nTZDpa

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Cat.No. 2150 - nTZDpa | C22H15Cl2NO2S | CAS No. 118414-59-8
Description: Potent, selective PPARγ partial agonist
Chemical Name: 5-Chloro-1-[(4-chlorophenyl)methyl]-3-(phenylthio)-1H-indole-2-carboxylic acid
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (4)

Biological Activity

Potent, selective non-thiazolidinedione PPARγ partial agonist (EC50 = 57 nM); produces ~25% maximum efficacy. Antagonizes full agonist activity by ~60% (IC50 ~ 285 nM). Displays no activity at PPARα or PPARδ receptors. Produces altered receptor conformation, and regulates adipocyte development and gene expression, in a differential manner to full PPARγ agonists. Modulates metabolism and insulin sensitivity without causing cardiac hypertrophy in mice in vivo.

Technical Data

M. Wt 428.33
Formula C22H15Cl2NO2S
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 118414-59-8
PubChem ID 9954280
InChI Key VUPOTURDKDMIGQ-UHFFFAOYSA-N
Smiles OC(=O)C1=C(SC2=CC=CC=C2)C2=CC(Cl)=CC=C2N1CC1=CC=C(Cl)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 42.83 100

Preparing Stock Solutions

The following data is based on the product molecular weight 428.33. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.33 mL 11.67 mL 23.35 mL
5 mM 0.47 mL 2.33 mL 4.67 mL
10 mM 0.23 mL 1.17 mL 2.33 mL
50 mM 0.05 mL 0.23 mL 0.47 mL

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References

References are publications that support the biological activity of the product.

Berger et al (2003) Distinct properties and advantages of a novel peroxisome proliferator-activated protein γ selective modulator. Mol.Endocrinol. 17 662 PMID: 12554792


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Keywords: nTZDpa, nTZDpa supplier, Potent, selective, PPARγ, PPARgamma, partial, agonists, Peroxisome, Proliferator-activating, Receptors, 2150, Tocris Bioscience

Citations for nTZDpa

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