|S2131||Roflumilast||<1 mg/mL||81 mg/mL||15 mg/mL|
|S1431||Sildenafil Citrate||<1 mg/mL||20 mg/mL||<1 mg/mL|
|S1455||Cilomilast||<1 mg/mL||69 mg/mL||50 mg/mL|
|S1512||Tadalafil||<1 mg/mL||78 mg/mL||<1 mg/mL|
|S2515||Vardenafil HCl Trihydrate||10 mg/mL||100 mg/mL||20 mg/mL|
|S8459||TAK-063||<1 mg/mL||85 mg/mL||<1 mg/mL|
|S1550||Pimobendan||<1 mg/mL||67 mg/mL||5 mg/mL|
|S2620||GSK256066||<1 mg/mL||5 mg/mL||<1 mg/mL|
|S2687||PF-2545920||<1 mg/mL||78 mg/mL||78 mg/mL|
|S1430||Rolipram||<1 mg/mL||55 mg/mL||55 mg/mL|
|S8034||Apremilast (CC-10004)||<1 mg/mL||92 mg/mL||<1 mg/mL|
|S1294||Cilostazol||<1 mg/mL||74 mg/mL||6 mg/mL|
|S2484||Milrinone||<1 mg/mL||42 mg/mL||<1 mg/mL|
|S4019||Avanafil||<1 mg/mL||97 mg/mL||<1 mg/mL|
|S2127||S- (+)-Rolipram||<1 mg/mL||55 mg/mL||55 mg/mL|
|S1673||Aminophylline||84 mg/mL||53 mg/mL||<1 mg/mL|
|S3172||Anagrelide HCl||<1 mg/mL||14 mg/mL||<1 mg/mL|
|S1929||Irsogladine||<1 mg/mL||2 mg/mL||<1 mg/mL|
|S1504||Dyphylline||51 mg/mL||51 mg/mL||<1 mg/mL|
|S1895||Dipyridamole||<1 mg/mL||101 mg/mL||50 mg/mL|
|S4164||Doxofylline||24 mg/mL||53 mg/mL||2 mg/mL|
|S4090||Fenspiride HCl||59 mg/mL||9 mg/mL||<1 mg/mL|
|S7224||Deltarasin||<1 mg/mL||100 mg/mL||100 mg/mL|
|S2291||Diosgenin||<1 mg/mL||<1 mg/mL||83 mg/mL|
|S2312||Icariin||<1 mg/mL||50 mg/mL||<1 mg/mL|
|S4683||Sildenafil Mesylate||100 mg/mL||100 mg/mL||4 mg/mL|
|S4684||Sildenafil||14 mg/mL||<1 mg/mL||<1 mg/mL|
|S2320||Luteolin||<1 mg/mL||57 mg/mL||3 mg/mL|
|S8218||PF-8380||<1 mg/mL||95 mg/mL||<1 mg/mL|
|S2368||Theobromine||<1 mg/mL||<1 mg/mL||<1 mg/mL|
Roflumilast is a selective, long-acting the enzyme PDE-4 inhibitor with an IC50 of 0.8 nM.
Mean plasma concentration versus time after single dose oral administration of IC87114 and RFM in wistar rats( n = 6).
Sildenafil citrate is an agent used to treat erectile dysfunction and pulmonary arterial hypertension (PAH).
ADOR lung cancer cells (a July 2015 PDX model) were transfected with an empty vector plasmid or plasmids to express GRP78 and HSP27 together. Twenty-four hours after transfection cells were treated with vehicle control or with OSU-03012 (2.0mM) sildenafil (2mM) for 6 h after which cells were fixed in place and permeabilized using 0.5% Triton X100. Immuno-fluorescence was performed to detect the expression levels of Calnexin; glucosidase I; and glucosidase IIa at 10 magnification using a Hermes WiScan system.
Cilomilast は強力なLPDE4とHPDE4阻害剤で、IC50 がそれぞれ 100 nM と120 nMになる。
LNCaP-C4 prostate cancer cells were suspended in matrigel and transplanted under the kidney capsule of male nude mice hosts. Mice were treated with vehicle-only (10% EtOH, 90% olive oil) control, cilomilast or NVP-ABE171 by gavage (n=7-11 for each respective group)The xenografts LNCaP-C4 xenografts were excised, fixed in formalin, and embedded in paraffin blocks. IHC with Ki67 (proliferation), TUNEL (apoptosis), or p21 (senescence) was performed. Representative Ki67 and TUNEL photomicrographs for cilomilast and NVP-ABE171 treatment group are shown.
Tadalafil is a PDE inhibitor.
