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T0070907

Alias: T-0070907; T 0070907; T0070907;
Cat No.:V0827 Purity: ≥98%
T0070907 (T-0070907; T 0070907) is a potent and selective PPARγ (Peroxisome proliferator-activated receptor γ) inhibitor with potential anti-inflammatory activity.
T0070907
T0070907 Chemical Structure CAS No.: 313516-66-4
Product category: PPAR
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

T0070907 (T-0070907; T 0070907) is a potent and selective PPARγ (Peroxisome proliferator-activated receptor γ) inhibitor with potential anti-inflammatory activity. It inhibits PPARγ with an IC50 of 1 nM in a cell-free assay.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
ME-180 and SiHa cells exposed with 4 Gy of radiation exhibit impaired IR-induced DNA DSB repair following pretreatment with T0070907 (50 μM). In ME-180 and SiHa cells, T0070907 (0-50 μM) dramatically lowers DNA-PKcs and RAD51 protein levels [1]. In ME180 and SiHa cells, T0070907 (50 μM) treatment inhibits DNA synthesis, suppresses radiation-induced alterations in cell cycle regulatory proteins, and decreases α- and β-tubulin levels in a time-dependent way [2]. T0070907 (10 μM) exhibits cytotoxicity that is unique to adipocytes and not dependent on PPARγ. Oxidative stress in immature adipocytes is elevated by T0070907 [3]. T0070907 (1 μM) prevents the adipogenic cell line 3T3-L1 from being treated in a way that induces adipogenesis. T0070907 covalently alters human PPAR 2 helix 3's cysteine 313 [4].
ln Vivo
Lipopolysaccharide preconditioning significantly attenuates the development of renal dysfunction, hepatocellular injury, and circulatory failure as well as the increase in the plasma levels of interleukin-1 [beta] caused by severe endotoxemia. T0070907 can attenuate all of these beneficial effects afforded by preconditioning with lipopolysaccharide.
Animal Protocol
Dissolved in 10% v/v dimethylsulfoxide [DMSO], 20–25% v/v DMSO, or saline; 1 mg/kg; i.p. injection
Preconditioning is performed by administering a low dose (1 mg/kg) of Escherichia coli LPS (serotype 0.127:B8) intraperitoneally 24 hr before the induction of severe endotoxemia.
References

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

[2]. 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]. 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]. 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.

Additional Infomation
2-chloro-5-nitro-N-pyridin-4-ylbenzamide is a carbonyl compound and an organohalogen compound.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C12H8CLN3O3
Molecular Weight
277.66
Exact Mass
277.025
CAS #
313516-66-4
Related CAS #
313516-66-4
PubChem CID
2777391
Appearance
White to light yellow solid powder
Density
1.5±0.1 g/cm3
Boiling Point
381.7±37.0 °C at 760 mmHg
Flash Point
184.6±26.5 °C
Vapour Pressure
0.0±0.9 mmHg at 25°C
Index of Refraction
1.684
LogP
2.25
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
2
Heavy Atom Count
19
Complexity
342
Defined Atom Stereocenter Count
0
InChi Key
FRPJSHKMZHWJBE-UHFFFAOYSA-N
InChi Code
InChI=1S/C12H8ClN3O3/c13-11-2-1-9(16(18)19)7-10(11)12(17)15-8-3-5-14-6-4-8/h1-7H,(H,14,15,17)
Chemical Name
2-chloro-5-nitro-N-(pyridin-4-yl)benzamide
Synonyms
T-0070907; T 0070907; T0070907;
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 26 mg/mL (93.6 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 1 mg/mL (3.60 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 1 mg/mL (3.60 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 1 mg/mL (3.60 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: 1% DMSO+30% polyethylene glycol+1% Tween 80: 30mg/mL

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.6015 mL 18.0076 mL 36.0153 mL
5 mM 0.7203 mL 3.6015 mL 7.2031 mL
10 mM 0.3602 mL 1.8008 mL 3.6015 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • T0070907


    T0070907 is a specific potent PPARγ antagonist.J Biol Chem.2002 May 31;277(22):19649-57.
  • T0070907


    T0070907 covalently binds to PPARγ at Cys313.J Biol Chem.2002 May 31;277(22):19649-57.
  • T0070907

    T0070907 is an inverse agonist of the GST-PPARγ LBD in vitro.J Biol Chem.2002 May 31;277(22):19649-57.
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