BRL 50481

SKU: orb1221199

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.

Key Properties

• CAS Number: 433695-36-4
• MW: 244.27
• Purity: >98% (HPLC)
• Formula: C₉H₁₂N₂O₄S
• SMILES: CN(C)S(=O)(=O)c1cc(ccc1C)[N+]([O-])=O
• Target: PDE
• Solubility: DMSO: 100 mg/mL;Ethanol: 20 mg/mL

Bioactivity

• In Vitro:
  BRL-50481 increases the cAMP content (19.1±6.2% of IBMX response at 300 μM) but is considerably less potent. BRL-50481 (30 μM) fails to suppress proliferation by itself but significantly potentiates the effect of rolipram. BRL-50481 (30 μM) has no effect on IL-15-induced proliferation but augments the inhibitory effect of rolipram. Pretreatment (30 min) of human monocytes with BRL-50481 has, by itself, a negligible (~2 to 10%) inhibitory effect on TNFα output at all concentrations tested. BRL-50481 also potentiates the inhibitory effect of PGE2 on LPS-induced TNFα release. BRL-50481 has no significant effect by itself on κB-dependent transcription (5.6±1.9% inhibition at 30 μM) and fails to enhance the effect of rolipram (maximum inhibition, 52.9±2.7%; pIC30 value of 5.33±0.12). BRL-50481 suppresses, in a concentration-dependent manner, LPS-induced TNFα release in monocytes in which PDE7A1 is induced (21.7±1.6% inhibition at 30 μM at the 12-h time point).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

PDE