(a): E. coli bacteria transformed to be resistant to ampicillin and kayamycin (AMPr KAYAr) were grown in AMPt KAYAt media and cells treated with OSU-03012 (2 μM); sildenafil (2 μM); tadalafil (2 μM), or in combination as indicated. Bacterial cell numbers were determined by assessing the protein concentration of the bacterial cell pellet 3 h, 6h and 12 h after drug exposure * P<0.05 less than corresponding vehicle value. The total protein content of each treatment condition was determined 3 h after addition of antibiotic. Portions of bacteria from each treatment condition were isolated and SDS PAGE and immuno-blotting performed to determine the expression of Dna J, Dna K, RecA and GrpE. (b): E. coli bacteria Gram stained and examined under a X100 oil immersion magnification.
Vardenafil HCl Trihydrate is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.
(G) Immunoblot analysis for TAZ and Nanog in PCSC after vardenafil treatments. (H) Cytotoxicity to DDP in PCSC treated with indicated concentrations of vardenafil. **p < 0.01, *p < 0.05 versus PC3 cells, vardenafil at 0 μM, or DDP at 0 μM; ++p < 0.01, +p < 0.05 versus vardenafil at 0 μM.
PF-2545920は、有力で選択的なPDE10A＜/b> 阻害剤で、IC50 が 0.37 nMです。
Rolipram is a PDE4 inhibitor and an anti-inflammatory agent.
D, average percentage difference of cell growth by PDE4D inhibitors between STK11 mutant and wild-type cell lines. The sensitivity on STK11mt cell lines represents the difference of average percentage growth between STK11-mutant (NCI-H1993 and NCI-H1395) and wild-type cell lines (NCI-H82 and NCI-H524). Average percentage growth of each cell line by a PDE4D inhibitor was based on the DMSO control. Cells were treated with a 20 μmol/L of PDE4D inhibitors for 3, 7, and 10 days incubation, respectively. The cell viability was determined using CellTiter-Blue fluorescence. *, P < 0.01 and **, P < 0.05 in the difference between STK11-mutant and wild-type cell lines. All cells used in the experiment were cultured in normal conditioned RPMI medium with 10% FBS and 1% penicillin/streptavidin.
Apremilast (CC-10004)は一種の経口生物有効なPDE4とTNF-α阻害剤で、IC50値が74 nMと77 nMです。
Cilostazol is a medication used in the alleviation of the symptom of intermittent claudication in individuals with peripheral vascular disease.
Milrinone is a potent and selective phosphodiesterase 3 inhibitor with an IC50 of 0.42 μM for the inhibition of FIII PDE.
Avanafilは、選択性の高いPDE5 の阻害剤で、IC50 が1 nMです。
Aminophylline is a competitive nonselective phosphodiesterase inhibitor with an IC50 of 0.12 mM and also a nonselective adenosine receptor antagonist.
Anagrelide HCl is a drug used for the treatment of essential thrombocytosis.
Irsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
Dyphylline is a xanthine derivative with bronchodilator and vasodilator effects.
Dipyridamole (Persantine) is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.
Fenspiride is a bronchodilator with anti-inflammatory properties, inhibiting phosphodiesterase 4 and phosphodiesterase 3 activities with logIC50 values of 4.16 and 3.44, respectively, in human isolated bronchi.
Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.
Diosgenin is a steroid sapogenin and the precursor for the semisynthesis of progesterone which in turn was used in early combined oral contraceptive pills.
Icariin is a flavonol and PDE5 inhibitor with IC50 of 1.0, 0.75, and 1.1 μM for PDE5A1, A2, and A3, respectively.
Sildenafil MesylateはSildenafilのメシル酸（mesylate）の形式です。SildenafilはPhosphodiesterase 5の阻害剤です。
Sildenafilは1種のPhosphodiesterase 5の阻害剤です。このIC50値は5.22 nMです。
mRNA and protein expression levels of Id‑1 following treatment with 5 μM sildenafil for 24 h. (A) Relative mRNA expression levels of Id‑1 in the HemECs were significantly decreased by 44.2%, according to the 2‑ΔΔCq method (***P=0.0006 vs. control). (B) Western blotting revealed that the protein expression levels of Id‑1 markedly decreased following treatment with sildenafil when compared with the negative control. The TCA 8113 cell line was used as a positive control. HemECs, hemangioma endothelial cells; SIL, sildenafil; ID‑1, inhibitor of differentiation 1.
Luteolin is a non-selective PDE inhibitor for PDE1-5 with Ki of 15.0 μM, 6.4 μM, 13.9 μM, 11.1 μM and 9.5 μM, respectively.
Bioactive compounds inhibit recombinant HDAC activity. Recombinant HDACs were incubated with flavonoid Luteolin (C) for 2 h prior to the addition of cell permeable HDAC substrates. Luteolin inhibited activity of most classes I, IIa, and IIb HDAC isoforms.
Theobromine is a xanthine alkaloid that is used as a bronchodilator and as a vasodilator.