BRL 50481
BRL 50481 Basic information
- Product Name:
- BRL 50481
- Synonyms:
-
- 5-NITRO-2,N,N-TRIMETHYLBENZENESULFONAMIDE
- BRL 50481
- N,N,2-TRIMETHYL-5-NITRO-BENZENESULFONAMIDE
- 3-(N,N-Dimethylsulfonamido)-4-methylnitrobenzene,5-Nitro-2-N,N-trimethylbenzenesulfonamide
- Benzenesulfonamide, N,N,2-trimethyl-5-nitro-
- -50481
- CAS:
- 433695-36-4
- MF:
- C9H12N2O4S
- MW:
- 244.27
- EINECS:
- 1592732-453-0
- Product Categories:
-
- All Inhibitors
- Inhibitors
- Cyclic Nucleotide related
- Mol File:
- 433695-36-4.mol
BRL 50481 Chemical Properties
- 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.
MSDS
- Language:English Provider:SigmaAldrich
BRL 50481 Usage And Synthesis
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
BRL 50481Supplier
- Tel
- 010-82848833 400-666-7788
- jkinfo@jkchemical.com
- Tel
- 821-50328103-801 18930552037
- 3bsc@sina.com
- Tel
- 021-50135380
- shchemsky@sina.com
- Tel
- 021-61312847 13636370518
- shyysw007@163.com
- Tel
- 03-36680489
- Sales-JP@TCIchemicals.com
BRL 50481(433695-36-4)Related Product Information
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- BRL 50481
- 1-(2-METHYL-5-NITRO-BENZENESULFONYL)-PIPERIDINE-4-CARBOXYLIC ACID
- 1-[(2-METHYL-5-NITROPHENYL)SULFONYL]PIPERIDINE-2-CARBOXYLIC ACID
- TIMTEC-BB SBB001165
- 4-[4-[(2-METHYL-5-NITROPHENYL)SULFONYL]PIPERAZIN-1-YL]-4-OXOBUTANOIC ACID
- 1-[(2-METHYL-5-NITROPHENYL)SULFONYL]PIPERAZINE