Search Result
Results for "
PDE4 inhibitor
" in MedChemExpress (MCE) Product Catalog:
12
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-108623
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CP-80,633
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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Atizoram (CP-80,633), a cyclic nucleotide phosphodiesterase (PDE4) inhibitor, elevates plasma cyclic AMP levels and decreases tumor necrosis factor-α (TNFα) production in mice .
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- HY-155830
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-
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- HY-U00410
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- HY-162797
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Phosphodiesterase (PDE)
TNF Receptor
Interleukin Related
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Inflammation/Immunology
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PDE4-IN-18 (compound 1l) is a PDE4 inhibitor (IC50=1.55 μM) with anti-inflammatory activity. PDE4-IN-18 exerts anti-inflammatory effects by reducing excessive immune cell infiltration and intestinal membrane formation, as well as reducing the mRNA expression of pro-inflammatory cytokines (such as TNF-α and IL-6) in synovial tissue. PDE4-IN-18 can be used in the study of rheumatoid arthritis and psoriasis .
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- HY-155692
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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PDE4-IN-13 is a PDE4 inhibitor with an IC50 of 1.56 μM. PDE4-IN-13 shows anti-inflammatory and antioxidant properties, and can be used for chronic obstructive pulmonary disease (COPD) research .
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- HY-122167
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-
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- HY-69172
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-
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- HY-19393
-
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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SCH 351591 is a potent, selective and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 58 nM. SCH 351591 can inhibit all 4 PDE4 subtypes (A, B, C, and D). SCH 351591 has the potential for the asthma and chronic obstructive pulmonary disease (COPD) research .
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- HY-124388
-
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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PDE4-IN-20 is a selective submicromolar phosphodiesterase-4 (PDE4) inhibitor with anti-TNF-α properties. PDE4-IN-20 exhibits significant biological activity in vitro and in vivo. The mechanism of action of PDE4-IN-20 is supported by molecular modeling studies, which reveal its binding mode with PDE4. PDE4-IN-20 was optimized in further conformational analysis and showed pharmacological characteristics similar to those of known PDE4 inhibitors .
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- HY-W787896
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-
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- HY-146974
-
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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PDE4-IN-9 (Compound 5j) is a potent inhibitor of PDE4. PDE4-IN-9 exhibits lower IC50 value (1.4 μM) against PDE4 than parent rolipram (2.0 μM) in in vitro enzyme assay. PDE4-IN-9 also displays good in vivo activity in animal models of asthma/COPD and sepsis induced by LPS .
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- HY-115871A
-
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mAChR
Phosphodiesterase (PDE)
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Others
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(Rac)-PDE4-IN-4 is the diastereomer mixture of PDE4-IN-4 (HY-115871). PDE4-IN-4 is a dual M3 (pIC50 = 10.2) antagonist-PDE4 (pIC50 = 8.8) inhibitor for the inhaled research of pulmonary diseases .
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- HY-147950
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-
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- HY-169258
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Phosphodiesterase (PDE)
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Metabolic Disease
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PDE4-IN-21 (Compound L19) is a poetent PDE4 inhibitor, with an IC50 of 0.48 μM. PDE4-IN-21 exhibits good inhibitory activity and remarkable metabolic stability in rat liver microsomes .
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- HY-132887
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-
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- HY-162583
-
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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PDE4-IN-17 (compound 4e) is a potent PDE4 inhibitor. PDE4-IN-17 inhibits PDE4B and PDE4D with IC50s of 10.0 and 15.2 nM, respectively. PDE4-IN-17 has good oral bioavailability (F=66%) and longer half-life (t1/2=2.0 h) in SD rats .
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- HY-151174
-
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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PDE4-IN-12 is a potent pan-PDE4 inhibitor, with IC50s of 3.5 and 15 nM for PDE4 and PDE7, respectively (SI=2.71 and 4.27, respectively). PDE4-IN-12 shows well tolerated, can be used in study of inflammatory bowel diseases (IBDs) .
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- HY-150060
-
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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PDE4-IN-11 is an inhibitor of phosphodiesterase isoenzyme 4 (PDE4). PDE4-IN-11 displays highly effective bronchodilatory and anti-inflammatory properties, can be used for obstructive or inflammatory airway diseases research .
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- HY-108617
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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YM976 is a phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.2 nM. YM976 shows the dissociation of anti-inflammatory activities from emetic effects and inhibits the antigen-induced airway responses .
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- HY-172135
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p38 MAPK
Phosphodiesterase (PDE)
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Inflammation/Immunology
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PDE4-IN-26 (Compound A5) is an orally active and highly selective PDE4 inhibitor. PDE4-IN-26 has anti-inflammatory activity and can inhibit the phosphorylation of p38 MAPK. In mouse models of acute lung injury and chronic obstructive pulmonary disease, PDE4-IN-26 can improve pulmonary inflammation, injury and fibrosis, promote sputum secretion and relieve cough in mice. PDE4-IN-26 can be used for the research of lung injury-related diseases .
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- HY-144265
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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PDE4-IN-5 (compound 33a) is a potent and selective PDE4 inhibitor (IC50=3.1 nM). PDE4-IN-5 has favorable skin permeability and a well-characterized binding mechanism. Anti-psoriasis effect .
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- HY-W186242
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-
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- HY-159654
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Phosphodiesterase (PDE)
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Others
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PDE4-IN-19 (compound 1) is a PDE4 inhibitor, with IC50 values of <10 nM and 10-100 nM for PDE4B1 and PDE4D3, respectively .
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- HY-161381
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-
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- HY-10978
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-
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- HY-115913
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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PDE4-IN-6 is a potent, safe and moderately selective PDE4 inhibitor with IC50s of 0.125 and 0.43 µM for PDE4B and PDE4D, respectively. PDE4-IN-6 can downregulate the expression level of TNF-α and IL-6. PDE4-IN-6 has potent immunomodulatory activity thereby its potential against rheumatoid arthritis. Anti-inflammatory and anti-arthritic effects .
