8-Bromo-cGMP sodium, a membrane-permeable analogue of cGMP, is a PKG (protein kinase G) activator. 8-Bromo-cGMP sodium significantly inhibits Ca macroscopic currents and impairs insulin release stimulated with high K. 8-Bromo-cGMP sodium has antinociceptive effects and results in vasodilator responses.
体外研究
8-Bromo-cGMP sodium (1-100 μM; 8 h) increases resistance of LLC-PK1 cells to CsA toxicity concentration-dependently.
8-Bromo-cGMP sodium (1-100 μM; 16 h) induces the synthesis of HO-1 protein in a concentration-dependent fashion.
Cell Viability Assay
Cell Line:
LLC-PK1 cells (ATCC CL 101)
Concentration:
1-100 μM
Incubation Time:
8 hours
Result:
Increased resistance of LLC-PK1 cells to Cyclosporin A (CsA) toxicity concentration-dependently and augmented cell viability by up to 65%.
Western Blot Analysis
Cell Line:
LLC-PK1 cells (ATCC CL 101)
Concentration:
1-100 μM
Incubation Time:
16 hours
Result:
Induced the synthesis of HO-1 protein in a concentration-dependent fashion.
体内研究
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.
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).
分子式
C10H10N5O7Pbr-.Na+
分子量
446.08
CAS号
51116-01-9
运输条件
Room temperature in continental US; may vary elsewhere.