BRL-50481A selective inhibitor of PDE 7

BRL-50481 (CAS 433695-36-4)

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Synonym: 5-Nitro-2,N,N-trimethylbenzenesulfonamide
Application: A selective inhibitor of PDE 7
CAS Number: 433695-36-4
Purity: ≥98%
Molecular Weight: 244.27
Molecular Formula: C9H12N2O4S
* Refer to Certificate of Analysis for lot specific data (including water content).
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BRL-50481 is a selective inhibitor of phosphodiesterase 7 (PDE 7) that has acceptable selectivity for in vitro studies. Studies suggest that BRL-50481 is used to inhibit the activity of hrPDE7A1 which is usually expressed in baculovirus-infected Spodoptera frugiperda in a competitive manner. In osteoblasts, BRL-50481increases mineralization and bALP as a result of PDE7 silencing which upregulates several osteogenic genes. Further studies show that BRL-50481increases apoptosis in CLL cells via a mitochondrial-dependent process, and is associated with increased cAMP accumulation and down-regulation of the antiapoptotic protein survivin. BRL-50481 is a inhibitor of PDE7A.


References

1. Smith, S.J., et al. 2004. Mol. Pharmacol. 66: 1679-1689. PMID: 15371556
2. Pekkinen, M., et al. 2008. Bone. 43: 84-91. PMID: 18420479
3. Zhang, L., et al. 2008. Proc. Natl. Acad. Sci. U.S.A. 105: 19532-19537. PMID: 19033455

Physical State :
Solid
Solubility :
Soluble in DMSO (>40 mg/mL), and ethanol (5 mg/mL). Insoluble in water.
Storage :
Store at room temperature
Melting Point :
141.24° C (Predicted)
Boiling Point :
~391.1° C at 760 mmHg (Predicted)
Density :
~1.3 g/cm3 (Predicted)
Refractive Index :
n20D 1.56 (Predicted)
IC50 :
PDE7: IC50 = 260 nM
Ki Data :
PDE7: Ki= 180 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
2921148
MDL Number :
MFCD03039912
SMILES :
CC1=C(C=C(C=C1)[N+](=O)[O-])S(=O)(=O)N(C)C

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Certificate of Analysis

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BRL-50481  Product Citations

See how others have used BRL-50481. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 23656623  Ikari, J. et al. 2013. Am. J. Respir. Cell Mol. Biol. 49: 571-81.

Citations 1 to 1 of 1 total
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