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- HY-160864
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HWA 448
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Phosphodiesterase (PDE)
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Cancer
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Torbafylline is a PDE inhibitor. Torbafylline mitigates protein breakdown in rat skeletal muscle following burns by activating the PDE4/cAMP/EPAC/PI3K/Akt signaling pathway. Torbafylline suppresses the increased ubiquitin-proteasome-dependent protein degradation observed in the skeletal muscles of rats susceptible to cancer and sepsis .
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- HY-168212
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- HY-144684
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- HY-155819
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mAChR
Phosphodiesterase (PDE)
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Inflammation/Immunology
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M3/PDE4 modulator-1 (compound 10f) is a bifunctional molecule that is an M3 mAChR antagonist and a PDE4 inhibitor. M3/PDE4 modulator-1 (10-1000 nM/kg; iv) reduces cysteine eosinophil influx in the OVA rat model .
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- HY-115871
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- HY-161772
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- HY-147846
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- HY-169981
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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PDE4-IN-24 (compoud 14h) is a potent inhibitor of PDE4D with the IC50 of 0.57 nM and >4100-fold selectivity over other PDE families. PDE4-IN-24 plays an important role in inflammatory disease .
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- HY-10978S
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AN-2728-d4; PF-06930164-d4
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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Crisaborole-d4 is deuterium labeled Crisaborole. Crisaborole (AN-2728) is a potent inhibitor of PDE4 and cytokine release; inhibit PDE4 with an IC50 of 0.49 μM.
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- HY-106137
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- HY-10978R
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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Crisaborole (Standard) is the analytical standard of Crisaborole. This product is intended for research and analytical applications. Crisaborole (AN-2728) is a potent inhibitor of PDE4 and cytokine release; inhibit PDE4 with an IC50 of 0.49 μM.
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- HY-145583
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- HY-105096
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-
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- HY-130786
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BRL 30892
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Phosphodiesterase (PDE)
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Others
Inflammation/Immunology
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Denbufylline (BRL 30892) is an inhibitor of phosphodiesterase-4 (PDE4). Denbufylline is able to block the degradation of intracellular cAMP (cyclic adenosine phosphate) thereby increasing the level of intracellular cAMP, which helps regulate a variety of cellular functions. Denbufylline can be used in the study of chronic obstructive pulmonary disease (COPD), asthma and other inflammatory diseases .
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- HY-B0327A
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- HY-B0327
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- HY-16900
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-
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- HY-100118
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-
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- HY-115383
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- HY-16900A
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(R)-Rolipram; (-)-Rolipram
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Phosphodiesterase (PDE)
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Neurological Disease
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(R)-(-)-Rolipram is the R-enantiomer of Rolipram. Rolipram is a selective inhibitor of phosphodiesterases PDE4 with IC50 of 3 nM, 130 nM and 240 nM for PDE4A, PDE4B, and PDE4D, respectively.
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- HY-100927
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- HY-163606
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- HY-163605
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- HY-U00254
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- HY-100640
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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Roflumilast Impurity E is the impurity of Roflumilast. Roflumilast(Daliresp) is a agent which acts as a selective and long-acting inhibitor of the enzyme PDE-4 with an IC50 value of 0.8 nM.
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- HY-117977
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Phosphodiesterase (PDE)
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Neurological Disease
Inflammation/Immunology
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FCPR03 is a potent and selective phosphodiesterase 4 (PDE4) inhibitor with IC50 values of 60 nM, 31 nM and 47 nM for PDE4 catalytic domain, PDE4B1 and PDE4D7, respectively. FCPR03 displays at least 2100-fold selectivity over other PDEs (PDE1-3 and PDE5-11). FCPR03 has anti-inflammatory, neuroprotective and antidepressant-like effects .
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- HY-12740
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- HY-121491
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- HY-16900R
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Phosphodiesterase (PDE)
Bacterial
HIV
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Neurological Disease
Cancer
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Rolipram (Standard) is the analytical standard of Rolipram. This product is intended for research and analytical applications. Rolipram is a selective phosphodiesterases PDE4 inhibitor with IC50s of 3 nM, 130 nM and 240 nM for PDE4A, PDE4B, and PDE4D, respectively.
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- HY-162582
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- HY-117960
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LEO-32731
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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Orismilast (LEO-32731) is an orally active and selective PDE4 inhibitor used for the research of inflammatory diseases. Orismilast demonstrates potent inhibition of PDE4B and PDE4D subtype splice variants .
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- HY-100246
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- HY-10469
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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GSK256066 is a selective and high-affinity phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 is developed for the research of chronic obstructive pulmonary disease .
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- HY-12085
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- HY-105092
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- HY-103050
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ML-030
1 Publications Verification
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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ML-030 is a potent PDE4 inhibitor, with IC50 of 6.7 nM, 12.9 nM, 48.2 nM, 37.2 nM, 452 nM and 49.2 nM for PDE4A, PDE4A1, PDE4B1, PDE4B2, PDE4C1,and PDE4D2, respectively.
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- HY-108047
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Phosphodiesterase (PDE)
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Metabolic Disease
Inflammation/Immunology
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MK-0873 is a selective phosphodiesterase-4 (PDE4) inhibitor. MK-0873 increases intracellular levels of cyclic adenosine phosphate (cAMP) by inhibiting the activity of the PDE4 enzyme and subsequently activates protein kinase A (PKA). Activated PKA inhibits the activity of inflammatory cells and leads to direct relaxation of airway smooth muscle. MK-0873 can be used in studies of chronic obstructive pulmonary disease (COPD) .
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- HY-139095
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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Cipamfylline is a PDE4 inhibitor that can cause PDE4A4 to accumulate in specific areas of the cell through interaction with the ubiquitin scaffolding protein p62. Cipamfylline can be used in the research of atopic dermatitis .
