PDE

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抑制剂选择性比较

特异性亚型抑制剂

PDE产品

所有产品(50) PDE抑制剂(49) PDE激活剂(1)

目录号	产品描述	文献引用	实验数据
S2131	Roflumilast (B9302-107) Roflumilast (APTA 2217, B9302-107, BY 217, BYK 20869)是一种选择性的PDE4抑制剂，无细胞试验中IC50为0.2-4.3 nM。	EMBO Rep, 2021, e51329 Free Radic Biol Med, 2021, 163:281-296 Mol Cell, 2020, 80(6):1104-1122.e9	Mean plasma concentration versus time after single dose oral administration of IC87114 and RFM in wistar rats( n = 6).
S1431	Sildenafil Citrate Sildenafil Citrate，一种环鸟苷酸单磷酸盐(cGMP)特异性的Ⅵ型磷酸二酯酶(PDE5)选择性抑制剂，对勃起功能障碍具有良好的耐受性和较高作用效果。	Int J Mol Med, 2022, 49(2)19 J Clin Invest, 2021, 131(1)136779 Cardiovasc Res, 2021, 117(5):1391-1401	T24 cells were treated with vehicle, SIL (2 uM), DOX (200 nM) as indicated. Cells were isolated 6 and 12 hours after exposure, and the phosphorylation of γH2AX was determined, with the fold increase in phosphorylation shown.
S1455	Cilomilast Cilomilast (SB-207499)是一种有效的PDE4抑制剂，IC50为110 nM，具有抗炎活性和弱的中枢神经系统活性。Phase 3。	Am J Physiol Renal Physiol, 2020, 318(3):F576-F588 J Pharm Biomed Anal, 2016, 117:47-60 Mol Cancer Res, 2015, 13(1):149-60	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.
S1512	Tadalafil (IC351) Tadalafil (IC351)是一种PDE-5抑制剂，无细胞试验中IC50为1.8 nM。Tadalafil对PDE5的选择性比对PDEs家族中其他成员高9000倍以上，除了PDE11。它能部分抑制PDE11。	J Clin Invest, 2021, 131(1)136779 Biochim Biophys Acta Mol Basis Dis, 2021, 1867(12):166267 Mol Biochem Parasitol, 2021, 244:111392	β-Catenin levels in 293T cells treated with PDE5 inhibitor in the presence or absence of Wnt3a. (a) Tadalafil reduced β-catenin protein levels. Immunofluorescence and confocal images of 293T cells treated with dimethyl sulfoxide (DMSO) or tadalafil at 10 uM in the presence or absence of recombinant Wnt3a for 24 h.
S2515	Vardenafil HCl Trihydrate Vardenafil HCl Trihydrate (BAY38-9456)是一种新型PDE抑制剂，作用于PDE5和PDE1，IC50分别为0.7和180 nM。	Gastroenterology, 2020, 159(3):1068-1084.e2 Bone, 2020, 10.1016/j.bone.2020.115305 Pulm Pharmacol Ther, 2020, 66:101985	(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.
E0346^New	Ro 20-1724 Ro 20-1724 是一种有效的 PDE IV 抑制剂，Ki 值为 3.1 μM, 也是一种有效的胃促分泌剂。
S1550	Pimobendan Pimobendan (UD-CG 115 BS) 是一种磷酸二酯酶III(PDE III)选择性抑制剂，IC50为0.32 μM。	Sci Rep, 2020, 10(1):19723 Front Microbiol, 2020, 10:2936 Cell Syst, 2019, 8(2):97-108
S2620	GSK256066 GSK256066是一种选择性的PDE4B(与A-D亚型具有相等的亲和力)抑制剂，IC50为3.2 pM，比作用于PDE1/2/3/5/6选择性高380，000倍以上，作用于PDE4B比作用于PDE7选择性高2500倍以上。Phase 2。	J Aerosol Med Pulm Drug Deliv, 2019, 32(6):396-404
S2687	Mardepodect (PF-2545920) Mardepodect (PF-2545920)是一种有效的，选择性的PDE10A抑制剂，IC50为0.37 nM，比作用于PDE选择性高1000倍以上。	J Neuroimmune Pharmacol, 2020, 10.1007/s11481-020-09943-6 Front Mol Neurosci, 2017, 10:100 Oncotarget, 2017, 8(41):69264-69280
S1430	Rolipram (ZK-62711) PDE4的选择性抑制剂，Rolipram (ZK-62711, SB 95952)，抑制免疫纯化的PDE4B和PDE4D活性，IC50分别为130 nM和240 nM。具有抗炎活性。	Antioxidants (Basel), 2021, 10(3)460 Sci Rep, 2021, 11(1):19737 Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00768-4	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.
