BRL 50481, also known as 433695-36-4, is a potent and selective inhibitor of phosphodiesterase-7 (PDE7) with a Ki value of 180 nM. It is an off-white solid that exhibits cell permeability and has been found to induce apoptosis in chronic lymphocytic leukemia cells expressing PDE7B. Additionally, BRL 50481 has been shown to increase mineralization in osteoblasts differentiated from hMSC.
433695-36-4
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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-
- CAS NO:433695-36-4
- Molecular Formula: C9H12N2O4S
- Molecular Weight: 244.27
- EINECS: 1592732-453-0
- Product Categories: All Inhibitors;Inhibitors;Cyclic Nucleotide related
- Mol File: 433695-36-4.mol
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Chemical Properties
- Melting Point: 65-67°C
- Boiling Point: 391.1°C at 760 mmHg
- Flash Point: 190.4°C
- Appearance: white/solid
- Density: 1.334g/cm3
- Vapor Pressure: 2.52E-06mmHg at 25°C
- Refractive Index: 1.561
- Storage Temp.: 2-8°C
- Solubility: DMSO: 12 mg/mL
- PKA: -5?+-.0.70(Predicted)
- 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.
- CAS DataBase Reference: BRL 50481(CAS DataBase Reference)
- NIST Chemistry Reference: BRL 50481(433695-36-4)
- EPA Substance Registry System: BRL 50481(433695-36-4)
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Safety Data
- Hazard Codes: N/A
- Statements: N/A
- Safety Statements: N/A
- WGK Germany: 3
- RTECS:
- HazardClass: N/A
- PackingGroup: N/A
- Hazardous Substances Data: 433695-36-4(Hazardous Substances Data)
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433695-36-4 Usage
Uses
Used in Pharmaceutical Industry:BRL 50481 is used as a PDE7 inhibitor for its acceptable selectivity, making it a valuable compound for in vivo studies. Its ability to induce apoptosis in chronic lymphocytic leukemia cells and increase mineralization in osteoblasts suggests potential applications in the treatment of leukemia and bone-related conditions.
Used in Research and Development:
BRL 50481 is used as a research tool for studying the role of PDE7 in various cellular processes. Its selectivity and potency make it an ideal candidate for investigating the effects of PDE7 inhibition on cell signaling pathways and other biological functions.
Used in Drug Development:
BRL 50481's properties as a PDE7 inhibitor and its effects on apoptosis and mineralization make it a promising starting point for the development of new drugs targeting leukemia, bone disorders, and other related conditions. Its cell permeability also suggests potential for use in drug delivery systems to improve the bioavailability and therapeutic outcomes of PDE7 inhibitors.
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).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 84Check Digit Verification of cas no
The CAS Registry Mumber 433695-36-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 4,3,3,6,9 and 5 respectively; the second part has 2 digits, 3 and 6 respectively.Calculate Digit Verification of CAS Registry Number 433695-36:
(8*4)+(7*3)+(6*3)+(5*6)+(4*9)+(3*5)+(2*3)+(1*6)=164
164 % 10 = 4
So 433695-36-4 is a valid CAS Registry Number.
InChI:InChI=1/C9H12N2O4S/c1-7-4-5-8(11(12)13)6-9(7)16(14,15)10(2)3/h4-6H,1-3H3
433695-36-4 Well-known Company Product Price
- Brand
- (Code)Product description
- CAS number
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- Price
- Detail
TCI America
(T3112) N,N,2-Trimethyl-5-nitrobenzenesulfonamide >98.0%(HPLC)(N)
433695-36-4
200mg
760.00CNY
- Detail
TCI America
(T3112) N,N,2-Trimethyl-5-nitrobenzenesulfonamide >98.0%(HPLC)(N)
433695-36-4
1g
2,660.00CNY
- Detail
Sigma
(B0936) BRL 50481 ≥98% (HPLC), solid
433695-36-4
B0936-5MG
1,606.41CNY
- Detail
Sigma
(B0936) BRL 50481 ≥98% (HPLC), solid
433695-36-4
B0936-25MG
6,347.25CNY
- Detail
433695-36-4Upstream product
433695-36-4Downstream Products
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BRL 50481
