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PDE1A Inhibitors

PDE1A inhibitors encompass a diverse group of chemical compounds specifically designed or identified for their ability to inhibit the activity of the Phosphodiesterase 1A (PDE1A) enzyme. PDE1A is a member of the phosphodiesterase family, which plays a crucial role in regulating intracellular levels of cyclic nucleotides, cAMP, and cGMP. These cyclic nucleotides are pivotal in various physiological processes, including vascular regulation, neuronal activity, and cardiac function. The inhibition of PDE1A leads to an increase in the levels of these cyclic nucleotides, thereby modulating the physiological processes they govern. The inhibitors listed, such as Vinpocetine, typically function by binding to the catalytic site of the PDE1A enzyme. This binding can be competitive, where the inhibitor mimics the structure of the substrate (cGMP or cAMP), or non-competitive, where the inhibitor binds to a site other than the active site, altering the enzyme's conformation and reducing its activity. The selectivity of these inhibitors varies; some, like Vinpocetine and MY-5445, are more selective towards PDE1A, whereas others, including Zardaverine and Anagrelide, also inhibit other PDE isoforms, such as PDE3 and PDE4. The specificity of these inhibitors is a critical factor in their utility. Chemically, these inhibitors range from synthetic derivatives to naturally occurring compounds. Vinpocetine, for instance, is a synthetic alkaloid derivative, while others, like IBMX, are synthetic xanthine derivatives.

Product Name	CAS #	Catalog #	QUANTITY	Price	Citations	RATING
Ibudilast	50847-11-5	sc-203080	10 mg	$218.00	1	(1)
Ibudilast functions as a selective phosphodiesterase 1A (PDE1A) inhibitor, distinguished by its ability to engage in specific electrostatic interactions with the enzyme's active site. This compound demonstrates unique conformational flexibility, allowing it to stabilize transient enzyme-substrate complexes. Its kinetic profile reveals a non-competitive inhibition mechanism, which alters the enzyme's turnover rate and impacts calcium signaling pathways, showcasing its intricate role in cellular regulation.
Vinpocetine	42971-09-5	sc-201204 sc-201204A sc-201204B	20 mg 100 mg 15 g	$55.00 $214.00 $2400.00	4	(1)
Vinpocetine is a selective inhibitor of PDE1A. It binds to the catalytic site, reducing the enzyme's ability to hydrolyze cGMP and cAMP.
8-Methoxymethyl-IBMX	78033-08-6	sc-201192 sc-201192A	10 mg 50 mg	$354.00 $1173.00	2	(0)
8-MM-IBMX acts as a non-selective inhibitor of PDE1A. It competitively inhibits the enzyme by mimicking the structure of cGMP.
Zardaverine	101975-10-4	sc-201208 sc-201208A	5 mg 25 mg	$88.00 $379.00	1	(0)
Zardaverine is a dual PDE3/PDE4 inhibitor that also shows inhibitory activity against PDE1A, blocking the enzyme's action on cAMP and cGMP.
MY-5445	78351-75-4	sc-201195	10 mg	$153.00	2	(1)
MY-5445 is a selective PDE1A inhibitor, effectively blocking the enzyme′s catalytic activity towards cGMP and cAMP.
8-Bromoguanosine 3′, 5′ -cyclic monophosphoric acid	31356-94-2	sc-291685 sc-291685A	5 mg 10 mg	$116.00 $206.00		(0)
8-Br-cGMP inhibits PDE1A by mimicking cGMP's structure, competitively binding to the active site and reducing enzyme activity.
Anagrelide hydrochloride	58579-51-4	sc-203513 sc-203513A	10 mg 50 mg	$103.00 $587.00	1	(0)
Anagrelide, a PDE3 inhibitor, also exhibits inhibitory activity against PDE1A, interfering with the hydrolysis of cAMP and cGMP.
EHNA hydrochloride	51350-19-7	sc-201184 sc-201184A	10 mg 50 mg	$104.00 $379.00	6	(1)
EHNA hydrochloride inhibits PDE1A by competing with cAMP, thereby reducing the enzyme′s activity in hydrolyzing cAMP and cGMP.
IBMX	28822-58-4	sc-201188 sc-201188B sc-201188A	200 mg 500 mg 1 g	$260.00 $350.00 $500.00	34	(1)
IBMX is a non-selective inhibitor of PDE1A, reducing the hydrolysis of cAMP and cGMP by competitively binding to the active site.
Milrinone	78415-72-2	sc-201193 sc-201193A	10 mg 50 mg	$165.00 $697.00	7	(0)
Milrinone, primarily a PDE3 inhibitor, also exhibits some inhibitory activity towards PDE1A, particularly affecting cAMP hydrolysis.

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PDE1A Inhibitors

Ibudilast

Vinpocetine

8-Methoxymethyl-IBMX

Zardaverine

MY-5445

8-Bromoguanosine 3′, 5′ -cyclic monophosphoric acid

Anagrelide hydrochloride

EHNA hydrochloride

IBMX

Milrinone