S8034	Apremilast (CC-10004) Apremilast (CC-10004)是一种口服生物有效的PDE4和TNF-α抑制剂，IC50分别为74 nM和77 nM。	Int J Mol Sci, 2021, 22(23)12878 J Immunotoxicol, 2021, 18(1):154-162 Acta Pharmaceutica Sinica B, 2021, 10.1016/j.apsb.2021.04.007
S1294	Cilostazol (OPC-13013) Cilostazol (OPC-13013)是一种环核苷酸磷酸二酯酶3型(PDE3)抑制剂，IC50为0.2 μM，也抑制腺苷酸的摄取。	Cell Chem Biol, 2022, S2451-9456(22)00006-X Front Pharmacol, 2021, 12:749930 Front Cell Infect Microbiol, 2021, 11:783085
S2484	Milrinone Milrinone (Win 47203)是一种有效的，选择性的磷酸二酯酶-3抑制剂，抑制FIII PDE，IC50为0.42 μM。	J Assist Reprod Genet, 2022, 10.1007/s10815-021-02330-x Biochem Biophys Res Commun, 2018, 503(3):1409-1414 Mol Pharm, 2017, 10.1021/acs.molpharmaceut.7b00360	Viability of H9c2 cells incubated with MRN-HSA-NPs (black bars) compared with MRN-Lactate (grey bars) at different MRN concentrations, at (a) 4 hours, (b) 24 hours and (c) 48 hours. The graph shows a representative result of mean±SD (n=3). **P<0.0001, P<0.001, P<0.01 and P<0.05 were considered significant based on Sidak’s posthoc analysis.
S4019	Avanafil Avanafil是一种高度选择性PDE5抑制剂，IC50为1nM.	Cell Rep, 2021, 37(1):109774
S2127	S-(+)-Rolipram S-(+)-Rolipram 抑制人体单核细胞环AMP特异性的PDE4，IC50为0.75 μM，作用于中枢神经系统，具有消炎和抗抑郁活性，比其R-对映体作用效果稍弱。	Viruses, 2019, 11(12)
S1673	Aminophylline Aminophylline (Phyllocontin)是一种竞争性的，非选择性的磷酸二酯酶抑制剂，IC50为0.12 mM，也是非选择性的腺苷受体拮抗剂。	Gastroenterology, 2020, 159(3):1068-1084.e2
S3172	Anagrelide HCl Anagrelide (BL-4162A)是一种治疗原发性血小板增多症的药物。是一种口服的imidazoquinazoline药剂，具有抗环腺苷酸磷酸二酯酶的活性并且在人和动物中都能抑制血小板聚集。Anagrelide通过抑制巨核细胞成熟为血小板来起作用。	Cell Chem Biol, 2022, S2451-9456(22)00006-X Nat Cancer, 2020, 1(2):235-248
S1929	Irsogladine Irsogladine是一种抗胃溃疡剂，通过M1 muscarininc乙酰胆碱受体结合，有利于细胞间隙连接通讯。
S1504	Dyphylline Dyphylline (Diprophylline)是一种黄嘌呤衍生物，具有扩张支气管和血管的作用。	Biogerontology, 2016, 17(5-6):907-920
S1895	Dipyridamole (NSC 515776) Dipyridamole (NSC-515776, Persantine)是一种磷酸二酯酶抑制剂，通过红细胞和血管内皮细胞，抑制腺苷的摄取和代谢。	Stem Cells, 2020, 38(8):1020-1033 Stem Cells, 2020, 28 Am J Hum Genet, 2017, 100(1):5-20
S4164	Doxofylline Doxofylline (Doxophylline) 是一种磷酸二酯酶抑制剂，是黄嘌呤衍生物，用于治疗哮喘。
S4090	Fenspiride HCl Fenspiride是一种支气管扩张剂，具有抗炎特性，作用于人离体的支气管，抑制磷酸二酯酶4和磷酸二酯酶3活性，logIC50值分别为4.16和3.44。
S0501	Enpp-1-IN-1 Enpp-1-IN-1 (UUN28589, MV 658)是一种 Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1) 的抑制剂。	NPJ Breast Cancer, 2022, 8(1):44 Arthritis Res Ther, 2022, 24(1):44