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- HY-118408
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- HY-N10317
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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Toddacoumalone is a natural inhibitor of phosphodiesterase 4 (PDE4) with moderate potency and imperfect agent-like properties. Toddacoumalone has the potential for the research of inflammatory diseases such as psoriasis .
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- HY-12887
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- HY-N2958
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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Braylin, a coumarin, is a potent phosphodiesterase-4 (PDE4) inhibitor and is involved in anti-inflammatory and immunomodulation, which may serve as a potential target for the study of immunoinflammatory diseases .
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- HY-131707
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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LEO 39652 is a dual-soft PDE4 inhibitor with IC50s of 1.2 nM, 1.2 nM, 3.0 nM and 3.8 nM for PDE4A, PDE4B, PDE4C and PDE4D, respectively. LEO 39652 also inhibits TNF-α with an IC50 value of 6.0 nM. LEO 39652 is used for topical research of Atopic dermatitis (AD) .
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- HY-12085S
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CC-10004-d5
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Phosphodiesterase (PDE)
TNF Receptor
Apoptosis
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Inflammation/Immunology
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Apremilast-d5 is a deuterium labeled Apremilast. Apremilast is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM[1].
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- HY-11071
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- HY-N0014
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- HY-11072
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- HY-11070
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- HY-12318
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IBMX
Maximum Cited Publications
40 Publications Verification
3-Isobutyl-1-methylxanthine; Isobutylmethylxanthine
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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IBMX is a broad-spectrum phosphodiesterase (PDE) inhibitor, with IC50s of 6.5, 26.3 and 31.7 μM for PDE3, PDE4 and PDE5, respectively.
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- HY-106003
-
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Phosphodiesterase (PDE)
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Neurological Disease
Inflammation/Immunology
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GSK356278 is a potent, selective, orally bioavailable and brain-penetrant inhibitor of phosphodiesterase 4 (PDE4), with pIC50s of 8.6, 8.8, and 8.7 for human PDE4A, PDE4B, and PDE4D, respectively. GSK356278 has anti-inflammatory activity, and exhibits anxiolytic and cognition-enhancing effects .
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- HY-12348
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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LEO 29102 is a potent phosphodiesterase 4 (PDE4) inhibitor with an IC50 value of 5 nM. LEO 29102 inhibits TNFα release. LEO 29102 has the potential for the research of atopic dermatitis .
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- HY-U00179
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- HY-157457
-
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Phosphodiesterase (PDE)
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Metabolic Disease
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Z21090 (ZL40) is a potent inhibitor of PDE4 with the IC50 value of 37.4 nM and oral bioavailability. Z21090 plays an important role in alcohol-related diseases research .
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- HY-19830
-
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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AN3199 is a PDE4 inhibitor with an IC50 of 94.5 nM. AN3199 can be used for the research of inflammation-associated diseases such as asthma and chronic obstructive pulmonary disease (COPD) .
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- HY-106245
-
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Phosphodiesterase (PDE)
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Neurological Disease
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HT-0712 is a Phosphodiesterase Type 4 (PDE4) inhibitor. HT-0712 enhances rehabilitation-dependent motor recovery and cortical reorganization after focal cortical ischemia .
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- HY-100640R
-
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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Roflumilast Impurity E (Standard) is the analytical standard of Roflumilast Impurity E. This product is intended for research and analytical applications. Roflumilast Impurity E is the impurity of Roflumilast. Roflumilast(Daliresp) is a agent which acts as a selective and long-acting inhibitor of the enzyme PDE-4 with an IC50 value of 0.8 nM.
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- HY-12085R
-
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Phosphodiesterase (PDE)
Apoptosis
TNF Receptor
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Inflammation/Immunology
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Apremilast (Standard) is the analytical standard of Apremilast. This product is intended for research and analytical applications. Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM .
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- HY-15178
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GRC 3886
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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Oglemilast (GRC 3886) is a potent and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 0.5 nM for PDE4D3. Oglemilast inhibits pulmonary cell infiltration, including eosinophilia and neutrophilia in vitro and in vivo. Oglemilast has the potential for inflammatory airway diseases .
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- HY-114766
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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Pumafentrine is an orally active, potent dual PDE3/PDE4 inhibitor. Pumafentrine dose-dependently ameliorates the clinical score and colonic TNFα production in murine Dextran sulphate sodium (DSS; HY-116282C)-induced colitis in a preventive setting .
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- HY-10790
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SB-207499
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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Cilomilast (SB-207499) is a potent, selective and orally active inhibitor of Phosphodiesterase 4 (PDE4), with IC50s of ~100 and 120 nM for LPDE4 and HPDE4, respectively. Cilomilast shows selectivity for PDE4 over PDE1, PDE2, PDE3 and PDE5 (IC50=74, 65, >100, and 83 μM, respectively). Cilomilast has anti-inflammatory and immunomodulatory effects and can be used for thr research of asthma and chronic obstructive pulmonary disease (COPD) .
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- HY-162581
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- HY-129785
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- HY-109586
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- HY-12085S1
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-
- HY-12085S3
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- HY-122942
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-
- HY-147263
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CC-11050
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Phosphodiesterase (PDE)
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Infection
Inflammation/Immunology
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Dovramilast (CC-11050) is an orally active phosphodiesterase 4 (PDE4) inhibitor and can reduce the inflammatory response and improves Isoniazid (INH)-mediated bacillary clearance from the lungs. Dovramilast, as an adjunct, is used for the research of tuberculosis (TB) .
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- HY-149661
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- HY-15455
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APTA-2217; BYK 20869; B9302-107
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Phosphodiesterase (PDE)
RSV
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Inflammation/Immunology
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Roflumilast (APTA-2217) is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.
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- HY-12887R
-
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Phosphodiesterase (PDE)
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Inflammation/Immunology
Cancer
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Piclamilast (Standard) is the analytical standard of Piclamilast. This product is intended for research and analytical applications. Piclamilast (RP 73401) is a phosphodiesterase 4 (PDE4) inhibitor, with IC50 values of 16 nM and 2 nM in pig aorta and eosinophil soluble, respectively .
