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BRL-50481

Catalog No. T5106 CAS 433695-36-4

BRL-50481 is a novel and selective inhibitor of PDE7 with IC50s of 0.15, 12.1, 62 and 490 μM for PDE7A, PDE7B, PDE4 and PDE3, respectively.

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BRL-50481, CAS 433695-36-4

Pack Size	Availability	Price/USD
5 mg	In stock	$ 50.00
10 mg	In stock	$ 60.00
25 mg	In stock	$ 126.00
50 mg	In stock	$ 225.00
100 mg	In stock	$ 378.00

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Purity: 99.88%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	BRL-50481 is a novel and selective inhibitor of PDE7 with IC50s of 0.15, 12.1, 62 and 490 μM for PDE7A, PDE7B, PDE4 and PDE3, respectively.
Targets&IC50	PDE7B:12 μM, PDE7A:0.15 μM, PDE3:490 μM, PDE4:62 μM
In vitro	BRL-50481 marginally increases cAMP levels (19.1±6.2% of the IBMX response at 300 μM) but demonstrates lower potency. At a concentration of 30 μM, BRL-50481 does not independently hinder proliferation but significantly enhances the efficacy of rolipram in this regard. Similarly, it does not affect IL-15-driven proliferation alone, yet amplifies rolipram’s inhibitory properties. A 30-minute pretreatment of human monocytes with BRL-50481 exhibits a minor inhibitory impact (~2 to 10%) on TNFα production across all examined concentrations but boosts the suppressive action of PGE2 on LPS-induced TNFα release. Alone, BRL-50481 has a negligible influence on κB-dependent transcription (5.6±1.9% inhibition at 30 μM) and does not bolster rolipram’s effectiveness (maximum inhibition, 52.9±2.7%; pIC30 value of 5.33±0.12). However, BRL-50481 dose-dependently curtails LPS-induced TNFα secretion in monocytes where PDE7A1 is elevated (21.7±1.6% inhibition at 30 μM after 12 hours) [2].
Cell Research	MOLT-4 cells in 96-well plates are treated for 30 min with BRL-50481. The cAMP content is then determined by an immuno-specific ELISA. Results are expressed as a percentage of the response affected by 100 μM IBMX[2].

Molecular Weight	244.27
Formula	C9H12N2O4S
CAS No.	433695-36-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 20 mg/mL

DMSO: 100 mg/mL

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Highly Selective Inhibitor Library Anti-Neurodegenerative Disease Compound Library Anti-Alzheimer's Disease Compound Library Anti-Metabolism Disease Compound Library Anti-Cardiovascular Disease Compound Library NO PAINS Compound Library Bioactive Lipid Compound Library Metabolism Compound Library Bioactive Compound Library

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Keywords

BRL-50481 433695-36-4 Metabolism PDE inhibit BRL50481 Inhibitor BRL 50481 Phosphodiesterase (PDE) inhibitor

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