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T0070907 was identified as a potent and selective PPARgamma antagonist. With an apparent binding affinity (concentration at 50% inhibition of [(3)H]rosiglitazone binding or IC(50)) of 1 nm, T0070907 covalently modifies PPARgamma on cysteine 313 in helix 3 of human PPARgamma2.
Targets
| PPARγ (Cell-free assay) | PPARα (Cell-free assay) | PPARδ (Cell-free assay) | ||
| 1 nM | 0.85 μM | 1.8 μM |
| In vitro (25°C) | DMSO | 24 mg/mL (86.43 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 5% DMSO+45% PEG 300+ddH2O | 8 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
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| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 36.02 mL | 180.08 mL | 360.15 mL |
| 0.5 mM | 7.2 mL | 36.02 mL | 72.03 mL |
| 1 mM | 3.6 mL | 18.01 mL | 36.02 mL |
| 5 mM | 0.72 mL | 3.6 mL | 7.2 mL |
*The above data is based on the productmolecular weight 277.66. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A11588 |
|---|---|
| Actions | Antagonist |
| CAS No. | 313516-66-4 |
| Formula | C12H8ClN3O3 |
| M. Wt | 277.66 |
| Purity | >98% |
| Synonyms | T 0070907 |
| SMILES | ClC1=CC=C([N+]([O-])=O)C=C1C(NC2=CC=NC=C2)=O |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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