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- HY-B0392
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- HY-106996
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GW 842470
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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AWD 12-281 is an orally active and highly selective phosphodiesterase 4 (PDE4) inhibitor (IC50 = 9.7 nM). AWD 12-281 is used in the study of allergic dermatitis, asthma, chronic obstructive pulmonary disease (COPD), and allergic rhinitis .
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- HY-119799
-
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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UK-500001 is an orally active inhibitor for phosphodiesterase 4 (PDE4), which inhibits PDE4D3 (IC50 is 0.28 nM), PDE4B2 (IC50 is 22.8 nM), PDE4A4 (IC50 is 26.1 nM) and PDE4C2 (IC50 is 271 nM). UK-500001 exhibits anti-inflammatory efficacy and inhibits TNF-α and IFN-γ release in human and rodent macrophagic cell lines in nanomolar levels. UK-500001 ameliorates chronic obstructive pulmonary disease (COPD) and asthma .
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- HY-103024
-
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Phosphodiesterase (PDE)
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Neurological Disease
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ICI-63197 is a phosphodiesterase 3 (PDE3) and PDE4 inhibitor with Ki values of 9 µM and 10 µM, respectively. ICI-63197 is selectivity against PDE1 and PDE2. ICI-63197 has antidepressant effects .
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- HY-N0014R
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- HY-12318R
-
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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IBMX (Standard) is the analytical standard of IBMX. This product is intended for research and analytical applications. IBMX is a broad-spectrum phosphodiesterase (PDE) inhibitor, with IC50s of 6.5, 26.3 and 31.7 μM for PDE3, PDE4 and PDE5, respectively.
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- HY-15455S2
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APTA-2217-d3; BYK 20869-d3; B9302-107-d3
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Isotope-Labeled Compounds
Phosphodiesterase (PDE)
RSV
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Inflammation/Immunology
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Roflumilast-d3 is deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.
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- HY-108974
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Phosphodiesterase (PDE)
Calcium Channel
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Neurological Disease
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Drotaverine hydrochloride is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calcium channel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine (hydrochloride) exhibits in vivo antispasmodic efficacy without anticholinergic effects.
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- HY-U00186
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- HY-109085
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OPA-15406
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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Difamilast (OPA-15406) is a topical, selective and nonsteroidal phosphodiesterase-4 (PDE4) inhibitor with particularly efficient inhibition of subtype B (IC50=11.2 nM). Difamilast can be used for the research of mild to moderate atopic dermatitis (AD) .
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- HY-19672
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BAY 19-8004
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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Lirimilast (BAY 19-8004) is a potent, selective and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 value of 49 nM. Lirimilast can be used for the treatment of asthma or chronic obstructive pulmonary disease (COPD). Lirimilast has potently anti-inflammatory properties .
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- HY-144683
-
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Phosphodiesterase (PDE)
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Inflammation/Immunology
|
PF-07038124 is a PDE4 inhibitor with an IC50 of 0.5 nM for PDE4B2. PF-07038124 shows inhibitory activities against IL-13, IL4, and IFNγ (IC50=125, 4.1, 1.06 nM, respectively). PF-07038124 can be used for research of atopic dermatitis and plaque psoriasis .
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- HY-144683A
-
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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PF-07038124 hydrochloride is a PDE4 inhibitor with an IC50 of 0.5 nM for PDE4B2. PF-07038124 hydrochloride shows inhibitory activities against IL-13, IL4, and IFNγ (IC50=125, 4.1, 1.06 nM, respectively). PF-07038124 hydrochloride can be used for research of atopic dermatitis and plaque psoriasis .
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- HY-15455S
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APTA-2217-d4; BYK 20869-d4; B9302-107-d4
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Isotope-Labeled Compounds
Phosphodiesterase (PDE)
RSV
|
Inflammation/Immunology
|
Roflumilast-d4 is the deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells[1][2].
|
-
- HY-161936
-
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Z21115 is an orally active inhibitor for phosphodiesterase 4 (PDE4), that inhibits PDE4D7 with IC50 of 10.5 nM. Z21115 inhibits Lipopolysaccharide (HY-D1056)-induced expression of IL-6, TNF-α and iNOS. Z21115 exhibits anti-inflammatory activity in DSS (HY-116282)-induced mouse colitis models without significant toxicity (1 g/kg) .
|
-
- HY-15455R
-
|
Phosphodiesterase (PDE)
RSV
|
Inflammation/Immunology
|
Roflumilast (Standard) is the analytical standard of Roflumilast. This product is intended for research and analytical applications. Roflumilast (APTA-2217) is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.
|
-
- HY-15455S1
-
|
Phosphodiesterase (PDE)
RSV
|
Inflammation/Immunology
|
Roflumilast-d4 N-Oxide is the deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells[1][2].
|
-
- HY-119708
-
RPL-554
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Ensifentrine (RPL-554) is an inhaled first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC50s of 0.4 nM and 1479 nM, respectively. Ensifentrine has bronchoprotective and anti-inflammatory activities. Ensifentrine can be used for chronic obstructive pulmonary disease (COPD) research .
|
-
- HY-B1639
-
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
Inflammation/Immunology
|
Enoximone is an inotropic vasodilating agent and a selective and orally active phosphodiesterase III (PDE3) inhibitor with an IC50 of 5.9 μM. Enoximone induces vasodilatation and increases intracellular levels of cAMP by inhibiting cGMP-inhibited PDE. Enoximone also exhibits PDE4 inhibitory effect with an IC50 of 21.1 μM for myocardial PDE4A. Enoximone has the potential for congestive heart failure research and has bronchodilatory, antiasthma and anti-inflammatory effects .
