1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. BRL-50481

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.

For research use only. We do not sell to patients.

BRL-50481 Chemical Structure

BRL-50481 Chemical Structure

CAS No. : 433695-36-4

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 66 In-stock
10 mg USD 86 In-stock
25 mg USD 172 In-stock
50 mg USD 290 In-stock
100 mg USD 475 In-stock
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Based on 1 publication(s) in Google Scholar

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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.

IC50 & Target

IC50: 0.15 μM (PDE7A), 12 μM (PDE7B), 62 μM (PDE4), 490 μM (PDE3)[1]

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)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

244.27

Formula

C9H12N2O4S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC([N+]([O-])=O)=CC=C1C)(N(C)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (409.38 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0938 mL 20.4692 mL 40.9383 mL
5 mM 0.8188 mL 4.0938 mL 8.1877 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References
Cell Assay
[2]

MOLT-4 cells in 96-well plates are treated for 30 min with BRL-50481 as indicated. The cAMP content is then determined by an immunospecific ELISA. Results are expressed as a percentage of the response affected by 100 μM IBMX[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.0938 mL 20.4692 mL 40.9383 mL 102.3458 mL
5 mM 0.8188 mL 4.0938 mL 8.1877 mL 20.4692 mL
10 mM 0.4094 mL 2.0469 mL 4.0938 mL 10.2346 mL
15 mM 0.2729 mL 1.3646 mL 2.7292 mL 6.8231 mL
20 mM 0.2047 mL 1.0235 mL 2.0469 mL 5.1173 mL
25 mM 0.1638 mL 0.8188 mL 1.6375 mL 4.0938 mL
30 mM 0.1365 mL 0.6823 mL 1.3646 mL 3.4115 mL
40 mM 0.1023 mL 0.5117 mL 1.0235 mL 2.5586 mL
50 mM 0.0819 mL 0.4094 mL 0.8188 mL 2.0469 mL
60 mM 0.0682 mL 0.3412 mL 0.6823 mL 1.7058 mL
80 mM 0.0512 mL 0.2559 mL 0.5117 mL 1.2793 mL
100 mM 0.0409 mL 0.2047 mL 0.4094 mL 1.0235 mL
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BRL-50481 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
BRL-50481
Cat. No.:
HY-109586
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