S4837	Ibudilast Ibudilast (KC-404, AV411, MN166) 是一种相对非选择性的phosphodiesterase抑制剂，具有抗炎和神经保护活性。	Neuron, 2020, 108(5):876-886.e4 CU Scholar, 2019, N/A
S5014	Crisaborole (AN2728) Crisaborole (AN2728) 是选择性的小分子PDE4抑制剂，具有广谱的抗炎活性。
S6844	Zatolmilast (BPN14770) Zatolmilast (BPN14770)是一种 phosphodiesterase 4D (PDE4D) 的选择性变构抑制剂，对于PDE4D7和PDE4D3的IC50值分别为7.8 nM和7.4 nM。
S8895	Ziritaxestat (GLPG1690) Ziritaxestat (GLPG1690)是选择性的自毒素抑制剂，IC50为131 nM，Ki值为15 nM。	Front Cell Dev Biol, 2021, 9:656153
S7224	Deltarasin Deltarasin是一种小分子抑制剂，抑制KRAS-PDEδ相互作用，其结合到纯PDEδ的K_d值为38 nM。	Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0268-y Cell Death Differ, 2019, 26(11):2400-2415 Nat Commun, 2018, 9(1):672
S0039	BI-409306 BI 409306 (SUB 166499)是一种有效的、选择性的 PDE9A 抑制剂，对人类PDE9A和大鼠PDE9A的平均IC50值分别为65 nM和168 nM。BI 409306 可提高大脑cGMP水平并具有长期的增强作用，可提高啮齿动物的情景记忆和工作记忆的表现。
S5806	Cilostamide Cilostamide (OPC 3689)是type III phosphodiesterases的抑制剂，对PDE3A 和PDE3B的IC50值分别为27 nM和50 nM。
S5539	Olprinone Olprinone is a phosphodiesterase III (PDE3) inhibitor with IC50 values of 0.35 mM, 150 mM and 100 mM for human cardiac PDE III, PDE I and PDE II, respectively.
S6186	3-Methylxanthine 3-Methylxanthine (3-MX) 是3-甲基黄嘌呤，一种环状 guanosine monophosphate (GMP) phosphodiesterase (PDE) 的抑制剂，在豚鼠分离的气管肌肉中的IC50值为920 μM。
S8459	TAK-063 TAK-063 (Balipodect)是新型的、选择性的PDE10A抑制剂，IC50为0.30 nM。	Int J Mol Sci, 2021, 22(18)9665
S5957	Vardenafil hydrochloride Vardenafil (BAY38-9456, Levitra, Staxyn) hydrochloride 是一种选择性的、口服活性的 phosphodiesterase (PDE) 的抑制剂，对PDE5、PDE6和PDE1的IC50值分别为0.7 nM、11 nM和180 nM。	Cells, 2021, 10(12)3502
S6576	BW-A78U BW-A78U是PDE抑制剂，具有抗惊厥活性。
S2291	Diosgenin Diosgenin 是一种类固醇皂甙元，为半合成孕激素的前体，在早期与口服避孕药一起使用。	Neurochem Res, 2020, 10.1007/s11064-020-03093-0
S2312	Icariin Icariin是一种cGMP特异性的PDE5抑制剂，IC50为0.432 μM，作用于PDE5比作用于PDE4选择性高167倍。	Phytomedicine, 2021, 80:153387 Br J Nutr, 2021, 1-11 J Med Virol, 2019, 91(8):1440-1447
S0127	CP-671305 CP-671305 是一种有效的、选择性的、口服活性的 phosphodiesterase-4-D (PDE4-D) 抑制剂，其IC50值为3 nM。
S4683	Sildenafil Mesylate Sildenafil Mesylate是Sildenafil的甲磺酸盐形式，Sildenafil是Phosphodiesterase 5的抑制剂。	Cardiovasc Res, 2021, 117(5):1391-1401 Sci Rep, 2020, 10(1):18084 Oncotarget, 2016, 7(11):12975-96
S4684	Sildenafil Sildenafil (Revatio, UK-92480, Viagra) 是Phosphodiesterase 5抑制剂，其IC50为5.22 nM。	Cardiovasc Res, 2021, 117(5):1391-1401 J Cell Physiol, 2020, 10.1002/jcp.29580 Bone, 2020, 10.1016/j.bone.2020.115305	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.
