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Search Results for " phosphodiesterase-4 "

65

抑制剂 & 化合物

11

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T36018	Phosphodiesterase 4 Inhibitor
	Phosphodiesterase 4 (PDE4) inhibitor is an inhibitor of PDE4 with an IC50 value of 0.10 μM for the human recombinant enzyme.
T27172	Difamilast	PDE	Metabolism
	Difamilast 是局部的、选择性的非甾体磷酸二酯酶 4 抑制剂，对 B 亚型抑制作用较好 (IC50=11.2 nM)。它在研究轻度至中度特应性皮炎方面有研究的价值。
T7954	YM976	PDE	Metabolism
	YM976 是磷酸二酯酶 4 抑制剂(IC50:2.2 nM)。它能够抑制抗原诱导的气道反应，并有抗炎的作用。
T2923	Apremilast 阿普斯特,CC-10004,阿普司特	Apoptosis; TNF; PDE	Apoptosis; Metabolism
	Apremilast (CC-10004) 是一种口服有效的磷酸二酯酶 4 抑制剂，IC50为 74 nM。它抑制脂多糖释放TNF-α，IC50为 104 nM。
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。
T33422	MK-0873 MK 0873,MK0873	PDE	Metabolism
	MK-0873 是一种新型且有效的选择性磷酸二酯酶 4 (PDE4) 抑制剂。
T4695	CP671305	PDE	Metabolism
	CP671305 是口服具有活力的 phosphodiesterase-4-D 选择性抑制剂，具有很高的活性。
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。
T3987	Lotamilast E6005,RVT-501	PDE	Metabolism
	Lotamilast (RVT-501) 是一种磷酸二酯酶4(PDE4) 选择性抑制剂，IC50=2.8 nM。
T30232	AWD 12-281 GSK 842470,GSK-842470,AWD12-281,AWD-12-281,GW 842470	PDE	Metabolism
	AWD 12-281 是一种选择性磷酸二酯酶 4 (PDE4) 抑制剂，具有抗炎活性和支气管扩张活性，用于研究慢性阻塞性肺疾病（COPD）。
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。
T27475	GSK356278 GSK-356278,GSK 356278	PDE	Metabolism
	GSK356278 是一种有效的特异性磷酸二酯酶 4 (PDE4) 抑制剂，对人 PDE4A、PDE4B 和 PDE4D 的 pIC50 分别为 8.6、8.8 和 8.7。 GSK356278 具有抗炎、抗焦虑和增强认知的作用。
T4285	Crisaborole 克立硼罗,AN-2728,PF-06930164	PDE	Metabolism
	Crisaborole (AN-2728) 是一种有效的 PDE4和 cytokine 释放抑制剂，能够抑制 PDE4(IC50=0.49 μM)。
T67815	uk-50001	PDE	Metabolism
	uk-50001是一种磷酸二酯酶(PDE4) 4抑制剂，可用于许多疾病，特别是炎症、过敏、呼吸系统疾病、失调和病症以及伤口。
T12103	MR-L2	PDE	Metabolism
	MR-L2 是可逆的、非竞争性的长型异构体磷酸二酯酶 -4激活剂，可以激活代表性的 PDE4 长型异构体 (PDE4A4、PDE4B1、PDE4C3、PDE4D5)。它可抑制 PGE2- 诱导的 MDCK 细胞囊肿形成，其EC50=1.2 µM。
T23256	RS-25344 hydrochloride	PDE	Metabolism
	RS 25344 hydrochloride 是 cAMP-磷酸二酯酶 4 的选择性抑制剂，在人淋巴细胞中的 IC50为 0.28 nM，对 PDE I、II、III 仅具有微弱的抑制作用，IC50分别为 >100 μM、160 μM、330 μM。它具有抗炎、增强记忆力和认知能力以及抗肿瘤活性。
T31792	Filaminast UNII-CDD69JC61J,Way-pda-641,WAY-PDA 641,CDD69JC61J	PDE	Metabolism
	Filaminast (UNII-CDD69JC61J) 是磷酸二酯酶4抑制剂(PDE4抑制剂)和罗利普兰的类似物，罗利普兰被用作抗哮喘药物。
T39341	FCPR03	PDE	Metabolism
	FCPR03 是一种特异性磷酸二酯酶 4 (PDE4) 抑制剂，对 PDE4B1、PDE4D7 和 PDE4 催化结构域的 IC50 分别为 31 nM、47 nM 和 60 nM。 FCPR03 具有神经保护、抗炎和抗抑郁样作用。
T9239	RS-25344	PDE	Metabolism
	RS-25344 是一种有效的选择性磷酸二酯酶 (PDE) 4 抑制剂。它在体外抑制嗜酸性粒细胞趋化性并增加精子的进行性运动。
T10201	PDE IV-IN-1	PDE	Metabolism
	PDE IV-IN-1 是一种有效的磷酸二酯酶4 (PDE4)抑制剂，具有抗炎活性，可用于治疗哮喘，慢性阻塞性肺病和其他炎症性疾病，是研究抑郁症的潜在化合物。
T38625	Tanimilast CHF-6001	PDE	Metabolism
