BRL-50481

BRL-50481
BRL-50481
BRL-50,481.svg
임상자료
ATC 코드
  • 없음
식별자
  • N,N,2-트리메틸-5-니트로벤젠설폰아미드
CAS 번호
펍켐 CID
IUPHAR/BPS
켐스파이더
유니
체비
켐벨
CompTox 대시보드 (EPA)
화학 및 물리적 데이터
공식C9H12N2O4S
어금질량244.27 g·201−1
3D 모델(JSmol)
  • Cc1cc(N(=O)=O)cc1S(=O)N(C)C
  • InChi=1S/C9H12N2O4S/c1-7-4-5-8(11(12)-13)6-9-9(7)16(14,15)10(2)3/h4-6H,1-3H3 ☒N
  • 키:IFIUFCJFLGCQPH-UHFFFAOYSA-N ☒N
☒NcheckY (이게 뭐야?) (iii)

BRL-50481은 글락소스미스클라인이 개발한 약물로, PDE7 계열에 선택적으로 인산염 억제제 역할을 하는 최초의 화합물이다.[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]

참조

  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.