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8-Bromo-cGMP sodium

Cat. No. M22480
8-Bromo-cGMP sodium Structure
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Biological Activity

8-Bromo-cGMP sodium is a PKG (protein kinase G) activator, it is a membrane-permeable analogue of cGMP. 8-Bromo-cGMP sodium significantly inhibits Ca2+ macroscopic currents and impairs insulin release stimulated with high K+. 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. 

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). 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).

Chemical Information
Molecular Weight 446.08
Formula C10H10BrN5NaO7P
CAS Number 51116-01-9
Solubility (25°C) Water 90 mg/mL
Storage -20°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Hong-Guang Nie, et al. J Physiol. Regulation of epithelial sodium channels by cGMP/PKGII

[2] S T Christensen, et al. Cell Biol Int. Cell death, survival and proliferation in Tetrahymena thermophila. Effects of insulin, sodium nitroprusside, 8-Bromo cyclic GMP, NG-methyl-L-arginine and methylene blue

[3] R L Chevalier, et al. Am J Physiol. Extracellular cGMP inhibits transepithelial sodium transport by LLC-PK1 renal tubular cells

[4] D W Cheung, et al. Br J Pharmacol. The effects of sodium nitroprusside and 8-bromo-cyclic GMP on electrical and mechanical activities of the rat tail artery

[5] E Butt, et al. Biochem Pharmacol. Analysis of the functional role of cGMP-dependent protein kinase in intact human platelets using a specific activator 8-para-chlorophenylthio-cGMP

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