48
8
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T21389 |
Enprofylline
Enprofilina,3-propylxanthine,3-n-Propylxanthine,Enprofyllinum,恩丙茶碱 |
Others | Others |
Enprofylline (Enprofilina) 是具有选择性的 A2B 受体竞争性拮抗剂 (Ki:7 μM) ,也是磷酸二酯酶抑制剂。它可用于研究哮喘、慢性阻塞性肺疾病。 | |||
T5956 |
VP3.15 dihydrobromide
|
GSK-3; PDE | Metabolism; PI3K/Akt/mTOR signaling; Stem Cells |
VP3.15 dihydrobromide 是一种口服具有活力的、高效的、CNS 可渗透的PDE7-GSK3双重抑制剂,对 PDE7 和 GSK3 作用的IC50值分别为 1.59 μM 和 0.88 μM。它具有神经保护和神经修复作用,可用于研究多发性硬化症 (MS) 潜在的抗炎和促髓鞘再生联合。 | |||
T3465 |
Vesnarinone
维司力农,OPC-8212,Arkin,Piteranometozine |
HIV Protease; PDE | Metabolism; Microbiology/Virology; Proteases/Proteasome |
Vesnarinone (Arkin) 是一种喹啉酮衍生物,可抑制磷酸二酯酶III 活性,增加钙通量和减小钾通量。 | |||
T1713 |
IBMX
IBMX,3-异丁基-1-甲基黄嘌呤,3-Isobutyl-1-methylxanthine,1-Methyl-3-Isobutylxanthine,Methylisobutylxanthine,Isobutylmethylxanthine |
PDE | Metabolism |
IBMX (Methylisobutylxanthine) 是一种广谱的磷酸二酯酶 (PDE) 抑制剂,对 PDE3、PDE4 和 PDE5 均有抑制活性 (IC50=6.5/26.3/31.7 μM)。IBMX 可以增强细胞内 cAMP 水平。 | |||
T16164 |
MY-5445
N-(3-chlorophenyl)-4-phenylphthalazin-1-amine |
PDE | Metabolism |
MY-5445 (N-(3-chlorophenyl)-4-phenylphthalazin-1-amine) 是特异性的 cGMP 磷酸二酯酶 PDE5抑制剂,其 Ki=1.3 μM。它是一种 ABCG2转运蛋白调节剂,具有抗增殖活性。它能抑制人血小板凝集。 | |||
T19706 |
Ro 20-1724
Ro-20-1724,4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone,Ro20-1724 |
PDE | Metabolism |
Ro 20-1724 (4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone) 是 cAMP 特异性磷酸二酯酶抑制剂 b>(PDE4/PDE IV),其 Ki=1930 nM,具有神经保护作用。 | |||
T1096 |
Milrinone
Win 47203,米力农 |
PDE | Metabolism |
Milrinone (Win 47203) 是一种 PDE3抑制剂,也是一种强心药、血管舒张药。 | |||
T0462 |
Cilostazol
西洛他唑,OPC 21,OPC 13013 |
PDE; Autophagy | Autophagy; Metabolism |
Cilostazol (OPC 21) 是一种选择性的心血管系统中磷酸二酯酶 3 亚型PDE 3A 的抑制剂,IC50值为 0.2 μM。 | |||
T19865 |
GEBR-7b
3-环戊氧-4-甲氧基苯甲醛,3-(Cyclopentyloxy)-4-methoxybenzaldehyde |
PDE | Metabolism |
GEBR-7b (3-(Cyclopentyloxy)-4-methoxybenzaldehyde) 是一种磷酸二酯酶 4 (PDE4) 抑制剂。 | |||
T12267 |
NSP-805
|
PDE | Metabolism |
NSP-805 是一种强心剂,是一种选择性的 phosphodiesterase 3 抑制剂,具有舒张血管的作用。 | |||
T6644 |
Rolipram
SB 95952,ZK 62711,咯利普兰,(R,S)-Rolipram |
HIV Protease; Antibacterial; PDE | Metabolism; Microbiology/Virology; Proteases/Proteasome |
Rolipram (SB 95952) 是一种磷酸二酯酶 PDE4的选择性抑制剂,抑制 PDE4A,PDE4B 和 PDE4D 的 IC50分别为 3 nM,130 nM 和 240 nM。 | |||
T1265 |
Amrinone
Inamrinone,Inocor,氨力农,Wincoram |
TNF; PDE | Apoptosis; Metabolism |
Amrinone (Inocor) 是一种正性肌力血管扩张剂,是一种具有口服活性的,非糖苷和非儿茶酚胺的强心剂,也是一种选择性磷酸二酯酶 III (phosphodiesterase III) 抑制剂,能够防止环磷酸腺苷分解,从而增加环磷酸腺苷水平。 | |||
T3465L |
Vesnarinone HCl
Synonym 2,OPC-8212 HCl,Vesnarinone HCl(81840-15-5 Free base) |
Potassium Channel; Calcium Channel; PDE | Membrane transporter/Ion channel; Metabolism |
Vesnarinone HCl (OPC-8212 HCl) 是一种具有口服活性的 phosphodiesterase 3 (PDE3) 抑制剂。Vesnarinone HCl 可对钙离子和钾离子进行调节, 增加钙通量,减少钾通量。Vesnarinone HCl 是一种新的正性肌力化合物,可增强心肌收缩力,可用于心力衰竭的研究。 | |||