S2320	Luteolin Luteolin (Luteoline, Luteolol, Digitoflavone)是一种非选择性的PDE抑制剂，作用于PDE1-5，K_i分别为15.0 μM， 6.4 μM， 13.9 μM， 11.1 μM和9.5 μM。Phase 2.	Front Endocrinol (Lausanne), 2022, 13:866641 Cancer Lett, 2021, 515:36-48 Molecules, 2021, 26(5)1210	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.
S8218	PF-8380 PF-8380是一种有效的自毒素 (ATX)抑制剂，在体外酶活性实验中测得IC50为2.8 nM。	Leuk Lymphoma, 2021, 1-12
S4345	Pentoxifylline Pentoxifylline is a competitive nonselective phosphodiesterase inhibitor which raises intracellular cAMP, activates PKA, inhibits TNF and leukotriene synthesis, and reduces inflammation and innate immunity.	Biogerontology, 2016, 17(5-6):907-920
S5836	IBMX IBMX (Isobutylmethylxanthine, 1-Methyl-3-Isobutylxanthine)是一种非特异性phosphodiesterase (PDE)抑制剂，对PDE3、PDE4、PDE5的IC50值分别为6.5±1.2, 26.3±3.9 和 31.7±5.3 μM。它能增强细胞内cAMP水平，是adenosine (A1) receptor拮抗剂。	Bone Res, 2022, 10(1):27 PLoS One, 2019, 14(3):e0214554 Toxicology, 2018, 394:1-10
S9436	Pinoresinol dimethyl ether Pinoresinol dimethyl ether, which could be isolated from the wood of the basal tree Humbertieae, show a variety of activities as the inhibitor of cyclic AMP phosphodiesterase.
S5837	BRL-50481 BRL-50481是一种新型的PDE7选择性抑制剂，结合Ki值为180±10 nM，对hrPDE7A1的选择性是对其他PDEs选择性的至少200倍。	Oncogene, 2017, 36(23):3252-3262
S6433	Udenafil Udenafil是一种有效的PDE5拮抗剂，IC50为8.25 nM。其对其他PDEs的选择性与sildenafil相当。
S2368	Theobromine Theobromine (3,7-Dimethylxanthine)是黄嘌呤生物碱，作为一种支气管扩张剂，血管扩张剂。
S7858	Dibutyryl-cAMP (Bucladesine) Dibutyryl-cAMP (Bucladesine, dbcAMP)是一种细胞可渗透性 PKA 激活剂，通过模拟内源性 cAMP 发挥作用。Dibutyryl-cAMP (Bucladesine)也是一种 phosphodiesterase (PDE) 抑制剂。	Nucleic Acids Res, 2022, 50(5):2700-2718 Nat Commun, 2021, 12(1):4050 EMBO Mol Med, 2021, e12632
S9229	Linderane Linderane, isolated from Lindera strychnifolia vill., is an indirect PDE3 activator and possesses multiple biological effects, including superoxide anion radical-scavenging and antioxidative activity and protective activity against gastritis, gastric ulcers and backache.

