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BRL-50481

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Catalog No. T5106Cas No. 433695-36-4

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.

BRL-50481

BRL-50481

🥰Excellent
Purity: 99.89%
Catalog No. T5106Cas No. 433695-36-4
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 SizePriceAvailabilityQuantity
5 mg$50In Stock
10 mg$60In Stock
25 mg$126In Stock
50 mg$225In Stock
100 mg$378In Stock
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Purity:99.89%
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Product Introduction

Bioactivity
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].
Chemical Properties
Molecular Weight244.27
FormulaC9H12N2O4S
Cas No.433695-36-4
SmilesCN(C)S(=O)(=O)c1cc(ccc1C)[N+]([O-])=O
Relative Density.1.334 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM4.0938 mL20.4692 mL40.9383 mL204.6915 mL
5 mM0.8188 mL4.0938 mL8.1877 mL40.9383 mL
10 mM0.4094 mL2.0469 mL4.0938 mL20.4692 mL
20 mM0.2047 mL1.0235 mL2.0469 mL10.2346 mL
50 mM0.0819 mL0.4094 mL0.8188 mL4.0938 mL
100 mM0.0409 mL0.2047 mL0.4094 mL2.0469 mL

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