	Tanimilast (CHF-6001) 是一种新型的高效选择性磷酸二酯酶 4 抑制剂，IC 50值为0.026 ± 0.006 nM。Tanimilast 具有强大的抗炎活性，适用于肺部局部用药。Tanimilast 用于研究阻塞性肺病。
T16379	Oglemilast GRC 3886	PDE	Metabolism
	Oglemilast (GRC 3886) 是一种具有口服活性磷酸二酯酶 4 (PDE4) 抑制剂，对 PDE4D3 的 IC50 为 0.5 nM。Oglemilast 在体外和体内抑制肺细胞浸润，包括嗜酸性粒细胞增多和嗜中性粒细胞减少。Oglemilast 具有应用于炎症性气道疾病的潜力。
T63056	Dovramilast
	Dovramilast (CC-11050) 是一种口服具有活力的磷酸二酯酶 4 (PDE4) 抑制剂，可以降低炎症反应，改善 INH 介导的肺部细菌清除。Dovramilast (CC-11050) 能够作为辅助试剂，用于研究结核病。
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。
T24382	L-826141 L826141,L826,141,L 826141,L-826,141,L 826,141
	L-826141 is an inhibitor of phosphodiesterase 4.
T28969	THPP-4
	THPP-4 inhibits phosphodiesterase 10A (PDE10A).
T19824	Drotaverine Drotaverine Hydrochloride
	Drotaverine Hydrochloride is a selective inhibitor of phosphodiesterase 4.
T24772	SCH-351591 SCH351591,SCH 351591,D4396,D 4396,D-4396
	SCH-351591 is an orally active inhibitor of phosphodiesterase 4.
T69399	MK-0359 besylate
	MK-0359 besylate is a Phosphodiesterase-4 (PDE4) inhibitor.
T21043	Apremilast, (+/-)- Apremilast (+/-)-,
	Apremilast, (+/-)-, is a small molecule inhibitor of phosphodiesterase 4 (PDE4) with oral activity. It is used to treat psoriatic arthritis.
T26767	Benafentrine dimaleate Benafentrine
	Benafentrine dimaleate is a platelet activating factor receptor (PAFR) antagonists and phosphodiesterase (PDE) 3/4 inhibitors.
T26132	RS 14203 RS-14203,RS14203
	RS 14203 is a selective type 4 phosphodiesterase (PDE4) inhibitor.
T27557	HT-0712 IPL455903,IPL-455903,IPL 455903,HT0712
	HT-0712是一种磷酸二酯酶4 （PDE4）抑制剂。
T11810	L791943	Others	Others
	L791943 is a selective, potent) inhibitor of Phosphodiesterase-4 (PDE4,IC50 of 4.2 nM).
T62988	Mufemilast
	Mufemilast 是一种磷酸二酯酶 4(PDE4) 的抑制剂。
T70925	GS-5759
	GS-5759 is a bifunctional ß2-Adrenoceptor Agonist and Phosphodiesterase 4 Inhibitor for Chronic Obstructive Pulmonary Disease with a Unique Mode of Action.
T11483	GSK256066 Trifluoroacetate GSK 256066 Trifluoroacetate,GSK256066 (2,2,2-trifluoroacetic acid)	PDE	Metabolism
	GSK 256066 Trifluoroacetate is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor (IC50: 3.2 pM for PDE4B). It can be used for the treatment of chronic obstructive pulmonary disease.
T38944	Tetomilast OPC-6535,Tetomilast
	Tetomilast (OPC-6535) is a phosphodiesterase-4 (PDE4) inhibitor, potentially effective in treating inflammatory bowel disease (IBD) and chronic obstructive pulmonary disease (COPD).
T15766	Lirimilast BAY 19-8004	PDE	Metabolism
	Lirimilast is an effective, selective, and orally active phosphodiesterase-4 (PDE4) inhibitor (IC50: 49 nM). Lirimilast has potently anti-inflammatory properties. Lirimilast can be used for the treatment of asthma or chronic obstructive pulmonary disease.