目录号	产品描述	文献引用	实验数据
S2131	Roflumilast (B9302-107) Roflumilast (APTA 2217, B9302-107, BY 217, BYK 20869)是一种选择性的PDE4抑制剂，无细胞试验中IC50为0.2-4.3 nM。	EMBO Rep,2021, e51329 Free Radic Biol Med,2021, 163:281-296 Mol Cell,2020, 80(6):1104-1122.e9	Mean plasma concentration versus time after single dose oral administration of IC87114 and RFM in wistar rats( n = 6).
S1431	Sildenafil Citrate Sildenafil Citrate，一种环鸟苷酸单磷酸盐(cGMP)特异性的Ⅵ型磷酸二酯酶(PDE5)选择性抑制剂，对勃起功能障碍具有良好的耐受性和较高作用效果。	Int J Mol Med,2022, 49(2)19 J Clin Invest,2021, 131(1)136779 Cardiovasc Res,2021, 117(5):1391-1401	T24 cells were treated with vehicle, SIL (2 uM), DOX (200 nM) as indicated. Cells were isolated 6 and 12 hours after exposure, and the phosphorylation of γH2AX was determined, with the fold increase in phosphorylation shown.
S1455	Cilomilast Cilomilast (SB-207499)是一种有效的PDE4抑制剂，IC50为110 nM，具有抗炎活性和弱的中枢神经系统活性。Phase 3。	Am J Physiol Renal Physiol,2020, 318(3):F576-F588 J Pharm Biomed Anal,2016, 117:47-60 Mol Cancer Res,2015, 13(1):149-60	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.
S1512	Tadalafil (IC351) Tadalafil (IC351)是一种PDE-5抑制剂，无细胞试验中IC50为1.8 nM。Tadalafil对PDE5的选择性比对PDEs家族中其他成员高9000倍以上，除了PDE11。它能部分抑制PDE11。	J Clin Invest,2021, 131(1)136779 Biochim Biophys Acta Mol Basis Dis,2021, 1867(12):166267 Mol Biochem Parasitol,2021, 244:111392	β-Catenin levels in 293T cells treated with PDE5 inhibitor in the presence or absence of Wnt3a. (a) Tadalafil reduced β-catenin protein levels. Immunofluorescence and confocal images of 293T cells treated with dimethyl sulfoxide (DMSO) or tadalafil at 10 uM in the presence or absence of recombinant Wnt3a for 24 h.
S2515	Vardenafil HCl Trihydrate Vardenafil HCl Trihydrate (BAY38-9456)是一种新型PDE抑制剂，作用于PDE5和PDE1，IC50分别为0.7和180 nM。	Gastroenterology,2020, 159(3):1068-1084.e2 Bone,2020, 10.1016/j.bone.2020.115305 Pulm Pharmacol Ther,2020, 66:101985	(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.
E0346^New	Ro 20-1724 Ro 20-1724 是一种有效的 PDE IV 抑制剂，Ki 值为 3.1 μM, 也是一种有效的胃促分泌剂。
S1550	Pimobendan Pimobendan (UD-CG 115 BS) 是一种磷酸二酯酶III(PDE III)选择性抑制剂，IC50为0.32 μM。	Sci Rep,2020, 10(1):19723 Front Microbiol,2020, 10:2936 Cell Syst,2019, 8(2):97-108
S2620	GSK256066 GSK256066是一种选择性的PDE4B(与A-D亚型具有相等的亲和力)抑制剂，IC50为3.2 pM，比作用于PDE1/2/3/5/6选择性高380，000倍以上，作用于PDE4B比作用于PDE7选择性高2500倍以上。Phase 2。	J Aerosol Med Pulm Drug Deliv,2019, 32(6):396-404
S2687	Mardepodect (PF-2545920) Mardepodect (PF-2545920)是一种有效的，选择性的PDE10A抑制剂，IC50为0.37 nM，比作用于PDE选择性高1000倍以上。	J Neuroimmune Pharmacol,2020, 10.1007/s11481-020-09943-6 Front Mol Neurosci,2017, 10:100 Oncotarget,2017, 8(41):69264-69280
S1430	Rolipram (ZK-62711) PDE4的选择性抑制剂，Rolipram (ZK-62711, SB 95952)，抑制免疫纯化的PDE4B和PDE4D活性，IC50分别为130 nM和240 nM。具有抗炎活性。	Antioxidants (Basel),2021, 10(3)460 Sci Rep,2021, 11(1):19737 Acta Pharmacol Sin,2021, 10.1038/s41401-021-00768-4	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.
