PDE 3A Activators
PDE3A activators encompass a range of chemical compounds that either directly or indirectly enhance the hydrolytic activity of PDE3A on cyclic AMP (cAMP), a critical second messenger in cellular signaling. Prominent among these activators is Forskolin, which directly stimulates adenylyl cyclase, consequently raising intracellular cAMP levels and activating protein kinase A (PKA). PKA phosphorylates PDE3A, which increases its activity in breaking down cAMPto AMP, thereby fine-tuning cellular responses to hormonal stimulation. Similarly, beta-adrenoceptor agonists like Isoproterenol and Dobutamine increase cAMP by activating adenylyl cyclase, and the surge in cAMP activates PKA, which in turn phosphorylates and activates PDE3A. On the other hand, selective PDE inhibitors such as Milrinone, Cilostazol, Anagrelide, and Amrinone transiently inhibit PDE3A, leading to a compensatory increase in cAMP levels that enhance PDE3A activity through PKA-mediated phosphorylation as a feedback mechanism.
The regulation of PDE3A is further nuanced by the use of nonspecific PDE inhibitors like IBMX and selective PDE4 inhibitors such as Rolipram, which by inhibiting other PDEs, result in elevated cAMP levels and indirectly promote PDE3A activation via PKA phosphorylation. Prostaglandin E1 (Alprostadil) engages a similar pathway; it activates its receptors to increase cAMP levels, leading to the activation of PKA and subsequent phosphorylation of PDE3A. Catecholamines such as Epinephrine and Norepinephrine also activate PDE3A by binding to adrenergic receptors, which stimulates adenylyl cyclase, increases cAMP, and activates PKA, culminating in the phosphorylation of PDE3A. These various chemical compounds, despite their diverse initial targets and mechanisms, converge on the pathway that regulates PDE3A activity, ensuring the precise modulation of cAMP levels in response to physiological demands.
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| 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 directly stimulates adenylyl cyclase, increasing cAMP levels, which in turn activates protein kinase A (PKA). PKA phosphorylates and thus enhances the activity of PDE3A, leading to increased hydrolysis of cAMP to AMP. | ||||||
Milrinone | 78415-72-2 | sc-201193 sc-201193A | 10 mg 50 mg | $165.00 $697.00 | 7 | |
Milrinone is a selective PDE3 inhibitor that indirectly upregulates PDE3A activity by eliciting a compensatory mechanism. The transient inhibition causes an increase in intracellular cAMP which further stimulates the cAMP-PKA pathway, indirectly promoting PDE3A phosphorylation and activation. | ||||||
Cilostazol | 73963-72-1 | sc-201182 sc-201182A | 10 mg 50 mg | $109.00 $322.00 | 3 | |
Cilostazol inhibits PDE3, leading to increased cAMP levels. Similar to Milrinone, the initial inhibition by Cilostazol causes a feedback activation of the cAMP-PKA pathway, which can result in enhanced phosphorylation and activation of PDE3A. | ||||||
Anagrelide | 68475-42-3 | sc-491875 | 25 mg | $150.00 | ||
Anagrelide inhibits PDE3, increasing cAMP levels and subsequently activating PKA. PKA then phosphorylates PDE3A, enhancing its activity to regulate platelet aggregation and vascular smooth muscle function. | ||||||
Isoproterenol Hydrochloride | 51-30-9 | sc-202188 sc-202188A | 100 mg 500 mg | $28.00 $38.00 | 5 | |
Isoproterenol is a beta-adrenoceptor agonist that increases intracellular cAMP levels by activating adenylyl cyclase. The rise in cAMP activates PKA, which can phosphorylate and activate PDE3A. | ||||||
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 nonspecific inhibitor of phosphodiesterases. Its inhibition of other PDEs raises cAMP levels, indirectly invoking a compensatory increase in PDE3A activity through PKA-mediated phosphorylation. | ||||||
Rolipram | 61413-54-5 | sc-3563 sc-3563A | 5 mg 50 mg | $77.00 $216.00 | 18 | |
Rolipram selectively inhibits PDE4, causing an increase in cAMP levels and activation of PKA. PKA can then phosphorylate and activate PDE3A as part of a feedback mechanism. | ||||||
PGE1 (Prostaglandin E1) | 745-65-3 | sc-201223 sc-201223A | 1 mg 10 mg | $31.00 $145.00 | 16 | |
PGE1 activates its receptor, which couples to adenylyl cyclase, raising cAMP levels and activating PKA. PKA enhances PDE3A activity through phosphorylation. | ||||||
Dobutamine | 34368-04-2 | sc-507555 | 100 mg | $295.00 | ||
Dobutamine is a beta-adrenergic agonist that indirectly increases cAMP levels by stimulating adenylyl cyclase. The elevated cAMP activates PKA, which can enhance PDE3A activity by phosphorylation. | ||||||
(−)-Epinephrine | 51-43-4 | sc-205674 sc-205674A sc-205674B sc-205674C sc-205674D | 1 g 5 g 10 g 100 g 1 kg | $41.00 $104.00 $201.00 $1774.00 $16500.00 | ||
Epinephrine activates adrenergic receptors, leading to increased adenylyl cyclase activity and cAMP levels. The subsequent activation of PKA results in phosphorylation and activation of PDE3A. | ||||||