Date published: 2026-4-30

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PDE5A Inhibitors

PDE5A inhibitors belong to a chemical class of compounds that specifically target and inhibit the enzyme phosphodiesterase type 5A. This class of inhibitors works by selectively blocking the action of the phosphodiesterase enzyme, which is responsible for the breakdown of cyclic guanosine monophosphate (cGMP). By inhibiting PDE5A, these compounds effectively enhance the concentration of cGMP in various tissues and cells throughout the body. The mechanism of action of PDE5A inhibitors involves binding to the active site of the phosphodiesterase enzyme, blocking it from hydrolyzing cGMP. By doing so, these inhibitors allow cGMP to accumulate and exert its physiological effects for a more prolonged period. Elevated levels of cGMP have various downstream effects, primarily through activation of protein kinase G (PKG), leading to multiple signaling cascades. PDE5A inhibitors display selectivity towards the phosphodiesterase enzyme isoform 5A, thereby minimizing the chance for cross-reactivity with other phosphodiesterase isoforms. This selectivity ensures that the pharmacological effects of these inhibitors are primarily mediated through the inhibition of PDE5A, without significant interference with other phosphodiesterase enzymes. The use of PDE5A inhibitors has been extensively explored and researched for their effects in different physiological processes and conditions. These inhibitors modulate smooth muscle tone, vasodilation, platelet aggregation, and cell proliferation. Furthermore, their effects on cGMP signaling have been implicated in the regulation of cardiovascular function, neurotransmission, and cell growth.

Items 1 to 10 of 18 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Tadalafil

171596-29-5sc-208412
50 mg
$180.00
13
(2)

Tadalafil functions as a selective inhibitor of phosphodiesterase type 5 (PDE5), characterized by its unique binding affinity to the enzyme's active site. This interaction stabilizes the enzyme-substrate complex, leading to a significant reduction in the hydrolysis of cyclic guanosine monophosphate (cGMP). The compound's distinct molecular structure facilitates specific hydrogen bonding and hydrophobic interactions, enhancing its potency and selectivity in modulating cGMP levels within cellular pathways.

MBCQ

150450-53-6sc-221874
sc-221874A
5 mg
25 mg
$74.00
$224.00
1
(1)

MBCQ acts as a potent phosphodiesterase type 5 (PDE5) inhibitor, exhibiting a unique mechanism of action through its selective binding to the enzyme's allosteric site. This interaction alters the enzyme's conformation, effectively diminishing its catalytic activity. The compound's intricate molecular design promotes specific electrostatic interactions and steric hindrance, which contribute to its enhanced stability and prolonged efficacy in regulating cyclic nucleotide signaling pathways.

Ibudilast

50847-11-5sc-203080
10 mg
$218.00
1
(1)

Ibudilast functions as a selective phosphodiesterase type 5 (PDE5) inhibitor, characterized by its ability to modulate enzyme activity through competitive binding at the active site. This compound exhibits unique kinetic properties, allowing for a gradual onset of action. Its structural features facilitate specific hydrogen bonding and hydrophobic interactions, enhancing its affinity for the enzyme. Additionally, Ibudilast's conformational flexibility may influence substrate accessibility, impacting overall enzymatic regulation.

4-{[3′,4′-(Methylenedioxy)benzyl]amino}-6-methoxyquinazoline

150450-42-3sc-352371
1 mg
$140.00
(0)

4-{[3',4'-(Methylenedioxy)benzyl]amino}-6-methoxyquinazoline acts as a phosphodiesterase type 5 (PDE5A) inhibitor, distinguished by its intricate molecular architecture that promotes selective binding. The presence of methylenedioxy and methoxy groups enhances electron density, facilitating unique π-π stacking interactions with the enzyme. This compound's dynamic conformational changes may optimize its interaction with PDE5A, potentially influencing reaction kinetics and substrate turnover rates.

N-Desethyl Vardenafil

448184-46-1sc-208024
sc-208024A
sc-208024B
sc-208024C
sc-208024D
sc-208024E
5 mg
10 mg
25 mg
50 mg
100 mg
500 mg
$320.00
$660.00
$1480.00
$2600.00
$3525.00
$10000.00
4
(1)

N-Desethyl Vardenafil is a selective phosphodiesterase type 5 (PDE5A) inhibitor characterized by its unique structural features that enhance binding affinity. The compound exhibits significant hydrophobic interactions due to its aromatic rings, which stabilize the enzyme-inhibitor complex. Its ability to form hydrogen bonds with key amino acid residues in the active site may modulate enzyme activity, influencing the overall catalytic efficiency and substrate specificity.

Thiosildenafil

479073-79-5sc-208435
10 mg
$320.00
2
(0)

Thiosildenafil is a selective phosphodiesterase type 5 (PDE5A) inhibitor distinguished by its unique thiol group, which facilitates specific interactions with the enzyme's active site. This compound demonstrates a notable capacity for conformational flexibility, allowing it to adapt to various binding environments. Its electron-rich structure enhances π-π stacking interactions, contributing to a robust stabilization of the enzyme-inhibitor complex and potentially influencing reaction kinetics.

Avanafil

330784-47-9sc-397683
sc-397683A
sc-397683B
sc-397683C
sc-397683D
10 mg
100 mg
1 g
5 g
50 g
$260.00
$390.00
$490.00
$940.00
$8000.00
1
(0)

Avanafil is a PDE5A inhibitor used in the research of ED. It is known for its rapid onset of action compared to other PDE5A inhibitors.

rac Xanthoanthrafil

1020251-53-9sc-208282
sc-208282A
sc-208282B
5 mg
250 mg
500 mg
$734.00
$4692.00
$8874.00
(0)

Rac Xanthoanthrafil is a selective phosphodiesterase type 5 (PDE5A) inhibitor characterized by its unique structural motifs that promote specific hydrogen bonding and hydrophobic interactions within the enzyme's active site. Its distinct stereochemistry allows for enhanced molecular recognition, leading to increased binding affinity. The compound's dynamic conformational changes facilitate optimal alignment with the enzyme, influencing catalytic efficiency and modulating reaction pathways.

(1R,3S)-1-(1,3-Benzodioxol-5-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylic Acid Methyl Ester

171596-44-4sc-391567
25 mg
$360.00
(0)

(1R,3S)-1-(1,3-Benzodioxol-5-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylic Acid Methyl Ester exhibits remarkable selectivity as a phosphodiesterase type 5 (PDE5A) inhibitor. Its intricate molecular architecture enables effective π-π stacking and electrostatic interactions, enhancing its binding stability. The compound's unique functional groups contribute to its ability to modulate enzyme kinetics, influencing substrate accessibility and reaction dynamics within the PDE5A catalytic environment.

Vardenafil, Hydrochloride Salt

224785-91-5sc-394434
sc-394434A
sc-394434B
25 mg
100 mg
1 g
$89.00
$206.00
$401.00
(0)

Vardenafil, Hydrochloride Salt is characterized by its unique ability to selectively inhibit phosphodiesterase type 5 (PDE5A) through specific molecular interactions. The compound's structural features facilitate strong hydrogen bonding and hydrophobic interactions, optimizing its affinity for the enzyme's active site. This selective binding alters the enzyme's conformational dynamics, effectively modulating the hydrolysis of cyclic GMP, thereby influencing downstream signaling pathways.