylbenzamide
2-chloro-5-nitro-N-(pyridin-4-yl)benzamide
T0070907
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