|
-
- HY-14254
-
Loprinone Hydrochloride
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
Olprinone (Loprinone) Hydrochloride is a potent phosphodiesterase (PDE) 3 inhibitor, with IC50s of 150, 100, 0.35 and 14 μM for PDE1, PDE2, PDE3 and PDE4, respectively. Olprinone Hydrochloride is used for the research of heart failure due to its positive inotropic and vasodilative effects. Anti-inflammatory activity .
|
-
- HY-14254A
-
Loprinone
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
Olprinone (Loprinone) is a potent phosphodiesterase (PDE) 3 inhibitor, with IC50s of 150, 100, 0.35 and 14 μM for PDE1, PDE2, PDE3 and PDE4, respectively. Olprinone is used for the research of heart failure due to its positive inotropic and vasodilative effects. Anti-inflammatory activity .
|
-
- HY-108974S
-
|
Isotope-Labeled Compounds
Phosphodiesterase (PDE)
Calcium Channel
|
Neurological Disease
|
Drotaverine-d10 (hydrochloride) is the deuterium labeled Drotaverine hydrochloride. Drotaverine hydrochloride is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calcium channel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine hydrochloride exhibits in vivo antispasmodic efficacy without anticholinergic effects[1][2].
|
-
- HY-109085R
-
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Difamilast (Standard) is the analytical standard of Difamilast. This product is intended for research and analytical applications. Difamilast (OPA-15406) is a topical, selective and nonsteroidal phosphodiesterase-4 (PDE4) inhibitor with particularly efficient inhibition of subtype B (IC50=11.2 nM). Difamilast can be used for the research of mild to moderate atopic dermatitis (AD) .
|
-
- HY-A0027
-
|
Histamine Receptor
Phosphodiesterase (PDE)
|
Inflammation/Immunology
Endocrinology
|
Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases .
|
-
- HY-A0027A
-
|
Histamine Receptor
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases .
|
-
- HY-16558
-
Butein
4 Publications Verification
2’,3,4,4’-tetrahydroxy Chalcone
|
EGFR
Autophagy
Apoptosis
Phosphodiesterase (PDE)
|
Cancer
|
Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4 . Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60 c-src in HepG2 cells . Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a . Butein is a SIRT1 activator (STAC).
|
-
- HY-N11431
-
|
Others
|
Cancer
|
ent-Toddalolactone is a natural compound with anti-inflammatory and anticancer activities. Ent-Toddalolactone has shown inhibitory effects on phosphodiesterase-4 (PDE4) in vitro and is a potential drug target for inhibiting asthma and chronic obstructive pulmonary disease. The activity of ent-Toddalolactone is related to its unique chemical structure, and some of its derivatives showed IC50 values below 10 μM in inhibition experiments, showing high biological activity .
|
-
- HY-B0442C
-
|
Endogenous Metabolite
Phosphodiesterase (PDE)
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
Cancer
|
Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM respectively, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes - .
|
-
- HY-B0442
-
|
Phosphodiesterase (PDE)
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
Cancer
|
Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-B0442A
-
|
Phosphodiesterase (PDE)
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
Cancer
|
Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-B0442S
-
|
Phosphodiesterase (PDE)
Endogenous Metabolite
|
Endocrinology
|
Vardenafil-d5 is deuterium labeled Vardenafil. Vardenafil is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows selectivity over PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction[1][2].
|
-
- HY-101762
-
|
JAK
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
TyK2-IN-2 (Compoud 18) is a potent and selective TYK2 inhibitor with IC50s of 7 nM, 0.1 μM and 0.05 μM for TYK2 JH2, IL-23 and IFNα, respectively. TyK2-IN-2 also inhibits phosphodiesterase 4 (PDE4) with an IC50 of 62 nM. TyK2-IN-2 can be used for the research of inflammatory and autoimmune diseases .
|
-
- HY-100936
-
SQ 20009; EHT 0202 hydrochloride
|
Phosphodiesterase (PDE)
GABA Receptor
|
Neurological Disease
Inflammation/Immunology
|
Etazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC50 of 2 μM. Etazolate hydrochloride is a γ-aminobutyric acid A (GABAA) receptor regulator. Etazolate hydrochloride is an α-secretase activator and induced the production of soluble amyloid precursor protein (sAPPα). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects .
|
-
- HY-A0027AS
-
|
Isotope-Labeled Compounds
Histamine Receptor
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Fenspiride-d5 is the deuterium labeled Fenspiride. Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases[1][2][3].
|
-
- HY-B0442B
-
|
Endogenous Metabolite
Phosphodiesterase (PDE)
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-105349
-
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
T-0156 is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. T-0156 specifically inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) by PDE5 in a competitive manner (IC50=0.23 nM). T-0156 inhibits PDE6 (IC50=56 nM) and has low potencies against PDE1, PDE2, PDE3, and PDE4 (IC50>10 μM). T-0156 enhances the nitric oxide (NO)/cGMP pathway .
|
-
- HY-170435
-
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
PDE5-IN-13 (Compound 14b) inhibits phosphodiesterase 5 (PDE5A) with an IC50 of 3 nM. PDE5-IN-13 is a potential candidate for PAH (pulmonary arterial hypertension) research. PDE5-IN-13 has high selectivity for targets over PDE1, PDE2, PDE3, PDE4, PDE7, PDE8, PDE9, PDE10, and PDE11. PDE5-IN-13 is orally active .
|
-
- HY-16558R
-
|
EGFR
Autophagy
Apoptosis
Phosphodiesterase (PDE)
|
Cancer
|
Butein (Standard) is the analytical standard of Butein. This product is intended for research and analytical applications. Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4 . Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60c-src in HepG2 cells . Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a . Butein is a SIRT1 activator (STAC).
|
-
- HY-124582
-
NEO214
1 Publications Verification
|
Autophagy
mTOR
|
Cancer
|
NEO214 is an autophagy inhibitor and a covalent conjugate of the PDE4 inhibitor Rolipram (HY-16900) and perillyl alcohol (HY-N7000). It has anti-cancer activity and blood-brain barrier (BBB) permeability. Over sex. NEO214 prevents autophagy-lysosome fusion, thereby blocking autophagic flux and triggering glioma cell death. The process involves mTOR activation, andTFEB(Transcription Factor EB) aggregation. NEO214 inhibitionMacroautophagy/autophagy in glioblastoma cells has the potential to overcome chemotherapy resistance in glioblastoma .
