BRL 50481 Struktur

BRL 50481

Bezeichnung:BRL 50481

CAS-Nr433695-36-4

Englisch Name:BRL 50481

CBNumberCB4485083

SummenformelC9H12N2O4S

Molgewicht244.27

MOL-Datei433695-36-4.mol

BRL 50481 physikalisch-chemischer Eigenschaften

Schmelzpunkt	65-67°C
Siedepunkt	391.1±52.0 °C(Predicted)
Dichte	1.334±0.06 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	DMSO: 12 mg/mL
Aggregatzustand	solid
pka	-5?+-.0.70(Predicted)
Farbe	white
Stabilität	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.

Sicherheit

WGK Germany	3
HS Code	2935.90.9500

Gefahreninformationscode (GHS)

BRL 50481 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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.
Chemische Eigenschaften
Off-White Solid
Verwenden
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.
Biologische Aktivität
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).
Lager
Store at +4°C
Einzelnachweise
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

BRL 50481 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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