Catalog Number: 6311
Alternate Names: GF196960
Chemical Name: (6R,12aR)-6-(1,3-Benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methylpyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
Biological Activity
Potent and highly selective PDE5 inhibitor (IC50 = 5 nM). Exhibits > 2000-fold selectivity for PDE5 over PDEs 1,2,3 and 4 and 1000-fold selectivity over PDE6. Reduces blood pressure in hypertensive rats. Also delays tumor growth in a mouse model via inhibition of MDSC-mediated immunosuppression. Orally bioavailable.
Technical Data
  • M.Wt:
    389.4
  • Formula:
    C22H19N3O4
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at -20°C
  • CAS No:
    171596-29-5
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues.
    Daugan et al.
    J.Med.Chem., 2003;46:4533
  2. Phosphodiesterase-5 inhibition augments endogenous antitumor immunity by reducing myeloid-derived suppressor cell function.
    Serafini et al.
    J.Exp.Med., 2006;203:2691
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