BRL-50481

BRL-50481
Clinical data
ATC code	None;
Identifiers
	show IUPAC name
CAS Number	433695-36-4 ;
PubChem CID	2921148;
IUPHAR/BPS	5154;
ChemSpider	2194720 ;
UNII	03G869PR3P;
ChEBI	CHEBI:93472;
ChEMBL	ChEMBL484928 ;
CompTox Dashboard (EPA)	DTXSID30195832 ;
Chemical and physical data
Formula	C9H12N2O4S
Molar mass	244.27 g·mol−1
3D model (JSmol)	Interactive image;
	show SMILES
	show InChI
	(what is this?)

BRL-50481 is a drug developed by GlaxoSmithKline which is the first compound that acts as a phosphodiesterase inhibitor selective for the PDE7 family.^[1] PDE7 activity is encoded by two genes, PDE7A and PDE7B. BRL-50481 actually shows about an 80-fold preference for the PDE7A subtype, for which it was developed, over PDE7B.^[2] BRL-50481 has been shown to increase mineralisation activity in osteoblasts, suggesting a potential role for PDE7 inhibitors in the treatment of osteoporosis.^[3]

References[]

^ Smith SJ, Cieslinski LB, Newton R, Donnelly LE, Fenwick PS, Nicholson AG, et al. (December 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" (PDF). Molecular Pharmacology. 66 (6): 1679–89. doi:10.1124/mol.104.002246. PMID 15371556. S2CID 9491524.
^ Alaamery MA, Wyman AR, Ivey FD, Allain C, Demirbas D, Wang L, et al. (April 2010). "New classes of PDE7 inhibitors identified by a fission yeast-based HTS". Journal of Biomolecular Screening. 15 (4): 359–67. doi:10.1177/1087057110362100. PMC 2854023. PMID 20228279.
^ Pekkinen M, Ahlström ME, Riehle U, Huttunen MM, Lamberg-Allardt CJ (July 2008). "Effects of phosphodiesterase 7 inhibition by RNA interference on the gene expression and differentiation of human mesenchymal stem cell-derived osteoblasts". Bone. 43 (1): 84–91. doi:10.1016/j.bone.2008.02.021. PMID 18420479.

[1] Smith SJ, Cieslinski LB, Newton R, Donnelly LE, Fenwick PS, Nicholson AG, et al. (December 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" (PDF). Molecular Pharmacology. 66 (6): 1679–89. doi:10.1124/mol.104.002246. PMID 15371556. S2CID 9491524.

[2] Alaamery MA, Wyman AR, Ivey FD, Allain C, Demirbas D, Wang L, et al. (April 2010). "New classes of PDE7 inhibitors identified by a fission yeast-based HTS". Journal of Biomolecular Screening. 15 (4): 359–67. doi:10.1177/1087057110362100. PMC 2854023. PMID 20228279.

[3] Pekkinen M, Ahlström ME, Riehle U, Huttunen MM, Lamberg-Allardt CJ (July 2008). "Effects of phosphodiesterase 7 inhibition by RNA interference on the gene expression and differentiation of human mesenchymal stem cell-derived osteoblasts". Bone. 43 (1): 84–91. doi:10.1016/j.bone.2008.02.021. PMID 18420479.

[1]

[2]

[3]

show v t Phosphodiesterase inhibitors
PDE1	MMPX SCH-51866 Vinpocetine
PDE2	BAY 60-7550 EHNA Oxindole
PDE3	Adibendan Amrinone (inamrinone) Anagrelide Bucladesine Cilostamide Cilostazol Enoximone KMUP-1 Milrinone Olprinone Pimobendan Quazinone RPL-554 Siguazodan Trequinsin Vesnarinone Zardaverine
PDE4	Apremilast Arofylline Atizoram CC-1088 Cilomilast Crisaborole Drotaverine Etazolate Filaminast Glaucine HT-0712 ICI-63197 Irsogladine Luteolin Mesembrenone Mesembrine Piclamilast Roflumilast Rolipram RPL-554 YM-976 Zardaverine
PDE5	Acetildenafil Aildenafil Avanafil Benzamidenafil Icariin Homosildenafil Lodenafil Mirodenafil MY-5445 Nitrosoprodenafil SCH-51866 Sildenafil Sulfoaildenafil T-0156 Tadalafil Udenafil Vardenafil
PDE7	BRL-50481
PDE9	BAY 73-6691 Paraxanthine
PDE10	Mardepodect Papaverine Tofisopam
PDE11
Non-selective	Aminophylline Caffeine Choline theophyllinate CPX Dipyridamole Doxofylline Enprofylline Ibudilast IBMX Luteolin Pentoxifylline Propentofylline Theobromine Theophylline Zaprinast
Unsorted	Diazepam Diprophylline DPCPX Furafylline Lisofylline Moxaverine Pentifylline Proxyphylline Quercetin Trapidil
See also: Receptor/signaling modulators

Clinical data

ATC code	None
Identifiers
show IUPAC name N,N,2-Trimethyl-5-nitrobenzenesulfonamide
CAS Number	433695-36-4^Y
PubChem CID	2921148
IUPHAR/BPS	5154
ChemSpider	2194720^N
UNII	03G869PR3P
ChEBI	CHEBI:93472
ChEMBL	ChEMBL484928^N
CompTox Dashboard (EPA)	DTXSID30195832
Chemical and physical data
Formula	C₉H₁₂N₂O₄S
Molar mass	244.27 g·mol⁻¹
3D model (JSmol)	Interactive image
show SMILES Cc1ccc(N(=O)=O)cc1S(=O)(=O)N(C)C
show InChI InChI=1S/C9H12N2O4S/c1-7-4-5-8(11(12)13)6-9(7)16(14,15)10(2)3/h4-6H,1-3H3^N Key:IFIUFCJFLGCQPH-UHFFFAOYSA-N^N
^NY (what is this?)