Phosphodiesterases (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
A10066 SALE

Aminophylline

-
Aminophylline is a nonselective adenosine receptor antagonist and phosphodiesterase inhibitor capable of reversing ischemia-induced bradyasystole.
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
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.
A12619

Avanafil

PDE5 inhibitor
Avanafil is a PDE5 Inhibitor for the Treatment of Erectile Dysfunction
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).
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.
A13596

Cilostamide

PDE3 inhibitor
Cilostamide is a selective inhibitor of phosphodiesterase (PDE)3A and PDE3B with IC50 values of 27 and 50 nM, respectively.
A10217

Cilostazol

PDE3 inhibitor
Cilostazol is a selective inhibitor of 3-type phosphodiesterase (PDE3) with therapeutic focus on cAMP.
A13722 SALE

Deltarasin HCl

PDE-KRAS inhibitor
Deltarasin is a novel small molecule inhibiting the KRAS PDEδ interaction and thus impairing oncogenic KRAS signalling.
A10319

Dipyridamole

-
Dipyridamole (Persantine) is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.
A10339 SALE

Dyphylline

-
Dyphylline is a xanthine derivative with bronchodilator and vasodilator effects. It acts as an adenosine receptor antagonist and phosphodiesterase inhibitor.
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).
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.
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.
A11019 SALE

Ibudilast (KC-404)

PDE Inhibitor
Ibudilast, a pharmacologic phosphodiesterase inhibitor, prevents human immunodeficiency Virus-1 Tat-Mediated activation of microglial cells.
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.
A10480 SALE

Irsogladine

-
Rsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
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.
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
A13467

MK-0359

PDE4 inhibitor
MK-0359 is a selective and potent oral PDE4 inhibitor, in chronic asthma.
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.
A15197

Oglemilast

PDE4 inhibitor
Oglemilast is a potent inhibitor of PDE4.
A15198

Olprinone Hydrochloride

PDE3 inhibitor
Olprinone is a selective phosphodiesterase 3 (PDE3) inhibitor.
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.
A11191 SALE

PF-2545920

PDE10A inhibitor

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

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