BRL-50481
Based on 5 publication(s) in Google Scholar
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.81%
- CAS. Nr.: 433695-36-4
- Formel: C9H12N2O4S
- Molecular Weight:244.27
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Publications Citing Use of MedChemExpress (MCE) BRL-50481
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Biologische Aktivität
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PDE7 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
2.2 μM
Compound: BRL-50481
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Inhibition of human recombinant PDE7A1 expressed in baculovirus-infected insect Sf9 cells by modified two-step method
Inhibition of human recombinant PDE7A1 expressed in baculovirus-infected insect Sf9 cells by modified two-step method
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[PMID: 19303290] |
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.
Chemical Information
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CAS. Nr. 433695-36-4
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Appearance Solid
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Molecular Weight 244.27
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Formel C9H12N2O4S
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Color White to off-white
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SMILES
O=S(C1=CC([N+]([O-])=O)=CC=C1C)(N(C)C)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Biochem Pharmacol
2026 May:247:117785. PMID: 41679664 -
Int J Neuropsychopharmacol
Identification of Phosphodiesterase-7A (PDE7A) as a Novel Target for Reducing Ethanol Consumption in Mice. [Abstract]2024 Aug 5:pyae032. PMID: 39099166 -
Mol Biol Rep
Neuronal deletion of PDE7A averts morphine-induced behavioral plasticity and impairs downstream AKT signaling. [Abstract]2026 May 7;53(1):724. PMID: 42095971 -
Biochim Biophys Acta Gen Subj
2025 Aug 13;1869(11):130850. PMID: 40816541 -
bioRxiv
Host GPCR-cAMP signaling balances Gαs and Gαi activity to control intracellular Brucella infection. [Abstract]2026 Jan 6:2026.01.06.697936. PMID: 41542404
Lösungsmittel & Löslichkeit
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.
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Safavi M, et al. New methods for the discovery and synthesis of PDE7 inhibitors as new drugs for neurologicaland inflammatory disorders. Expert Opin Drug Discov. 2013 Jun;8(6):733-51. [Content Brief]
[2]. Smith SJ, et al. Discovery of BRL 50481 [3-(N,N-dimethylsulfonamido)-4-methyl-nitrobenzene], a selective inhibitor of phosphodiesterase 7: in vitro studies in human monocytes, lung macrophages, and CD8+ T-lymphocytes. Mol Pharmacol. 2004 Dec;66(6):1679-89. [Content Brief]
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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