S8034	Apremilast (CC-10004) Apremilast (CC-10004)是一种口服生物有效的PDE4和TNF-α抑制剂，IC50分别为74 nM和77 nM。	Int J Mol Sci,2021, 22(23)12878 J Immunotoxicol,2021, 18(1):154-162 Acta Pharmaceutica Sinica B,2021, 10.1016/j.apsb.2021.04.007
S1294	Cilostazol (OPC-13013) Cilostazol (OPC-13013)是一种环核苷酸磷酸二酯酶3型(PDE3)抑制剂，IC50为0.2 μM，也抑制腺苷酸的摄取。	Cell Chem Biol,2022, S2451-9456(22)00006-X Front Pharmacol,2021, 12:749930 Front Cell Infect Microbiol,2021, 11:783085
S2484	Milrinone Milrinone (Win 47203)是一种有效的，选择性的磷酸二酯酶-3抑制剂，抑制FIII PDE，IC50为0.42 μM。	J Assist Reprod Genet,2022, 10.1007/s10815-021-02330-x Biochem Biophys Res Commun,2018, 503(3):1409-1414 Mol Pharm,2017, 10.1021/acs.molpharmaceut.7b00360	Viability of H9c2 cells incubated with MRN-HSA-NPs (black bars) compared with MRN-Lactate (grey bars) at different MRN concentrations, at (a) 4 hours, (b) 24 hours and (c) 48 hours. The graph shows a representative result of mean±SD (n=3). **P<0.0001, P<0.001, P<0.01 and P<0.05 were considered significant based on Sidak’s posthoc analysis.
S4019	Avanafil Avanafil是一种高度选择性PDE5抑制剂，IC50为1nM.	Cell Rep,2021, 37(1):109774
S2127	S-(+)-Rolipram S-(+)-Rolipram 抑制人体单核细胞环AMP特异性的PDE4，IC50为0.75 μM，作用于中枢神经系统，具有消炎和抗抑郁活性，比其R-对映体作用效果稍弱。	Viruses,2019, 11(12)
S1673	Aminophylline Aminophylline (Phyllocontin)是一种竞争性的，非选择性的磷酸二酯酶抑制剂，IC50为0.12 mM，也是非选择性的腺苷受体拮抗剂。	Gastroenterology,2020, 159(3):1068-1084.e2
S3172	Anagrelide HCl Anagrelide (BL-4162A)是一种治疗原发性血小板增多症的药物。是一种口服的imidazoquinazoline药剂，具有抗环腺苷酸磷酸二酯酶的活性并且在人和动物中都能抑制血小板聚集。Anagrelide通过抑制巨核细胞成熟为血小板来起作用。	Cell Chem Biol,2022, S2451-9456(22)00006-X Nat Cancer,2020, 1(2):235-248
S1929	Irsogladine Irsogladine是一种抗胃溃疡剂，通过M1 muscarininc乙酰胆碱受体结合，有利于细胞间隙连接通讯。
S1504	Dyphylline Dyphylline (Diprophylline)是一种黄嘌呤衍生物，具有扩张支气管和血管的作用。	Biogerontology,2016, 17(5-6):907-920
S1895	Dipyridamole (NSC 515776) Dipyridamole (NSC-515776, Persantine)是一种磷酸二酯酶抑制剂，通过红细胞和血管内皮细胞，抑制腺苷的摄取和代谢。	Stem Cells,2020, 38(8):1020-1033 Stem Cells,2020, 28 Am J Hum Genet,2017, 100(1):5-20
S4164	Doxofylline Doxofylline (Doxophylline) 是一种磷酸二酯酶抑制剂，是黄嘌呤衍生物，用于治疗哮喘。
S4090	Fenspiride HCl Fenspiride是一种支气管扩张剂，具有抗炎特性，作用于人离体的支气管，抑制磷酸二酯酶4和磷酸二酯酶3活性，logIC50值分别为4.16和3.44。
S0501	Enpp-1-IN-1 Enpp-1-IN-1 (UUN28589, MV 658)是一种 Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1) 的抑制剂。	NPJ Breast Cancer,2022, 8(1):44 Arthritis Res Ther,2022, 24(1):44
