PDE

Inhibitory Selectivity
Catalog No.Inhibitor Name PDEPDE1PDE2PDE3PDE4PDE5PDE6PDE9APDE10AOther
A10804Roflumilast
****
A10216Cilomilast
***
A10883Tadalafil
***
A10733Pimobendan
**
A11073GSK256066
****
A11191PF-2545920
****
A10805Rolipram
**
A10217Cilostazol
**
A10592Milrinone
**
**
ATPase
A12619Avanafil
****
A10066Aminophylline
*
adenosine receptor
A15799TAK-063
****
A13722Deltarasin
***
A10541Luteolin
*
*
*
*
*
A10464Icariin
**
mAChR,AChR
A10480Irsogladine
A10319Dipyridamole
A10339Dyphylline
A11527PF-8380
***
A10965Vardenafil
***
****
A11019Ibudilast (KC-404)
A11289Apremilast (CC 10004)
***
A11326Bay 60-7550
****
A11602Vinpocetine
Sodium channel
A12550Zardaverine
**
**
A12631Sildenafil
***
***
A12776AN2728
***
A13121PF-04447943
***
A13467MK-0359
A13596Cilostamide
***
A15191Nortadalafil
A15197Oglemilast
****
A15198Olprinone Hydrochloride

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.



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Catalog No. Product Name Application Product Information
A11602

Vinpocetine

PDE1 inhibitor
Vinpocetine is a Ca2+-calmodulin-dependent phosphodiesterase I (PDE1) inhibitor.
A12631

Sildenafil

PDE5 inhibitor
Sildenafil, one of the selective phosphodiesterase-5 (PDE5) inhibitors(IC50= 5.22 nM), is considered the best treatment for erectile dysfunction.
A15799

TAK-063

PDE10A inhibitor‎
TAK-063 is a highly potent, selective and orally active PDE10A inhibitor with IC50 of 0.30 nM; >15000-fold selectivity over other PDEs.
A15198

Olprinone Hydrochloride

PDE3 inhibitor
Olprinone is a selective phosphodiesterase 3 (PDE3) inhibitor.
A15197

Oglemilast

PDE4 inhibitor
Oglemilast is a potent inhibitor of PDE4.
A15191

Nortadalafil

PDE5 inhibitor
Nortadalafil is demethyl Tadalafil, which is a PDE5 inhibitor, currently marketed in pill form for treating erectile dysfunction (ED) under the name Cialis; and under the name Adcirca for the treatment of pulmonary arterial hypertension.
A15097

GSK256066 2,2,2-trifluoroacetic acid

PDE Inhibitor
GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7.
A13467

MK-0359

PDE4 inhibitor
MK-0359 is a selective and potent oral PDE4 inhibitor, in chronic asthma.
A13596

Cilostamide

PDE3 inhibitor
Cilostamide is a selective inhibitor of phosphodiesterase (PDE)3A and PDE3B with IC50 values of 27 and 50 nM, respectively.
A12550

Zardaverine

PDE 3/4 inhibitor
Zardaverine is a phosphodiesterase inhibitor, selective for PDE3 and 4 (IC50 values are 0.5 and 0.8 uM respectively).
A10592 SALE

Milrinone (Primacor)

PDE3 inhibitor
Milrinone(Primacor) is a a potent and selective phosphodiesterase 3 inhibitor with an IC50 of 0.42 μM for the inhibition of FIII PDE
A10480 SALE

Irsogladine

-
Rsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
A10339 SALE

Dyphylline

Adenosine receptor antagonist
Dyphylline is a xanthine derivative with bronchodilator and vasodilator effects. It acts as an adenosine receptor antagonist and phosphodiesterase inhibitor.
A10319

Dipyridamole

PDE inhibitor
Dipyridamole (Persantine) is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.
A12619

Avanafil

PDE5 inhibitor
Avanafil is a PDE5 Inhibitor for the Treatment of Erectile Dysfunction
A12776 SALE

AN2728

PDE4 inhibitor‎
AN2728 is a topically administered, boron-containing, anti-inflammatory compound that inhibits PDE4 activity and thereby suppresses the release of TNFalpha, IL-12, IL-23 and other cytokines
A13121

PF-04447943

PDE9 inhibitor
PF-04447943 is a potent, selective brain penetrant PDE9 inhibitor that increased indicators of hippocampal synaptic plasticity and improved cognitive function in a variety of cognition models in both rats and mice.
A13722 SALE