|
-
- HY-18252
-
TA1790
|
Phosphodiesterase (PDE)
NO Synthase
Endogenous Metabolite
|
Cardiovascular Disease
Endocrinology
|
Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis .
|
-
- HY-18252R
-
|
Phosphodiesterase (PDE)
NO Synthase
Endogenous Metabolite
|
Cardiovascular Disease
Endocrinology
|
Avanafil (Standard) is the analytical standard of Avanafil. This product is intended for research and analytical applications. Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis .
|
-
- HY-18252A
-
TA1790 dibenzenesulfonate
|
Phosphodiesterase (PDE)
NO Synthase
Endogenous Metabolite
|
Cardiovascular Disease
Endocrinology
|
Avanafil (TA-1790) dibenzenesulfonate is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil dibenzenesulfonate activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil dibenzenesulfonate inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil dibenzenesulfonate can be used for the research of erectile dysfunction and osteoporosis .
|
-
- HY-113972R
-
|
Others
|
Inflammation/Immunology
|
Avanafil (Standard) is the analytical standard of Avanafil. This product is intended for research and analytical applications. Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis .
|
-
- HY-B0442CR
-
|
Endogenous Metabolite
Phosphodiesterase (PDE)
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
Cancer
|
Vardenafil (dihydrochloride) (Standard) is the analytical standard of Vardenafil (dihydrochloride). This product is intended for research and analytical applications. Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM respectively, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes - .
|
-
- HY-B0442R
-
|
Phosphodiesterase (PDE)
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
Vardenafil (Standard) is the analytical standard of Vardenafil. This product is intended for research and analytical applications. Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-W049735R
-
|
Drug Metabolite
Endogenous Metabolite
|
Metabolic Disease
|
Vardenafil (dihydrochloride) (Standard) is the analytical standard of Vardenafil (dihydrochloride). This product is intended for research and analytical applications. Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM respectively, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes - .
|
-
- HY-B0442AS
-
|
Endogenous Metabolite
Phosphodiesterase (PDE)
Isotope-Labeled Compounds
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
Vardenafil-d5 hydrochloride is deuterated labeled Vardenafil hydrochloride (HY-B0442A). Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-164685
-
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
T-0156 free base is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. T-0156 free base specifically inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) by PDE5 in a competitive manner (IC50=0.23 nM). T-0156 free base inhibits PDE6 (IC50=56 nM) and has low potencies against PDE1, PDE2, PDE3, and PDE4 (IC50>10 μM). T-0156 free base enhances the nitric oxide (NO)/cGMP pathway .
|
-
- HY-N3945R
-
|
Phosphodiesterase (PDE)
Calcium Channel
Adrenergic Receptor
Dopamine Receptor
Influenza Virus
|
Infection
Inflammation/Immunology
|
Glaucine (Standard) is the analytical standard of Glaucine. This product is intended for research and analytical applications. Glaucine (O,O-Dimethylisoboldine) is an alkaloid isolated from Glaucium flavum with antitussive, bronchodilation and anti-inflammatory properties. Glaucine is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor with Kis of 3.4 μM in human bronchus and polymorphonuclear leukocytes. Glaucine is also a non-selective α-adrenoceptor antagonist, a Ca2+ entry blocker, and a weak dopamine D1 and D2 receptor antagonist. Glaucine has antioxidative and antiviral activities .
|
-
- HY-B0442BR
-
|
Endogenous Metabolite
Phosphodiesterase (PDE)
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
Vardenafil (hydrochloride trihydrate) (Standard) is the analytical standard of Vardenafil (hydrochloride trihydrate). This product is intended for research and analytical applications. Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes - .
|
-
- HY-18252S1
-
|
Endogenous Metabolite
NO Synthase
Phosphodiesterase (PDE)
Isotope-Labeled Compounds
|
Cardiovascular Disease
Endocrinology
|
Avanafil- 13C5, 15N,d2 is 15N and deuterated labeled Avanafil (HY-18252). Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis .
|
-
- HY-N3945
-
O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396
|
Phosphodiesterase (PDE)
Calcium Channel
MMP
NF-κB
|
Inflammation/Immunology
Cancer
|
Glaucine (O,O-Dimethylisoboldine) is an alkaloid extracted from Glaucium flavum that possesses various activities, including cough relief, bronchodilation, anti-inflammatory effects, analgesia, antipyretic properties, and anticancer effects. Glaucine acts as a selective and orally active inhibitor of phosphodiesterase 4 (PDE4), with a Ki of 3.4 µM in human bronchial tissues and polymorphonuclear leukocytes. Glaucine induces relaxation of human isolated bronchi by antagonizing calcium channels. Additionally, Glaucine inhibits the activation of NF-κB, leading to a reduction in the expression of the MMP-9 gene, thereby suppressing the migration and invasion of breast cancer cells. Therefore, Glaucine holds potential for research in asthma and breast cancer .
|
-
- HY-115687
-
-
- HY-168558
-
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
PDE4B/D-IN-4 (compound 4p) is a potent inhibitor of PDE-4B and PDE-4D, with IC50s of 5.50 nM and 6.81 nM, respectively. PDE4B/D-IN-4 shows an increase in the level of intracellular cAMP .
|
-
- HY-147830
-
-
- HY-163604
-
-
- HY-117571
-
-
- HY-15444
-
-
- HY-170397
-
-
- HY-W700638A
-
-
- HY-N3180
-
-
- HY-108622
-
-
- HY-161851
-
-
- HY-126167
-
|
Fungal
Phosphodiesterase (PDE)
|
Infection
|
Deacetylsclerotiorin is a secondary metabolite of chloramphenicol isolated from the fungus Bartalinia robillardoides strain LF550. Deacetylsclerotiorin has significant inhibitory effects on Candida albicans (IC50=24 μM), Trichophyton rubrum (IC50=2.83 μM) and Septoria tritici (IC50=7..45 μM). In addition, Deacetylsclerotiorin also exhibits inhibitory effects on the enzyme phosphodiesterase 4 (PDE4) (IC50=2.8 μM) .
