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Submit ReviewBRL 50481
Description: Selective PDE7 inhibitor
Chemical Name: N,N,2-Trimethyl-5-nitro-benzenesulfonamide
Purity: ≥99% (HPLC)
Biological Activity for BRL 50481
BRL 50481 is a selective, substrate-competitive inhibitor of phosphodiesterase (PDE) 7 (Ki = 180 nM). Displays > 200-fold selectivity over PDE1B, PDE1C, PDE2, PDE3, PDE4A4 and PDE5.
Licensing Information
Sold with the permission of GlaxoSmithKline
Compound Libraries for BRL 50481
BRL 50481 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for BRL 50481
| M. Wt | 244.26 |
| Formula | C9H12N2O4S |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 433695-36-4 |
| PubChem ID | 2921148 |
| InChI Key | IFIUFCJFLGCQPH-UHFFFAOYSA-N |
| Smiles | CN(C)S(=O)(=O)C1=C(C)C=CC(=C1)[N+]([O-])=O |
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 for BRL 50481
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| ethanol | 24.43 | 100 | |
| DMSO | 24.43 | 100 |
Preparing Stock Solutions for BRL 50481
The following data is based on the product molecular weight 244.26. 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 | 4.09 mL | 20.47 mL | 40.94 mL |
| 5 mM | 0.82 mL | 4.09 mL | 8.19 mL |
| 10 mM | 0.41 mL | 2.05 mL | 4.09 mL |
| 50 mM | 0.08 mL | 0.41 mL | 0.82 mL |
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Product Datasheets for BRL 50481
References for BRL 50481
References are publications that support the biological activity of the product.
Smith et al (2004) Discovery of BRL 50481 [3-(N,N-dimethylsulfonamido)-4-methyl-nitrobenzene], a selective inhibitor of phosphodiesterase 7: in vitro studies in human monocytes, lung macrophages, and CD8+ T-lymphocytes. Mol.Pharmacol. 66 1679 PMID: 15371556
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Keywords: BRL 50481, BRL 50481 supplier, Selective, PDE7, inhibitors, inhibits, Phosphodiesterases, BRL50481, GlaxoSmithKline, GSK, 2237, Tocris Bioscience
3 Citations for BRL 50481
Citations are publications that use Tocris products. Selected citations for BRL 50481 include:
Zhai et al (2012) β-Adrenergic cAMP signals are predominantly regulated by phosphodiesterase type 4 in cultured adult rat aortic smooth muscle cells. PLoS One 7 e47826 PMID: 23094097
Meyers et al (2009) Chronic lymphocytic leukemia and B and T cells differ in their response to cyclic nucleotide phosphodiesterase inhibitors. J Immunol 182 5400 PMID: 19380787
Morales-Garcia et al (2011) Phosphodiesterase 7 inhibition preserves DArgic neurons in cellular and rodent models of Parkinson disease. J Biol Chem 6 e17240 PMID: 21390306
Do you know of a great paper that uses BRL 50481 from Tocris? Please let us know.
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