Deltarasin HCl

PDE-KRAS inhibitor
Deltarasin is a novel small molecule inhibiting the KRAS PDEδ interaction and thus impairing oncogenic KRAS signalling.
A15546

HA130

Autotaxin Inhibitor
N/A
A11527

PF-8380

Autotaxin inhibitor
PF-8380 is a potent and specific autotaxin inhibitor with an IC50 value of 2.8 nM.
A10883

Tadalafil

PDE5 inhibitor
Tadalafil is a PDE5 inhibitor with an IC50 value of 1.8 nM.
A10066 SALE

Aminophylline

Adenosine receptor antagonist
Aminophylline is a nonselective adenosine receptor antagonist and phosphodiesterase inhibitor capable of reversing ischemia-induced bradyasystole.
A11326

Bay 60-7550

PDE-2 Inhibitor
BAY 60-7550 is a potent PDE2 inhibitor with IC50 values of 2.0 nM (bovine) and 4.7 nM (human).
A10804 SALE

Roflumilast

PDE inhibitor
Roflumilast acts as a selective, long-acting inhibitor of the enzyme PDE-4.
A10217

Cilostazol

PDE3 inhibitor
Cilostazol is a selective inhibitor of 3-type phosphodiesterase (PDE3) with therapeutic focus on cAMP.
A10805 SALE

Rolipram

PDE4 inhibitor
Rolipram is a PDE4-inhibitor with IC50 = 2.0 μM.
A10464 SALE

Icariin

PDE5 inhibitor
Icariin is inhibitory to all three PDE5 isoforms that inhibits PDE5A1, A2, and A3 with an IC50 value of 1.0, 0.75, and 1.1 microM, respectively.
A10733

Pimobendan (Vetmedin)

PDE inhibitor
Pimobendan (Vetmedin) is a calcium sensitizer with positive inotropic and vasodilator effects. It is also a selective inhibitor of phosphodiesterase III (PDE3).
A11073

GSK256066

PDE Inhibitor
GSK256066 is an exceptionally high affinity and selective inhibitor of PDE4 that inhibits PDE4 isoforms A-D with equal affinity and has a high HARBS (High-Affinity Rolipram Binding Site) ratio (>17).
A11191 SALE

PF-2545920

PDE10A inhibitor

PF-2545920 is a phosphodiesterase inhibitor selective for the PDE10A subtype.

A11019 SALE

Ibudilast (KC-404)

PDE Inhibitor
Ibudilast, a pharmacologic phosphodiesterase inhibitor, prevents human immunodeficiency Virus-1 Tat-Mediated activation of microglial cells.
A10216

Cilomilast (SB-207499)

PDE-4 inhibitor
Cilomilast is orally active and acts as a selective Phosphodiesterase-4 inhibitor with antiinflammatory effects that target bronchoconstriction, mucus hypersecretion, and airway remodeling associated with COPD.
A10449 SALE

Hesperetin

PDE4 inhibitor
Hesperetin, a selective phosphodiesterase (PDE)4 inhibitor, is present in the traditional Chinese medicine, “Chen Pi.” Hesperetin is a citrus flavonoid that has been reported to lower plasma cholesterol. Hesperetin reduces the transcription of ACAT-2 mRNA in Hep-G2 cells and reduces ApoB protein synthesis in a dose-dependent manner. It also is a potential therapy for carcinoid cancer.
A10541 SALE

Luteolin

PDE4 inhibitor
Luteolin is a PDE4 inhibitor, phosphodiesterase inhibitor, and an interleukin 6 inhibitor, affecting xylazine/ketamine-induced anesthesia in mice. Luteolin acts as a monoamine transporter activator, and is one of the few chemicals demonstrated to possess this property.
A11289 SALE

Apremilast (CC 10004)

PDE4 Inhibitor
Apremilast, a novel PDE4 inhibitor, inhibits spontaneous production of tumour necrosis factor-alpha from human rheumatoid synovial cells and ameliorates experimental arthritis.
A10965 SALE

Vardenafil

PDE-5 Inhibitor
Vardenafil is a PDE5 inhibitor used for treating erectile dysfunction.
A16142

Sildenafil Mesylate

PDE5 inhibitor
Sildenafil Mesylate is a mesylate form of Sildenafil, an inhibitor of Phosphodiesterase 5.

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