BRL-50481

SKU: orb1302085

Description

BRL-50481 is a potent and selective PDE7 inhibitor, demonstrating high selectivity for PDE7A (IC50 = 0.15 µM) over PDE7B, PDE4, and PDE3. This tool compound is used in research to investigate PDE7's role in T-cell activation and neurological processes, with applications in both in vitro and in vivo models of inflammation and CNS disorders.

Research Area

Cell Biology

Key Properties

• CAS Number: 433695-36-4
• MW: 244.27
• Purity: >98%
• Formula: C₉H₁₂N₂O₄
• SMILES: CN(C)S(=O)(=O)c1cc(ccc1C)[N+]([O-])=O
• Target: PDE (Phosphodiesterase)
• Solubility: Soluble in DMSO (up to 40 mg/ml) or in Ethanol (up to 5 mg/ml).

Bioactivity

• Target IC50:
  PDE7A:0.15 μM|PDE7B:12 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) .
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• 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.
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Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BRL50481, BRL-50481, BRL 50481, inhibit, Inhibitor, PDE7, Phosphodiesterase (PDE), phosphodiesterase

Compound Identifiers

PubChem CID

2921148