BRL-50481

Alias: BRL-50481; BRL 50481; BRL50481
Cat No.:V4092 Purity: ≥98%
BRL-50481 is a novel, potent and selective inhibitor ofphosphodiesterase 7(PDE7) withIC50s of 0.15, 12.1, 62 and 490 μM forPDE7A,PDE7B,PDE4andPDE3, respectively.
BRL-50481 Chemical Structure CAS No.: 433695-36-4
Product category: Phosphodiesterase(PDE)
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

BRL-50481 is a novel, potent and selective inhibitor of phosphodiesterase 7 (PDE7) with IC50s of 0.15, 12.1, 62 and 490 μM for PDE7A, PDE7B, PDE4 and PDE3, respectively. BRL 50481 inhibited the activity of hrPDE7A1 expressed in baculovirus-infected Spodoptera frugiperda 9 cells in a competitive manner (Ki value of 180 nM) and was 416 and 1884 times less potent against PDE3 and 38 and 238 times less potent against PDE4 at a substrate concentration of 1 microM and 50 nM cAMP, respectively. Western blotting identified HSPDE7A1 but not HSPDE7A2 in three human cell types that are implicated in the pathogenesis of chronic obstructive lung disease, namely, CD8+ T-lymphocytes, monocytes, and lung macrophages. BRL 50481 is the first fully documented PDE7 inhibitor that has acceptable selectivity for in vitro studies.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
BRL-50481 had a relatively modest potency but did enhance cAMP content (19.1 ± 6.2% of IBMX reaction at 300 μM). While BRL-50481 (30 μM) did not prevent proliferation on its own, it greatly improved rolipram's effects. BRL-50481 (30 μM) improved rolipram's inhibitory action but had no effect on IL-15-induced proliferation. BRL-50481 pretreatment of human monocytes alone for 30 minutes had very little inhibitory effects on TNFα production at all tested doses (about 2 to 10%). Additionally, BRL-50481 improved PGE2's ability to block LPS-induced TNFα release. Neither BRL-50481 nor rolipram (maximum inhibition 52.9±2.7%; pIC30 value 5.33±0.12) significantly affect κB-dependent transcription (5.6±1.9% inhibition at 30 μM). In a concentration-dependent manner, BRL-50481 suppresses PDE7A1-induced LPS-induced TNFα production in monocytes (21.7±1.6% inhibition at 30 μM at the 12-hour time point) [2].
References
[1]. Safavi M, et al. New methods for the discovery and synthesis of PDE7 inhibitors as new drugs for neurologicaland inflammatory disorders. Expert Opin Drug Discov. 2013 Jun;8(6):733-51.
[2]. 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 Dec;66(6):1679-89
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C9H12N2O4S
Molecular Weight
244.27
CAS #
433695-36-4
SMILES
O=S(C1=CC([N+]([O-])=O)=CC=C1C)(N(C)C)=O
Chemical Name
N,N,2-Trimethyl-5-nitro-benzenesulfonamide
Synonyms
BRL-50481; BRL 50481; BRL50481
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO:≥ 45mg/mL
Water:< 1mg/mL
Ethanol:N/A
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 4.0938 mL 20.4692 mL 40.9383 mL
5 mM 0.8188 mL 4.0938 mL 8.1877 mL
10 mM 0.4094 mL 2.0469 mL 4.0938 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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