Product Description: Rp-8-Br-PET-cGMPS sodium (Rp-8-Bromo-PET-cGMPS) is an analog of cyclic GMP (cGMP). It is a cell permeable, competitive, and reversible inhibitor of cGMP-dependent protein kinases (cGKs) that blocks activation of cGKI and cGKII by cGMP (Kis=35 and 30 nM). It less potently inhibits protein kinase A (Ki=11 μM) and cGMP-induced activation of cyclic nucleotide-gated channels (IC50=25 μM). In the absence of cGMP stimulation, Rp-8-bromo-PET-cGMPS can act as a partial agonist of cGKI (Ki=1 μM). Rp-8-bromo-PET-cGMPS is resistant to hydrolysis by phosphodiesterase 11.
Applications: COVID-19-immunoregulation
Formula: C18H14BrN5NaO6PS
References: [1]Jäger, et al. Activation of PDE10 and PDE11 phosphodiesterases. J. Biol. Chem. 287(2), 1210-1219 (2012).
CAS Number: 185246-32-6
Molecular Weight: 562.27
Research Area: Inflammation/Immunology
Target: PKG
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