|
-
- HY-163777
-
|
Phosphodiesterase (PDE)
|
Others
Inflammation/Immunology
|
Talaroterphenyl A (compound 1) is a p-terphenyl derivative present in the mangrove sediment-derived fungus Talaromyces sp. SCSIO 41412, which exhibits phosphodiesterase 4 (PDE4) inhibitory activity (IC50=1.2 μM). Talaroterphenyl A also exhibits anti-inflammatory and anti-fibrotic activities, significantly reducing the mRNA levels of pro-inflammatory cytokines IL-6, TNF-α, and IL-1β .
|
-
- HY-70069
-
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
GSK256066 Trifluoroacetate is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 Trifluoroacetate is developed for the research of chronic obstructive pulmonary disease .
|
-
- HY-121162
-
(+)-Mesembrine
|
5-HT Receptor
Phosphodiesterase (PDE)
|
Neurological Disease
|
Mesembrine ((+)-Mesembrine) a main alkaloid that features an aryloctahydroindole skeleton. Mesembrine is a 5-HT transporter inhibitor with a Ki of 1.4 nM. Mesembrine also inhibits phosphodiesterase 4B (PDE4B) with an IC50 of 7.8 μM .
|
-
- HY-134937
-
-
- HY-154957
-
|
mTOR
|
Neurological Disease
|
mTOR inhibitor-11 (Compound 9) is a brain-penetrant mTOR inhibitor (IC50: 21 nM for pS6). mTOR inhibitor-11 also inhibits pCHK1 and PDE4D with IC50s of 17.2 and 17.0 μM. mTOR inhibitor-11 can be used for research of CNS disease .
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- HY-153192
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BI 1015550
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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Nerandomilast (BI 1015550) is an orally active inhibitor of PDE4B with an IC50 value of 7.2 nM. Nerandomilast has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD) .
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- HY-130262
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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PDE1-IN-3, compound 4 (WO2019156861), is a selective human phosphodiesterase 1 (PDE1) inhibitor. PDE1-IN-3 inhibits PDE4D and PDE6AB with IC50 values of 23.99 μM and 10 μM, respectively .
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- HY-153192A
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BI 1015550 dihydrate
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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Nerandomilast (BI 1015550) dihydrate is an orally active inhibitor of PDE4B with an IC50 value of 7.2 nM. Nerandomilast (dihydrate) has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD) .
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- HY-112704
-
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Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
PDE5-IN-2 is a potent, highly selective, and orally active PDE5 inhibitor, with an IC50 of 0.31 nM, less potently inhibits PDE2A, PDE10A, PDE4D2, and PDE6C, with IC50s of 106, 46, 43, 1.2 nM, respectively. Anti-pulmonary arterial hypertension activity .
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- HY-172365
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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P7-2302 inhibits PDE7 and PDE4B with IC50 of 0.18 nM and 77.3 nM. P7-2302 inhibits the efflux of P-gp and BCRP (breast cancer resistance protein), exhibits low uptake in rats brain. P7-2302 can be used as a PET tracer when labeled with 18F .
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- HY-167891
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Phosphodiesterase (PDE)
Apoptosis
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Inflammation/Immunology
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GPD-1116 is an orally active Phosphodiesterase (PDE) 4 and PDE1 inhibitor. GPD-1116 can reduce smoke-induced apoptosis of lung cells. GPD-1116 is effective in several disease models in animals, including emphysema, acute lung injury, chronic obstructive pulmonary disease (COPD), asthma and pulmonary hypertension .
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- HY-108621
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Phosphodiesterase (PDE)
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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RS-25344 hydrochloride is a selective cAMP-phosphodiesterase 4 (PDE 4; PDE IV) inhibitor with an IC50 of 0.28 nM in human lymphocytes. RS-25344 hydrochloride has only weak inhibitory effects on PDE I, II, III (IC50 of >100 μM, 160 μM, 330 μM, respectively). RS-25344 hydrochloride has anti-inflammatory, memory- and cognition enhancing, and antineoplastic effects .
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- HY-112831
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BI-409306
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Phosphodiesterase (PDE)
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Neurological Disease
|
Osoresnontrine (BI-409306) is a potent and selective PDE9A inhibitor, with an IC50 of 52 nM, and shows weak activity against other PDEs, such as PDE1A (IC50, 1.4 µM), PDE1C (IC50, 1.0 µM), PDE2A, PDE3A, PDE4B, PDE5A, PDE6AB, PDE7A, and PDE10A (IC50 all > 10 μM); Osoresnontrine can be used in the research of memory enhancement in CNS disorders.
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-N0014
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-
-
- HY-122942
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-
-
- HY-A0027
-
-
-
- HY-16558
-
-
-
- HY-B0442
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-
-
- HY-N10317
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-
-
- HY-N2958
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-
-
- HY-N0014R
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-
-
- HY-N11431
-
|
Toddalia asiatica (L.) Lam.
Structural Classification
Source classification
Rutaceae
Coumarins
Phenylpropanoids
Plants
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Others
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ent-Toddalolactone is a natural compound with anti-inflammatory and anticancer activities. Ent-Toddalolactone has shown inhibitory effects on phosphodiesterase-4 (PDE4) in vitro and is a potential drug target for inhibiting asthma and chronic obstructive pulmonary disease. The activity of ent-Toddalolactone is related to its unique chemical structure, and some of its derivatives showed IC50 values below 10 μM in inhibition experiments, showing high biological activity .
