| Name | BRL-50481 |
| 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. |
| 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]. |
| 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]. |
| 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)
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| Keywords | BRL-50481 | inhibit | BRL50481 | Inhibitor | BRL 50481 | Phosphodiesterase (PDE) |
| Inhibitors Related | Theophylline monohydrate | Diphylline | Acefylline | Roflumilast | Theobromine | Apremilast | Isoprenaline hydrochloride | Indomethacin | Icariin | Theophylline | Vardenafil hydrochloride | Doxofylline |
| Related Compound Libraries | Highly Selective Inhibitor Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Anti-Alzheimer's Disease Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Cardiovascular Disease Compound Library | Metabolism Compound Library | Bioactive Compounds Library Max | Bioactive Lipid Compound Library |
United States
