PDE
特异性亚型抑制剂
PDE产品
目录号 | 产品描述 | 文献引用 | 实验数据 |
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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。 |
![]() ![]() Mean plasma concentration versus time after single dose oral administration of IC87114 and RFM in wistar rats( n = 6). |
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S1431 |
Sildenafil CitrateSildenafil 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。 |
![]() ![]() 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. |
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S1455 |
CilomilastCilomilast (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。 |
![]() ![]() 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.
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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。 |
![]() ![]() 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.
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S2515 |
Vardenafil HCl TrihydrateVardenafil 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。 |
![]() ![]() (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.
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E0346New |
Ro 20-1724Ro 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。 |
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S1550 |
PimobendanPimobendan (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。 |
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S2620 |
GSK256066GSK256066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。 |
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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。 |
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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。 |
![]() ![]() 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.
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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。 |
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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。 |
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S2484 |
MilrinoneMilrinone (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。 |
![]() ![]() 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. |
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S4019 |
AvanafilAvanafil是一种高度选择性PDE5抑制剂,IC50为1nM. |
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S2127 |
S-(+)-RolipramS-(+)-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。 |
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S1673 |
AminophyllineAminophylline (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。 |
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S3172 |
Anagrelide HClAnagrelide (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。 |
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S1929 |
IrsogladineIrsogladine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。 |
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S1504 |
DyphyllineDyphylline (Diprophylline)是一种黄嘌呤衍生物,具有扩张支气管和血管的作用。 |
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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。 |
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S4164 |
DoxofyllineDoxofylline (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。 |
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S4090 |
Fenspiride HClFenspiride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。 |
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S0501 |
Enpp-1-IN-1Enpp-1-IN-1 (UUN28589, MV 658)是一种 Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1) 的抑制剂。 |
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S4837 |
IbudilastIbudilast (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。 |
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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。 |
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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。 |
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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。 |
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S7224 |
DeltarasinDeltarasin是一种小分子抑制剂,抑制KRAS-PDEδ相互作用,其结合到纯PDEδ的Kd值为38 nM。 |
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S0039 |
BI-409306BI 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。 |
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S5806 |
CilostamideCilostamide (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。 |
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S5539 |
OlprinoneOlprinone 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. |
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S6186 |
3-Methylxanthine3-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。 |
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S8459 |
TAK-063TAK-063 (Balipodect)是新型的、选择性的PDE10A抑制剂,IC50为0.30 nM。 |
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S5957 |
Vardenafil hydrochlorideVardenafil (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。 |
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S6576 |
BW-A78UBW-A78U是PDE抑制剂,具有抗惊厥活性。 |
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S2291 |
DiosgeninDiosgenin 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。 |
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S2312 |
IcariinIcariin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。 |
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S0127 |
CP-671305CP-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。 |
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S4683 |
Sildenafil MesylateSildenafil Mesylate是Sildenafil的甲磺酸盐形式,Sildenafil是Phosphodiesterase 5的抑制剂。 |
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S4684 |
SildenafilSildenafil (Revatio, UK-92480, Viagra) 是Phosphodiesterase 5抑制剂,其IC50为5.22 nM。 |
![]() ![]() 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.
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S2320 |
LuteolinLuteolin (Luteoline, Luteolol, Digitoflavone)是一种非选择性的PDE抑制剂,作用于PDE1-5,Ki分别为15.0 μM, 6.4 μM, 13.9 μM, 11.1 μM和9.5 μM。Phase 2. |
![]() ![]() 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. |
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S8218 |
PF-8380PF-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。 |
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S4345 |
PentoxifyllinePentoxifylline is a competitive nonselective phosphodiesterase inhibitor which raises intracellular cAMP, activates PKA, inhibits TNF and leukotriene synthesis, and reduces inflammation and innate immunity. |
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S5836 |
IBMXIBMX (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。 |
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S9436 |
Pinoresinol dimethyl etherPinoresinol 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. |
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S5837 |
BRL-50481BRL-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。 |
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S6433 |
UdenafilUdenafil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。 |
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S2368 |
TheobromineTheobromine (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。 |
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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。 |
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S9229 |
LinderaneLinderane, 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。 |
![]() ![]() Mean plasma concentration versus time after single dose oral administration of IC87114 and RFM in wistar rats( n = 6). |
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S1431 |
Sildenafil CitrateSildenafil 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。 |
![]() ![]() 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. |
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S1455 |
CilomilastCilomilast (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。 |
![]() ![]() 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.
