CNG-1 Activators
CNG-1 activators encompass a spectrum of chemical compounds that primarily fortify the channel's activity by modulating intracellular cyclic nucleotide levels, specifically cAMP. Compounds such as Forskolin, IBMX, Zaprinast, Cilostamide, Rolipram, Vinpocetine, Caffeine, Theophylline, Sildenafil, Dipyridamole, and Vardenafil, all function by either increasing the synthesis of cAMP or preventing its degradation by inhibiting various phosphodiesterases. This results in elevated cAMP levels that directly bind to CNG-1, leading to channel opening and enhanced ion flow. For instance, Forskolin directly stimulates adenylyl cyclase, thereby boosting cAMP synthesis, which in turn triggers the opening of CNG-1 channels.
On the other hand, IBMX and Zaprinast, while not increasing the synthesis of cAMP, prevent its breakdown, leading to a similar enhancement of CNG-1 activity by maintaining higher levels of cAMP that promote channel activation. The functional implications of these CNG-1 activators are grounded in their ability to heighten the channel's responsiveness to intracellular cAMP. By increasing the probability that CNG-1 will be in an open state, these activators facilitate the flow of ions across cellular membranes, which is critical for various physiological processes
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Forskolin | 66575-29-9 | sc-3562 sc-3562A sc-3562B sc-3562C sc-3562D | 5 mg 50 mg 1 g 2 g 5 g | $78.00 $153.00 $740.00 $1413.00 $2091.00 | 73 | |
Forskolin activates adenylyl cyclase, leading to increased cAMP levels, which in turn enhance the activity of CNG-1 by promoting cAMP binding to the channel, resulting in its opening. | ||||||
IBMX | 28822-58-4 | sc-201188 sc-201188B sc-201188A | 200 mg 500 mg 1 g | $260.00 $350.00 $500.00 | 34 | |
IBMX is a non-specific inhibitor of phosphodiesterases, which prevents the breakdown of cAMP, indirectly sustaining the activation of CNG-1 channels through elevated cAMP levels. | ||||||
Zaprinast (M&B 22948) | 37762-06-4 | sc-201206 sc-201206A | 25 mg 100 mg | $105.00 $250.00 | 8 | |
Zaprinast inhibits phosphodiesterases, particularly PDE5, leading to increased cAMP levels, thus enhancing the activity of CNG-1 by maintaining channel opening. | ||||||
Cilostamide (OPC 3689) | 68550-75-4 | sc-201180 sc-201180A | 5 mg 25 mg | $92.00 $357.00 | 16 | |
Cilostamide is a selective inhibitor of phosphodiesterase 3 (PDE3), which leads to an accumulation of cAMP, thereby potentiating the activity of CNG-1 channels. | ||||||
Rolipram | 61413-54-5 | sc-3563 sc-3563A | 5 mg 50 mg | $77.00 $216.00 | 18 | |
Rolipram inhibits phosphodiesterase 4 (PDE4), boosting intracellular cAMP levels and enhancing the functional activity of CNG-1 by increasing its probability of opening. | ||||||
Vinpocetine | 42971-09-5 | sc-201204 sc-201204A sc-201204B | 20 mg 100 mg 15 g | $55.00 $214.00 $2400.00 | 4 | |
Vinpocetine is a PDE1 inhibitor, which raises cAMP levels within cells, consequently enhancing the activity of CNG-1 channels by promoting their opening. | ||||||
Theophylline | 58-55-9 | sc-202835 sc-202835A sc-202835B | 5 g 25 g 100 g | $20.00 $32.00 $85.00 | 6 | |
Theophylline, similar to caffeine, is a non-selective phosphodiesterase inhibitor, which raises intracellular cAMP and thereby enhances the activity of CNG-1. | ||||||
Dipyridamole | 58-32-2 | sc-200717 sc-200717A | 1 g 5 g | $31.00 $102.00 | 1 | |
Dipyridamole inhibits various phosphodiesterases, leading to increased cAMP levels and thus enhancing CNG-1 activity by increasing the likelihood of channel opening. | ||||||
Vardenafil | 224785-90-4 | sc-362054 sc-362054A sc-362054B | 100 mg 1 g 50 g | $526.00 $735.00 $16653.00 | 7 | |
Vardenafil is a selective inhibitor of PDE5, increasing cAMP levels, and thereby indirectly enhancing CNG-1 activity by promoting the opening of its channels through cAMP binding. | ||||||