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BRL-50481 is a novel and selective PDE7 inhibitor with IC50 values of 0.15 μM for PDE7A, 12.1 μM for PDE7B, 62 μM for PDE4, and 490 μM for PDE3.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $50 | In Stock | |
10 mg | $60 | In Stock | |
25 mg | $126 | In Stock | |
50 mg | $225 | In Stock | |
100 mg | $378 | In Stock |
Description | BRL-50481 is a novel and selective PDE7 inhibitor with IC50 values of 0.15 μM for PDE7A, 12.1 μM for PDE7B, 62 μM for PDE4, and 490 μM for PDE3. |
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 |
Smiles | CN(C)S(=O)(=O)c1cc(ccc1C)[N+]([O-])=O |
Relative Density. | 1.334 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | Ethanol: 20 mg/mL DMSO: 45 mg/mL (184.22 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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