BRL-50481 Inhibitor CAS No. 433695-36-4

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Chemical Characteristic

Product Name	BRL-50481
CAS No.	433695-36-4
Molecular Weight	244.26
Formula	C₉H₁₂N₂O₄S
Chemical Name	?N,N,2-Trimethyl-5-nitro-benzenesulfonamide
Smiles	c1(c(ccc(c1)[N](=O)O)C)S(=O)(=O)N(C)C
Chemical Structure

Biological activities

BRL 50481 is a novel and selective inhibitor of phosphodiesterase (PDE) 7. BRL 50481 inhibits the activity of hrPDE7A1 expressed in baculovirus-infected Spodoptera frugiperda 9 cells in a competitive manner with a Ki of 180 nM. BRL 50481 also potentiates the inhibitory effect of PGE2 on LPS-induced TNFa release.^[1] BRL 50481 inhibits PDE4 with an IC50 of 92 µM. BRL 50481 enhances the inhibitory effects of the PDE4 inhibitor rolipram on cell proliferation in human T-lymphocytes.^[2]

Protocols

In vivo, BRL 50481 is dissolved in DMSO.^[3]

References

[1] Smith SJ, et al. 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. 2004, 66(6): 1679-1689. [2] Yamamoto S, et al. The effects of a novel phosphodiesterase 7A and -4 dual inhibitor, YM-393059, on T-cell-related cytokine production in vitro and in vivo. Eur J Pharmacol. 2006, 541(1-2): 106-114. [3] Mokry J, et al. Effects of selective inhibition of PDE4 and PDE7 on airway reactivity and cough in healthy and ovalbumin-sensitized guinea pigs. Adv Exp Med Biol. 2013, 756: 57-64.

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