8-Bromo-cGMP (sodium)

8-Bromo-cGMP sodium, a membrane-permeable analogue of cGMP, is a PKG (protein kinase G) activator. 8-Bromo-cGMP sodium significantly inhibits Ca²⁺ macroscopic currents and impairs insulin release stimulated with high K^+[1]. 8-Bromo-cGMP sodium has antinociceptive effects and results in vasodilator responses^[2]. In Vitro: 8-Bromo-cGMP sodium (1-100 μM; 8 h) increases resistance of LLC-PK1 cells to CsA toxicity concentration-dependently^[3].
8-Bromo-cGMP sodium (1-100 μM; 16 h) induces the synthesis of HO-1 protein in a concentration-dependent fashion^[3].
In Vivo: 8-Bromo-cGMP sodium (0.3, 1, 3.0 nmol; intrathecal administration; 10 min before test) dose-dependently and significantly increases the tail-flick latency in Vincristine-treated mice to the level observed in vehicle-treated naive mice (male ICR mice, 4weeks of age and weighing 20 g). Vincristine (0.05 mg/kg 1 day after the pre-drug tail-flick latency, and then 0.125 mg/kg twice a week for 6 weeks) can induce painful neuropathy in mice^[4].
8-Bromo-cGMP sodium (10 mg/kg; iv; single dose) results in vasodilator responses in eNOS-Tg mice and WT littermates in C57BL/6 background (19-35 g)^[5].