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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。 |
![]() ![]() 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.
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S2515 |
Vardenafil HCl TrihydrateVardenafil 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。 |
![]() ![]() (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.
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E0346New |
Ro 20-1724Ro 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。 |
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S1550 |
PimobendanPimobendan (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。 |
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S2620 |
GSK256066GSK256066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。 |
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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。 |
![]() ![]() |
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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。 |
![]() ![]() 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.
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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。 |
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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。 |
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S2484 |
MilrinoneMilrinone (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。 |
![]() ![]() 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. |
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S4019 |
AvanafilAvanafil是一种高度选择性PDE5抑制剂,IC50为1nM. |
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S2127 |
S-(+)-RolipramS-(+)-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。 |
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S1673 |
AminophyllineAminophylline (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。 |
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S3172 |
Anagrelide HClAnagrelide (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。 |
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S1929 |
IrsogladineIrsogladine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 |
DyphyllineDyphylline (Diprophylline)是一种黄嘌呤衍生物,具有扩张支气管和血管的作用。 |
||
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。 |
||
S4164 |
DoxofyllineDoxofylline (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。 |
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S4090 |
Fenspiride HClFenspiride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。 |
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S0501 |
Enpp-1-IN-1Enpp-1-IN-1 (UUN28589, MV 658)是一种 Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1) 的抑制剂。 |
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S4837 |
IbudilastIbudilast (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。 |
||
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。 |
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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。 |
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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。 |
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S7224 |
DeltarasinDeltarasin是一种小分子抑制剂,抑制KRAS-PDEδ相互作用,其结合到纯PDEδ的Kd值为38 nM。 |
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S0039 |
BI-409306BI 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。 |
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S5806 |
CilostamideCilostamide (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。 |
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S5539 |
OlprinoneOlprinone 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. |
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S6186 |
3-Methylxanthine3-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。 |
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S8459 |
TAK-063TAK-063 (Balipodect)是新型的、选择性的PDE10A抑制剂,IC50为0.30 nM。 |
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S5957 |
Vardenafil hydrochlorideVardenafil (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。 |
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S6576 |
BW-A78UBW-A78U是PDE抑制剂,具有抗惊厥活性。 |
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S2291 |
DiosgeninDiosgenin 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。 |
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S2312 |
IcariinIcariin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。 |
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S0127 |
CP-671305CP-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。 |
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S4683 |
Sildenafil MesylateSildenafil Mesylate是Sildenafil的甲磺酸盐形式,Sildenafil是Phosphodiesterase 5的抑制剂。 |
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S4684 |
SildenafilSildenafil (Revatio, UK-92480, Viagra) 是Phosphodiesterase 5抑制剂,其IC50为5.22 nM。 |
![]() ![]() 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.
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S2320 |
LuteolinLuteolin (Luteoline, Luteolol, Digitoflavone)是一种非选择性的PDE抑制剂,作用于PDE1-5,Ki分别为15.0 μM, 6.4 μM, 13.9 μM, 11.1 μM和9.5 μM。Phase 2. |
![]() ![]() 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. |
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S8218 |
PF-8380PF-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。 |
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S4345 |
PentoxifyllinePentoxifylline is a competitive nonselective phosphodiesterase inhibitor which raises intracellular cAMP, activates PKA, inhibits TNF and leukotriene synthesis, and reduces inflammation and innate immunity. |
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S5836 |
IBMXIBMX (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。 |
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S9436 |
Pinoresinol dimethyl etherPinoresinol 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. |
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S5837 |
BRL-50481BRL-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。 |
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S6433 |
UdenafilUdenafil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。 |
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S2368 |
TheobromineTheobromine (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。 |
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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。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S9229 |
LinderaneLinderane, 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. |