BRL 50481

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Cat.No. 2237 - BRL 50481 | C9H12N2O4S | CAS No. 433695-36-4
Description: Selective PDE7 inhibitor
Chemical Name: N,N,2-Trimethyl-5-nitro-benzenesulfonamide
Purity: ≥99% (HPLC)
Datasheet
Citations (3)
Reviews
Literature

Biological Activity

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

BRL 50481 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 24.43 100
DMSO 24.43 100

Preparing Stock Solutions

The following data is based on the product molecular weight 244.26. 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.

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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References

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 dopaminergic neurons in cellular and rodent models of Parkinson disease. J Biol Chem 6 e17240 PMID: 21390306


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