T5033 |
Olprinone
奥普力农,Loprinone |
PDE | Metabolism |
Olprinone (Loprinone) 是一种有效的磷酸二酯酶(PDE) 3抑制剂,对 PDE1,PDE2,PDE3,PDE4 的IC50分别为 150、100、0.35 和 14 μM,具有抗炎活性。它具有正性肌力和血管扩张作用,可用于心力衰竭的研究。 | |||
T0160 |
Anagrelide
Anagrelida,Xagrid,Anagrelidum,阿那格雷 |
PDE | Metabolism |
Anagrelide (Xagrid) 是III 型磷酸二酯酶(PDEIII)抑制剂 (IC50=36 nM),是咪唑喹唑啉衍生物。它能够抑制血小板生成,以及抗血栓形成作用,可用作血小板聚集抑制剂。 | |||
T10667 |
Calmidazolium chloride
R 24571,钙调蛋白抑制剂 |
CaMK; Autophagy | Autophagy; Neuroscience |
Calmidazolium chloride (R 24571) 是一种钙调蛋白拮抗剂,对CaM 依赖性磷酸二酯酶和钙调蛋白诱导的红细胞Ca2+转运ATP 酶活化有拮抗作用,IC50分别为0.15和0.35 μM。Calmidazolium chloride 结合CaMK 的Kd 值为3 nM。Calmidazolium chloride 在抗癌领域有研究的价值。 | |||
T1024 |
Roflumilast
罗氟司特,B9302-107,BYK 20869,APTA 2217,BY 217 |
PDE; RSV | Metabolism; Microbiology/Virology |
Roflumilast (APTA 2217) 是一种口服的长效 4 型磷酸二酯酶抑制剂 (PDE4),具有抗炎和潜在的抗肿瘤活性,作用于PDE4A1,PDEA4,PDEB1和PDEB2,IC50分别为 0.7,0.9,0.7 和 0.2 nM。 | |||
T25463 |
Griseolic acid
|
||
Griseolic acid is a cyclic adenosine 3',5'-monophosphate phosphodiesterase II inhibitor. | |||
T12391 |
PDE1-IN-3
|
Others | Others |
PDE1-IN-3 is a selective inhibitor of human phosphodiesterase 1 (PDE1). | |||
T15714 |
LAS-31180
|
Others | Others |
LAS-31180 is a phosphodiesterase 3 inhibitor. It also has positive inotropic and vasodilator properties. | |||
T12392 | PDE12-IN-3 | Others | Others |
PDE12-IN-3 is an inhibitor of phosphodiesterase 12 (PDE12) (pXC50 of 7.68),with antiviral activity. | |||
T26767 |
Benafentrine dimaleate
Benafentrine |
||
Benafentrine dimaleate is a platelet activating factor receptor (PAFR) antagonists and phosphodiesterase (PDE) 3/4 inhibitors. | |||
T69159 | AY-22,252 | ||
AY-22,252 is an inhibitor of beef heart & rat brain nucleoside-3',5'- monophosphate phosphodiesterase. | |||
T68716 | AY 17,605 | ||
AY 17,605 is an inhibitor of bovine heart and rat brain nucleoside-3',5'- monophosphate phosphodiesterase. | |||
T13310 |
VP3.15
|
Others | Others |
VP3.15 is an orally bioavailable and CNS-penetrant dual inhibitor of phosphodiesterase (PDE)7- GSK3 (IC50s: 1.59 μM and 0.88 μM for PDE7 and GSK-3). | |||
T15640 |
K134
OPC33509 |
PDE | Metabolism |
K134 is an inhibitor of phosphodiesterase 3. The IC50s of K134 for PDE3A, PDE3B, PDE5, PDE2 and PDE4 are 0.1, 0.28, 12.1, >300 and >300 μM, respectively. | |||
T32348 |
K 259-3
K2593 |
||
K 259-3 是 K 259-2 的甲酯,是钙调素依赖性环核苷酸磷酸二酯酶的抑制剂。 | |||
T69593 |
Sildenafil nitrate
|
||
Sildenafil nitrate is a selective inhibitor of PDE5 (type 5 cGMP phosphodiesterase) which catalyzes the hydrolysis of 3',5'-cyclic guanosine monophosphate (cGMP). | |||
T61208 | PDE4-IN-11 | ||
PDE4-IN-11 is a potent phosphodiesterase isoenzyme 4 (PDE4) inhibitor, exhibiting remarkable bronchodilatory and anti-inflammatory characteristics. It is specifically designed for studying obstructive or inflammatory airway diseases [1] [2] [3]. | |||
