BRL 50481 Property

Melting point:

65-67°C

Boiling point:

391.1±52.0 °C(Predicted)

Density 

1.334±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: 12 mg/mL

form 

solid

pka

-5?+-.0.70(Predicted)

color 

white

Stability:

Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.

Safety

WGK Germany 

3

HS Code 

2935.90.9500

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

BRL 50481 Chemical Properties,Usage,Production

Description

BRL-50481 (433695-36-4) is a potent and selective inhibitor of phosphodiesterase-7 (PDE7), Ki=180 nM.1?Induces apoptosis in chronic lymphocytic leukemia cells which express PDE7B.2?BRL-50481 increases mineralization in osteoblasts differentiated from hMSC.3?Cell permeable.

Chemical Properties

Off-White Solid

Uses

A PDE7 inhibitor that has acceptable selectivity for in vivo studies

Definition

ChEBI: BRL-50481 is a C-nitro compound that is benzene substituted by N,N-dimethylaminosulfonyl, methyl and nitro groups at positions 1, 2 and 5, respectively. It is a phosphodiesterase inhibitor selective for the PDE7 subtype (Ki = 180 nM). It has a role as an EC 3.1.4.53 (3',5'-cyclic-AMP phosphodiesterase) inhibitor, a geroprotector and a bone density conservation agent. It is a sulfonamide, a C-nitro compound and a member of toluenes.

Biological Activity

Selective, substrate-competitive inhibitor of phosphodiesterase (PDE) 7 (K i = 180 nM). Displays > 200-fold selectivity over PDE1B, PDE1C, PDE2, PDE3, PDE4A4 and PDE5.

Biochem/physiol Actions

BRL 50481 is a potent and selective PDE7 inhibitor (IC50 = 260 nM).

storage

Store at +4°C

References

1) Smith et al. (2004), 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., 66 1679 2) Zhang et al. (2008), Cyclic nucleotide phosphodiesterase profiling reveals increased expression of phosphodiesterase 7B in chronic lymphocytic leukemia; Proc. Natl. Acad. Sci. USA 105 19532 3) Pekkinen et al. (2008), Effects of phosphodiesterase 7 inhibition by RNA interference on the gene expression and differentiation of human mesenchymal stem cell-derived osteoblasts; Bone 43 84