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-
- HY-B0442C
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-
-
- HY-B0442A
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-
-
- HY-B0442B
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-
-
- HY-16558R
-
-
-
- HY-18252
-
TA1790
|
Cardiovascular Disease
Structural Classification
Natural Products
Classification of Application Fields
Source classification
Endogenous metabolite
Disease Research Fields
Endocrinology
|
Phosphodiesterase (PDE)
NO Synthase
Endogenous Metabolite
|
Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis .
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-
- HY-18252R
-
|
Structural Classification
Natural Products
Source classification
Endogenous metabolite
|
Phosphodiesterase (PDE)
NO Synthase
Endogenous Metabolite
|
Avanafil (Standard) is the analytical standard of Avanafil. This product is intended for research and analytical applications. Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis .
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-
-
- HY-18252A
-
TA1790 dibenzenesulfonate
|
Cardiovascular Disease
Structural Classification
Natural Products
Classification of Application Fields
Source classification
Endogenous metabolite
Disease Research Fields
Endocrinology
|
Phosphodiesterase (PDE)
NO Synthase
Endogenous Metabolite
|
Avanafil (TA-1790) dibenzenesulfonate is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil dibenzenesulfonate activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil dibenzenesulfonate inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil dibenzenesulfonate can be used for the research of erectile dysfunction and osteoporosis .
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-
- HY-113972R
-
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Structural Classification
Monophenols
Microorganisms
Marine natural products
Phenols
Marine microorganism
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Others
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Avanafil (Standard) is the analytical standard of Avanafil. This product is intended for research and analytical applications. Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis .
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-
- HY-B0442CR
-
|
Structural Classification
Natural Products
Source classification
Endogenous metabolite
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Endogenous Metabolite
Phosphodiesterase (PDE)
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Vardenafil (dihydrochloride) (Standard) is the analytical standard of Vardenafil (dihydrochloride). This product is intended for research and analytical applications. Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM respectively, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes - .
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-
- HY-B0442R
-
|
Structural Classification
Natural Products
Source classification
Endogenous metabolite
|
Phosphodiesterase (PDE)
Endogenous Metabolite
|
Vardenafil (Standard) is the analytical standard of Vardenafil. This product is intended for research and analytical applications. Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
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-
-
- HY-W049735R
-
|
Structural Classification
Monophenols
Source classification
Phenols
Endogenous metabolite
|
Drug Metabolite
Endogenous Metabolite
|
Vardenafil (dihydrochloride) (Standard) is the analytical standard of Vardenafil (dihydrochloride). This product is intended for research and analytical applications. Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM respectively, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes - .
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-
-
- HY-N3945R
-
-
-
- HY-B0442BR
-
|
Structural Classification
Natural Products
Source classification
Endogenous metabolite
|
Endogenous Metabolite
Phosphodiesterase (PDE)
|
Vardenafil (hydrochloride trihydrate) (Standard) is the analytical standard of Vardenafil (hydrochloride trihydrate). This product is intended for research and analytical applications. Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes - .
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-
-
- HY-N3945
-
O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396
|
Infection
Alkaloids
Structural Classification
other families
Classification of Application Fields
Source classification
Plants
Isoquinoline Alkaloids
Glaucium flavum
Inflammation/Immunology
Disease Research Fields
Papaveraceae
|
Phosphodiesterase (PDE)
Calcium Channel
MMP
NF-κB
|
Glaucine (O,O-Dimethylisoboldine) is an alkaloid extracted from Glaucium flavum that possesses various activities, including cough relief, bronchodilation, anti-inflammatory effects, analgesia, antipyretic properties, and anticancer effects. Glaucine acts as a selective and orally active inhibitor of phosphodiesterase 4 (PDE4), with a Ki of 3.4 µM in human bronchial tissues and polymorphonuclear leukocytes. Glaucine induces relaxation of human isolated bronchi by antagonizing calcium channels. Additionally, Glaucine inhibits the activation of NF-κB, leading to a reduction in the expression of the MMP-9 gene, thereby suppressing the migration and invasion of breast cancer cells. Therefore, Glaucine holds potential for research in asthma and breast cancer .
|
-
-
- HY-N3180
-
-
-
- HY-163777
-
-
-
- HY-121162
-
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-10978S
-
|
Crisaborole-d4 is deuterium labeled Crisaborole. Crisaborole (AN-2728) is a potent inhibitor of PDE4 and cytokine release; inhibit PDE4 with an IC50 of 0.49 μM.
|
-
-
- HY-12085S
-
|
Apremilast-d5 is a deuterium labeled Apremilast. Apremilast is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM[1].
|
-
-
- HY-15455S1
-
|
Roflumilast-d4 N-Oxide is the deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells[1][2].
|
-
-
- HY-12085S1
-
|
Apremilast-d8 (CC-10004-d8) is deuterium labeled Apremilast. Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM .
|
-
-
- HY-12085S3
-
|
Apremilast-d3 (CC-10004-d3) is deuterium labeled Apremilast. Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM .
|
-
-
- HY-15455S2
-
|
Roflumilast-d3 is deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.
|
-
-
- HY-15455S
-
|
Roflumilast-d4 is the deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells[1][2].
|
-
-
- HY-108974S
-
|
Drotaverine-d10 (hydrochloride) is the deuterium labeled Drotaverine hydrochloride. Drotaverine hydrochloride is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calcium channel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine hydrochloride exhibits in vivo antispasmodic efficacy without anticholinergic effects[1][2].
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-
-
- HY-B0442S
-
|
Vardenafil-d5 is deuterium labeled Vardenafil. Vardenafil is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows selectivity over PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction[1][2].
|
-
-
- HY-A0027AS
-
|
Fenspiride-d5 is the deuterium labeled Fenspiride. Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases[1][2][3].
|
-
-
- HY-B0442AS
-
|
Vardenafil-d5 hydrochloride is deuterated labeled Vardenafil hydrochloride (HY-B0442A). Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
-
- HY-18252S1
-
|
Avanafil- 13C5, 15N,d2 is 15N and deuterated labeled Avanafil (HY-18252). Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis .
|
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