T40356 |
PDE4-IN-3
PDE4-IN-3 |
||
PDE4-IN-3 is a newly developed oral compound that acts as a potent inhibitor of the enzyme phosphodiesterase 4 (PDE4), displaying a high affinity for inhibition with an IC50 value of 4.2 nM. | |||
T32156 |
Indimilast
|
||
Indimilast is used to inhibit phosphodiesterase IV that regulates lung inflammation and causes bronchiectasis by increasing intracellular cyclic adenosine 3', 5'-monophosphate in airway smooth muscle and inflammatory cells. Potential to treat chronic obst | |||
T60417 | Fenspiride | ||
Fenspiride 是 H1-组胺受体的拮抗剂。 Fenspiride 是一种具有口服活性的非甾体类抗炎药,可用于治疗呼吸道感染和中耳炎。 Fenspiride 抑制磷酸二酯酶 4 和磷酸二酯酶 3 的活性,-logIC50 值分别为 4.16+/-0.09 和 3.44+/-0.12。 磷酸二酯酶 5 活性也受到抑制,-logIC50 值约为 3.8。 | |||
T69491 |
(E/Z)-Ensifentrine
|
||
(E/Z)-Ensifentrine is a potent and selective PDE3/4 inhibitor. (E/Z)-Ensifentrine acts as a long-acting inhibitor of the phosphodiesterase enzymes PDE-3 and PDE-4, producing both bronchodilator and antiinflammatory effects. It is being developed by Verona Pharma as a potential treatment for asthma and hay fever, and is currently in clinical trials. | |||
T78559 | PDE7-IN-3 | ||
PDE7-IN-3(例2)是一种具有潜在镇痛活性的PDE7磷酸二酯酶抑制剂,可用于探究炎性、神经性、内脏性及伤害性疼痛。 | |||
T69262 | ABE171 | ||
ABE171, also known as NVP-ABE171, is a potent and novel phosphodiesterase 4 inhibitor with anti-inflammatory activities. NVP-ABE171 inhibited the activity of phosphodiesterase 4A, 4B, 4C, and 4D with respective IC(50) values of 602, 34, 1230, and 1.5 nM. In human cells, NVP-ABE171 inhibited the eosinophil and neutrophil oxidative burst, the release of cytokines by T cells, and the tumor necrosis factor-alpha release from monocytes, in the nanomolar range. NVP-ABE171 inhibited the airway neutrop... | |||
T36133 |
3,3'-((2-Chlorophenyl)methylene)bis(4-hydroxy-2H-chromen-2-one)
|
||
3,3'-((2-Chlorophenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) is a non-nucleotide inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1; Ki = 50 μM).1,2 It also inhibits urease (IC50 = 84.53 μM for the Jack bean enzyme).3 |1. Choudhary, M.I., Fatima, N., Khan, K.M., et al. New biscoumarin derivatives-cytotoxicity and enzyme inhibitory activities. Bioorg. Med. Chem. 14(23), 8066-8072 (2006).|2. Onyedibe, K.I., Wang, M., and Sintim, H.O. ENPP1, an old enzyme with new functions, ... | |||
T36547 |
Quazinone
|
||
Quazinone is a selective inhibitor of phosphodiesterase 3 (PDE3) with positive inotropic and vasodilating properties.1,2 It induces relaxation of precontracted isolated human cavernous smooth muscle (IC50 = 4.2 μM).1 Quazinone (10-300 μg/kg) increases myocardial contractile force in anesthetized open-chest dogs in a dose-dependent manner, as well as decreases systolic and diastolic blood pressure.2 It also inhibits DNA synthesis induced by the PDGF isoform PDGF-BB in bovine coronary artery smoot... | |||
