PDE6G Inhibitors
Chemical inhibitors of PDE6G operate by leveraging the protein's role in the hydrolysis of cGMP to 5'-GMP, a critical step in phototransduction within the visual process. Sildenafil, Vardenafil, and Tadalafil are selective inhibitors of PDE5, a closely related phosphodiesterase, and due to the structural similarity in their catalytic sites, they can also bind to and inhibit PDE6G. This binding prevents PDE6G from performing its normal function of breaking down cGMP, resulting in increased levels of this cyclic nucleotide within the cellular environment. Zaprinast, with its selective inhibition profile for PDE5 and PDE6, directly inhibits PDE6G, leading to similar outcomes in the buildup of cGMP. Dipyridamole and Theophylline, as non-selective phosphodiesterase inhibitors, increase cGMP levels indirectly by inhibiting its degradation, thereby reducing PDE6G activity because of the decreased availability of its substrate.
Continuing with this theme of substrate competition and indirect inhibition, Cilostazol and Anagrelide, through their inhibition of PDE3, can cause an increase in cGMP levels. This rise in cGMP can inhibit PDE6G by occupying the enzyme's active site, effectively preventing the hydrolysis of its substrate. Icariin and Quercetin, although not as selective, function similarly by inhibiting PDE5 and other PDEs, consequently increasing the concentration of cGMP within the cell and leading to a functional inhibition of PDE6G. Pentoxifylline, with its broad PDE inhibition spectrum, elevates both cAMP and cGMP levels, with the latter inhibiting PDE6G. Milrinone, finally, selectively inhibits PDE3, which indirectly leads to increased cGMP levels, and this elevation in cGMP can inhibit PDE6G through a feedback loop mechanism, where the high concentration of the substrate cGMP competitively inhibits the breakdown of cGMP by PDE6G.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Vardenafil | 224785-90-4 | sc-362054 sc-362054A sc-362054B | 100 mg 1 g 50 g | $516.00 $720.00 $16326.00 | 7 | |
Vardenafil is another selective inhibitor of PDE5, which, like Sildenafil, can also inhibit PDE6G due to the structural similarity between PDE5 and PDE6. Vardenafil binds to the catalytic site of PDE5 and consequently can inhibit PDE6G, resulting in elevated levels of cGMP within cells. | ||||||
Tadalafil | 171596-29-5 | sc-208412 | 50 mg | $176.00 | 13 | |
Tadalafil is a potent inhibitor of PDE5, known for its long half-life. By inhibiting PDE5, Tadalafil can indirectly inhibit PDE6G due to the overlapping substrate specificity, leading to an increase in intracellular cGMP concentration, which is the substrate for PDE6G. | ||||||
Zaprinast (M&B 22948) | 37762-06-4 | sc-201206 sc-201206A | 25 mg 100 mg | $103.00 $245.00 | 8 | |
Zaprinast is a selective inhibitor of PDE5 and PDE6. It increases intracellular levels of cGMP by inhibiting its breakdown, thereby functionally inhibiting PDE6G by preventing it from hydrolyzing cGMP to 5'-GMP. | ||||||
Dipyridamole | 58-32-2 | sc-200717 sc-200717A | 1 g 5 g | $30.00 $100.00 | 1 | |
Dipyridamole is a non-selective phosphodiesterase inhibitor that increases intracellular cGMP levels by inhibiting its degradation. By doing so, it functionally inhibits PDE6G activity by reducing the availability of its substrate. | ||||||
Cilostazol | 73963-72-1 | sc-201182 sc-201182A | 10 mg 50 mg | $107.00 $316.00 | 3 | |
Cilostazol inhibits several phosphodiesterases, including PDE3, which can lead to an indirect increase in cGMP levels as a result of reduced cGMP degradation, thus inhibiting PDE6G functionality by substrate competition. | ||||||
Icariin | 489-32-7 | sc-279198 sc-279198A sc-279198B | 1 g 5 g 10 g | $142.00 $413.00 $814.00 | ||
Icariin is reported to inhibit PDE5 and could indirectly inhibit PDE6G by increasing cGMP levels due to the reduced hydrolysis of cGMP, which is the natural substrate for PDE6G. | ||||||
Quercetin | 117-39-5 | sc-206089 sc-206089A sc-206089E sc-206089C sc-206089D sc-206089B | 100 mg 500 mg 100 g 250 g 1 kg 25 g | $11.00 $17.00 $108.00 $245.00 $918.00 $49.00 | 33 | |
Quercetin is a flavonoid that has been shown to inhibit PDEs. By inhibiting these enzymes, quercetin can indirectly inhibit PDE6G by preventing the degradation of cGMP, thereby increasing its intracellular concentration. | ||||||
Anagrelide hydrochloride | 58579-51-4 | sc-203513 sc-203513A | 10 mg 50 mg | $103.00 $587.00 | 1 | |
Anagrelide inhibits PDE3, and through this inhibition, it can lead to an increase in cGMP levels indirectly, thus inhibiting PDE6G by elevating the concentration of its substrate, which in high levels can lead to feedback inhibition. | ||||||
Theophylline | 58-55-9 | sc-202835 sc-202835A sc-202835B | 5 g 25 g 100 g | $20.00 $31.00 $83.00 | 6 | |
Theophylline is a non-selective PDE inhibitor, and by inhibiting other PDEs, it can cause a non-specific increase in cGMP levels, which can result in the functional inhibition of PDE6G through substrate saturation. | ||||||
Pentoxifylline | 6493-05-6 | sc-203184 | 1 g | $20.00 | 3 | |
Pentoxifylline is a non-selective inhibitor of PDEs, including PDE3 and PDE4, which leads to increased cAMP and cGMP levels, thereby indirectly inhibiting PDE6G by increasing the intracellular concentration of cGMP. | ||||||