S4837	Ibudilast Ibudilast (KC-404, AV411, MN166) 是一种相对非选择性的phosphodiesterase抑制剂，具有抗炎和神经保护活性。	Neuron,2020, 108(5):876-886.e4 CU Scholar,2019, N/A
S5014	Crisaborole (AN2728) Crisaborole (AN2728) 是选择性的小分子PDE4抑制剂，具有广谱的抗炎活性。
S6844	Zatolmilast (BPN14770) Zatolmilast (BPN14770)是一种 phosphodiesterase 4D (PDE4D) 的选择性变构抑制剂，对于PDE4D7和PDE4D3的IC50值分别为7.8 nM和7.4 nM。
S8895	Ziritaxestat (GLPG1690) Ziritaxestat (GLPG1690)是选择性的自毒素抑制剂，IC50为131 nM，Ki值为15 nM。	Front Cell Dev Biol,2021, 9:656153
S7224	Deltarasin Deltarasin是一种小分子抑制剂，抑制KRAS-PDEδ相互作用，其结合到纯PDEδ的K_d值为38 nM。	Acta Pharmacol Sin,2019, 10.1038/s41401-019-0268-y Cell Death Differ,2019, 26(11):2400-2415 Nat Commun,2018, 9(1):672
S0039	BI-409306 BI 409306 (SUB 166499)是一种有效的、选择性的 PDE9A 抑制剂，对人类PDE9A和大鼠PDE9A的平均IC50值分别为65 nM和168 nM。BI 409306 可提高大脑cGMP水平并具有长期的增强作用，可提高啮齿动物的情景记忆和工作记忆的表现。
S5806	Cilostamide Cilostamide (OPC 3689)是type III phosphodiesterases的抑制剂，对PDE3A 和PDE3B的IC50值分别为27 nM和50 nM。
S5539	Olprinone Olprinone is a phosphodiesterase III (PDE3) inhibitor with IC50 values of 0.35 mM, 150 mM and 100 mM for human cardiac PDE III, PDE I and PDE II, respectively.
S6186	3-Methylxanthine 3-Methylxanthine (3-MX) 是3-甲基黄嘌呤，一种环状 guanosine monophosphate (GMP) phosphodiesterase (PDE) 的抑制剂，在豚鼠分离的气管肌肉中的IC50值为920 μM。
S8459	TAK-063 TAK-063 (Balipodect)是新型的、选择性的PDE10A抑制剂，IC50为0.30 nM。	Int J Mol Sci,2021, 22(18)9665
S5957	Vardenafil hydrochloride Vardenafil (BAY38-9456, Levitra, Staxyn) hydrochloride 是一种选择性的、口服活性的 phosphodiesterase (PDE) 的抑制剂，对PDE5、PDE6和PDE1的IC50值分别为0.7 nM、11 nM和180 nM。	Cells,2021, 10(12)3502
S6576	BW-A78U BW-A78U是PDE抑制剂，具有抗惊厥活性。
S2291	Diosgenin Diosgenin 是一种类固醇皂甙元，为半合成孕激素的前体，在早期与口服避孕药一起使用。	Neurochem Res,2020, 10.1007/s11064-020-03093-0
S2312	Icariin Icariin是一种cGMP特异性的PDE5抑制剂，IC50为0.432 μM，作用于PDE5比作用于PDE4选择性高167倍。	Phytomedicine,2021, 80:153387 Br J Nutr,2021, 1-11 J Med Virol,2019, 91(8):1440-1447
S0127	CP-671305 CP-671305 是一种有效的、选择性的、口服活性的 phosphodiesterase-4-D (PDE4-D) 抑制剂，其IC50值为3 nM。
S4683	Sildenafil Mesylate Sildenafil Mesylate是Sildenafil的甲磺酸盐形式，Sildenafil是Phosphodiesterase 5的抑制剂。	Cardiovasc Res,2021, 117(5):1391-1401 Sci Rep,2020, 10(1):18084 Oncotarget,2016, 7(11):12975-96
S4684	Sildenafil Sildenafil (Revatio, UK-92480, Viagra) 是Phosphodiesterase 5抑制剂，其IC50为5.22 nM。	Cardiovasc Res,2021, 117(5):1391-1401 J Cell Physiol,2020, 10.1002/jcp.29580 Bone,2020, 10.1016/j.bone.2020.115305	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.