T76138 | Phosphodiesterase | ||
Phosphodiesterase(PDE) 是一种可以催化环核苷酸3 '环磷酸键水解的酶,常用于生化研究。Phosphodiesterase 可作为第二信使分子 cAMP 和 cGMP 介导的信号转导的重要调节因子。根据其对环核苷酸的特异性也可以分别不同类型,如 PDE1-PDE11,在多种疾病方面也具有一定的潜力。 | |||
T82989 |
AP-C6
|
||
AP-C6 是一种有效的 cGMP 依赖性蛋白激酶 II (cGKII) 抑制剂,其 pIC50 值为 6.5。该化合物能够在体外浓度依赖性地抑制人 cGKII 的活性,并能够通过抑制 PDE 来增强 cAMP 信号传导。 | |||
T5033L |
Olprinone Hydrochloride
|
||
Olprinone (Loprinone) Hydrochloride 是一种有效的磷酸二酯酶(PDE) 3抑制剂,对 PDE1,PDE2,PDE3,PDE4 的IC50分别为 150、100、0.35 和 14 μM。Olprinone Hydrochloride 由于具有正性肌力和血管扩张作用而被用于心力衰竭的研究。Olprinone Hydrochloride 具有抗炎活性。 | |||
T75790 |
CALP2 TFA
|
||
CALP2 TFA 是一种钙调蛋白 (CaM) 拮抗剂 (Kd 为 7.9 µM),以亲和力结合CaMEF-hand/Ca2+结合位点。CALP2 TFA 抑制CaM 依赖性磷酸二酯酶 (phosphodiesterase) 活性并增加细胞内 Ca2+浓度。CALP2 TFA 有效抑制粘附和脱粒。CALP2 TFA 还是肺泡巨噬细胞的强激活剂。 | |||
T73708 |
Sp-cAMPS triethylamine
|
||
Sp-cAMPS triethylamine,一种 cAMP 类似物,是一种依赖 cAMP 的PKAI 和PKAII 的有效激活剂。Sp-cAMPS triethylamine 还是一种有效的竞争性磷酸二酯酶 (PDE3A) 抑制剂,Ki 为 47.6 µM。Sp-cAMPS triethylamine 以EC50为 40 μM 来结合PDE10GAF 域。 | |||
T75791 |
CALP1 TFA
|
||
CALP1 TFA 是一种钙调蛋白 (CaM) 激动剂 (Kd 为 88 µM),与 CaMEF-hand/Ca2+结合位点结合。CALP1 TFA 通过抑制钙通道 (calcium channel) 的开放来阻止钙的流入和凋亡 (IC50为 44.78 µM)。CALP1 TFA 阻止谷氨酸受体 (glutamate receptor channels) 通道,并阻止存储操作的非选择性阳离子通道。CALP1 TFA 激活 CaM 依赖性磷酸二酯酶 (phosphodiesterase) 活性。 | |||
T63776 | PDE1-IN-4 | ||
PDE1-IN-4 是有效的、选择性的 PDE1 (磷酸二酯酶 -1) 抑制剂,能够作用于 PDE1C (IC50: 10 nM)、PDE1A (IC50: 145 nM) 和 PDE1B (IC50: 354 nM)。PDE1-IN-4 能够调控 cAMP (3′,5′- 环磷酸腺苷) 和 cGMP (3′,5′- 环磷酸鸟苷),表现出抗纤维化效果。PDE1-IN-4 能够抑制 TGF-β1 诱导的人肺成纤维细胞分化。PDE1-IN-4 能够用于研究特发性肺纤维化 (IPF)。 | |||
T21697 |
Sp-Cyclic AMPS (sodium salt)
|
||
Sp-cAMPS sodium salt 作为 cAMP 类似物,是一种依赖 cAMP 的PKA I 和PKA II 的有效激活剂。Sp-cAMPS sodium salt 还是一种有效的竞争性磷酸二酯酶 (PDE3A) 抑制剂,Ki 为 47.6 μM。Sp-cAMPS sodium salt 结合PDE10 GAF 结构域,EC50为 40 μM 。 | |||
T37832 |
CAY10761
CAY10761 |
||
CAY10761 is an inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1; IC50s = 467 and 429 μM for the human and snake venom enzymes, respectively).1,2 It also inhibits mushroom tyrosinase (Ki = 1.9 μM) and urease from jack bean, P. mirabilis, and B. pasteurii (IC50s = 0.093, <0.125, and 0.089 mM, respectively, at pH 8.2).3,4 |1. Khan, K.M., Fatima, N., Rasheed, M., et al. 1,3,4-Oxadiazole-2(3H)-thione and its analogues: A new class of non-competitive nucleotide pyrophosphatases/p... | |||
T35929 |
O-Demethyl Apremilast
|
||
O-Demethyl apremilast is an active metabolite of the phosphodiesterase 4 (PDE4) inhibitor apremilast .1It inhibits the activity of PDE4 isolated from U937 cells and LPS-induced TNF-α production in isolated human peripheral blood mononuclear cells (PBMCs; IC50s = 8.3 and 5.6 μM, respectively). O-Demethyl apremilast is also an oxidative degradation product of apremilast.2,3 1.Hoffmann, M., Kumar, G., Schafer, P., et al.Disposition, metabolism and mass balance of [14C]apremilast following oral admi... | |||
