PDE- resistant PKG Inhibitors

  • 8- (2- Aminoethylthio)guanosine- 3', 5'- cyclic monophosphorothioate, Rp- isomer, immobilized on agarose ( Rp-8-AET-cGMPS-Agarose )
  • 8- Bromo- ß- phenyl- 1, N²- ethenoguanosine- 3', 5'- cyclic monophosphorothioate, Rp- isomer ( Rp-8-Br-PET-cGMPS )
  • 8- Bromoguanosine- 3', 5'- cyclic monophosphorothioate, Rp- isomer ( Rp-8-Br-cGMPS )
  • 8- (4- Chlorophenylthio)- ß- phenyl- 1, N²- ethenoguanosine- 3', 5'- cyclic monophosphorothioate, Rp- isomer ( Rp-8-pCPT-PET-cGMPS )
  • 8- (4- Chlorophenylthio)guanosine- 3', 5'- cyclic monophosphorothioate, Rp- isomer ( Rp-8-pCPT-cGMPS )
  • Guanosine- 3', 5'- cyclic monophosphorothioate, Rp-isomer ( Rp- cGMPS )
     

  • 8- (2- Aminoethylthio)guanosine- 3', 5'- cyclic monophosphorothioate, Rp- isomer, immobilized on agarose
       ( Rp-8-AET-cGMPS-Agarose )
       Immobilized cGMP antagonist. used for affinity chromatography of various cyclic nucleotide-responsive proteins such as protein
       kinases, phosphodiesterases and others.
       Protected under US Patent 5,625,056 issued to BIOLOG LSI
    A 009 0.6 ml, 2.5 ml, 6 ml  

    8- Bromo- ß- phenyl- 1, N²- ethenoguanosine- 3', 5'- cyclic monophosphorothioate, Rp- isomer
       ( Rp-8-Br-PET-cGMPS )
       Selective and membrane-permeant inhibitor of both cyclic GMP dependent protein kinase I a and I ß and of retinal cGMP-gated
       ion channels.
       Butt et. al., Br. J. Pharmacol., 116, 3110 - 3116 (1995).
    P 007 1 uM/ ~0.6 mg, 5 x 1 uM CAS No.: [172806-20-1]

    8- Bromoguanosine- 3', 5'- cyclic monophosphorothioate, Rp- isomer ( Rp-8-Br-cGMPS )
       PDE-resistant inhibitor of protein kinase G I α and I ß .
       Zhuo et al., Nature 368, 635 - 639 (1994).
    B 005 5 uM/ ~2.3 mg, 5 x 5 uM CAS No.: [150418-07-8]

    8- (4- Chlorophenylthio)- ß- phenyl- 1, N²- ethenoguanosine- 3', 5'- cyclic monophosphorothioate, Rp- isomer
       ( Rp-8-pCPT-PET-cGMPS )
       Potent inhibitor of protein kinase G. Most probably retinal cGMP-gated ion channels are inhibited as well.
       Broderick, K.E.; Mol. Endocrinol., 21, 1148 - 1162 (2007)
    C 046 1 uM/ ~0.6 mg, 5 x 1 uM CAS No.: [pending]

    8- (4- Chlorophenylthio)guanosine- 3', 5'- cyclic monophosphorothioate, Rp- isomer ( Rp-8-pCPT-cGMPS )
       Potent selective inhibitor of protein kinase G I a, I ß and especially of type II.
       Butt et al., Eur. J. Pharmacol., 269, 265 - 268 (1994); Gamm et al., J. Biol. Chem., 270, 27380 - 27388 (1996); Kramer et al., J. Neurosci., 16, 1285 - 1293 (1996).
    C 013 1 uM/ ~0.5 mg, 5 x 1 uM CAS No.: [153660-04-9]

    Guanosine- 3', 5'- cyclic monophosphorothioate, Rp-isomer ( Rp- cGMPS )
       Inhibitor of protein kinase G Iα. Resistant against mammalian cyclic nucleotide-dependent phosphodiesterases, no metabolic
       side effects.
       Butt et al., FEBS Lett., 263, 47 - 50 (1990).
    G 016 1 uM/ ~0.5 mg, 5 x 1 uM CAS No.: [153660-04-9]