S2320	Luteolin Luteolin (Luteoline, Luteolol, Digitoflavone)是一种非选择性的PDE抑制剂，作用于PDE1-5，K_i分别为15.0 μM， 6.4 μM， 13.9 μM， 11.1 μM和9.5 μM。Phase 2.	Front Endocrinol (Lausanne),2022, 13:866641 Cancer Lett,2021, 515:36-48 Molecules,2021, 26(5)1210	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.
S8218	PF-8380 PF-8380是一种有效的自毒素 (ATX)抑制剂，在体外酶活性实验中测得IC50为2.8 nM。	Leuk Lymphoma,2021, 1-12
S4345	Pentoxifylline Pentoxifylline is a competitive nonselective phosphodiesterase inhibitor which raises intracellular cAMP, activates PKA, inhibits TNF and leukotriene synthesis, and reduces inflammation and innate immunity.	Biogerontology,2016, 17(5-6):907-920
S5836	IBMX IBMX (Isobutylmethylxanthine, 1-Methyl-3-Isobutylxanthine)是一种非特异性phosphodiesterase (PDE)抑制剂，对PDE3、PDE4、PDE5的IC50值分别为6.5±1.2, 26.3±3.9 和 31.7±5.3 μM。它能增强细胞内cAMP水平，是adenosine (A1) receptor拮抗剂。	Bone Res,2022, 10(1):27 PLoS One,2019, 14(3):e0214554 Toxicology,2018, 394:1-10
S9436	Pinoresinol dimethyl ether Pinoresinol dimethyl ether, which could be isolated from the wood of the basal tree Humbertieae, show a variety of activities as the inhibitor of cyclic AMP phosphodiesterase.
S5837	BRL-50481 BRL-50481是一种新型的PDE7选择性抑制剂，结合Ki值为180±10 nM，对hrPDE7A1的选择性是对其他PDEs选择性的至少200倍。	Oncogene,2017, 36(23):3252-3262
S6433	Udenafil Udenafil是一种有效的PDE5拮抗剂，IC50为8.25 nM。其对其他PDEs的选择性与sildenafil相当。
S2368	Theobromine Theobromine (3,7-Dimethylxanthine)是黄嘌呤生物碱，作为一种支气管扩张剂，血管扩张剂。
S7858	Dibutyryl-cAMP (Bucladesine) Dibutyryl-cAMP (Bucladesine, dbcAMP)是一种细胞可渗透性 PKA 激活剂，通过模拟内源性 cAMP 发挥作用。Dibutyryl-cAMP (Bucladesine)也是一种 phosphodiesterase (PDE) 抑制剂。	Nucleic Acids Res,2022, 50(5):2700-2718 Nat Commun,2021, 12(1):4050 EMBO Mol Med,2021, e12632

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S9229	Linderane Linderane, isolated from Lindera strychnifolia vill., is an indirect PDE3 activator and possesses multiple biological effects, including superoxide anion radical-scavenging and antioxidative activity and protective activity against gastritis, gastric ulcers and backache.

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S9229

Linderane

Linderane, isolated from Lindera strychnifolia vill., is an indirect PDE3 activator and possesses multiple biological effects, including superoxide anion radical-scavenging and antioxidative activity and protective activity against gastritis, gastric ulcers and backache.

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