T60511 |
Theophylline sodium glycinate
|
||
Theophylline (1,3-Dimethylxanthine) sodium glycinate 是一种有效的磷酸二酯酶 (PDE) 抑制剂,可抑制 PDE3 活性以松弛气道平滑肌。Theophylline sodium glycinate 可用于研究哮喘和慢性阻塞性肺疾病 (COPD) 。Theophylline sodium glycinate 也是一种腺苷受体拮抗剂和组蛋白脱乙酰酶 (HDAC) 激活剂。 Theophylline sodium glycinate 通过增加 IL-10 和抑制 NF-κB 的核输入而具有抗炎活性。Theophyllin sodium glycinate 可诱导细胞凋亡。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN1266 |
3-O-Methylquercetin
|
IL Receptor; cAMP; PDE | GPCR/G Protein; Immunology/Inflammation; Metabolism |
3-O-Methylquercetin 是分离自植物Rhamnus nakaharai 的天然产物,可抑制总 cAMP 和cGMP-phosphodiesterase (PDE)。它对PDE1、PDE5、PDE 和PDE4的IC50分别是31.9 μM、86.9 μM、18.6 μM 和1.6 μM。 | |||
T17199 |
Udenafil
3-(6,7-二氢-1-甲基-7-氧代-3-丙基-1H-吡唑并[4,3-D]嘧啶-5-基)-N-[2-(1-甲基-2-吡咯烷基)乙基]-4-丙氧基苯磺酰胺,乌地那非 |
PDE | Metabolism |
Udenafil 是一种选择性的,有效的,具有口服活性的 5 型磷酸二酯酶 (PDE5) 抑制剂。它能够抑制 cGMP 水解,可用于研究勃起功能障碍的。 | |||
T1083 |
Theophylline
Theo-24,1,3-Dimethylxanthine,茶碱 |
Endogenous Metabolite; HDAC; PDE; Adenosine Receptor; Autophagy | Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; GPCR/G Protein; Metabolism; Neuroscience |
Theophylline (1,3-Dimethylxanthine) 是茶中的甲基黄嘌呤衍生物,具有利尿、平滑肌松弛、支气管扩张、心脏和中枢神经系统兴奋作用。 | |||
T8787 |
Drotaverine hydrochloride
|
PDE | Metabolism |
Drotaverine hydrochloride 是磷酸二酯酶 4 (PDE4)的抑制剂,也是 L 型电压依赖钙通道(L-VDCC)的阻滞剂,可阻断3',5'-环腺苷单磷酸的降解。它在体内有抗痉挛效果,但无抗胆碱能的效果。 | |||
TN2974 |
3-O-Methylquercetin tetraacetate
|
IL Receptor; TNF; PDE | Apoptosis; Immunology/Inflammation; Metabolism |
Quercetin 3-O-methyl ether is a potent phosphodiesterase (PDE)3/4 inhibitor, it has potential for treating asthma against ovalbumin-induced airway hyperresponsiveness. | |||
TN1841 |
Kushenol A
苦参新醇 A,Leachianone E |
cAMP | GPCR/G Protein |
Kushenol A is a kind of Adenosine 3', 5'-cyclic monophosphate(cAMP)phosphodiesterase inhibitiors, it shows selective alpha-glucosidase inhibitory activity. Kushenol A and kushenol C exhibit inhibitory activity against Sodium-dependent glucose cotransporter 2(SGLT2). | |||
TN4886 | Quinovic acid 3-O-alpha-L-rhamnopyranoside | Others | Others |
Quinovic acid 3-O-alpha-L-rhamnopyranoside shows significant inhibitory activity against snake venom phosphodiesterase-I. | |||
TN4433 |
Licoarylcoumarin
|
cAMP; HIV Protease; Antifection | GPCR/G Protein; Microbiology/Virology; Proteases/Proteasome |
Licoarylcoumarin is a strong inhibitor of adenosine 3',5'-cyclic monophosphate (cAMP) phosphodiesterase. Licoarylcoumarin has antibacterial effects on the VRE strains; it has anti-HIV activity, and it has inhibitory effects on xanthine oxidase. |