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].
T62367	Enpp-1-IN-4
	Enpp-1-IN-4 是一种有效的外核苷酸焦磷酸酶-磷酸二酯酶 1 (enpp-1) 抑制剂。Enpp-1-IN-4 具有潜力进行癌症疾病的研究。
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.
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.
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。
T79538	PDE4-IN-13
	PDE4-IN-13 is a phosphodiesterase 4 inhibitor with an IC50 value of 1.56 μM, exhibiting anti-inflammatory and antioxidative properties. It is utilized in the study of chronic obstructive pulmonary disease (COPD).
T69223	CC-1088
	CC-1088 is an analog of thalidomide with potential antineoplastic activity that belongs to the functional class of agents called selective cytokine inhibitory drugs (SelCIDs). SelCIDs inhibit phosphodiesterase-4 (PDE 4), an enzyme involved in tumor necrosis factor alpha (TNF alpha) production. CC-1088 inhibits production of the cytokines vascular endothelial growth factor (VEGF) (a pro-angiogenic factor) and interleukin-6 (IL-6).
T71561	LEO-29102
	LEO-29102 is a potent, selective, and soft-drug phosphodiesterase 4 (PDE4) inhibitor, which may be potentially useful for treatment of dermatological diseases. LEO 29102 shows properties suitable for patient-friendly formulations giving efficient drug delivery to the skin. LEO-29102 has reached phase 2 and demonstrated clinically relevant efficacy in the treatment of atopic dermatitis.
T73240	PDE5-IN-4
	PDE5-IN-4为磷酸二酯酶5（PDE5）抑制剂，应用于急性心肌梗死及再灌注损伤、消化系统疾病、糖尿病相关损害及肝功能衰竭的研究。
T11168	EHNA hydrochloride	Others	Others
	EHNA hydrochloride play roles in mediating diverse pharmacological responses, including antiviral, antitumour and antiarrhythmic effects. EHNA hydrochloride is a potent and selective dual inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2)(IC50=4 μM) and adenosine deaminase (ADA). EHNA hydrochloride exerts a concentration inhibition of the cGMP-stimulated PDE II (cGs-PDE)(IC50:0.8 μM (human), 2 μM (porcine myocardium)), but has smaller inhibitory effect on the unstimulated PDE2 activity.

化合物

Phosphodiesterase 4 Inhibitor

Cat.No: T36018

Cat.No: T27172

Target: PDE

Cat.No: T7954

Target: PDE

Cat.No: T2923

Synonym: 阿普斯特,CC-10004,阿普司特

Target: Apoptosis, TNF, PDE

Cat.No: T16164

Synonym: N-(3-chlorophenyl)-4-phenylphthalazin-1-amine

Target: PDE

Cat.No: T19706

Synonym: Ro-20-1724,4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone,Ro20-1724

Target: PDE

Cat.No: T33422

Synonym: MK 0873,MK0873

Target: PDE

Cat.No: T4695

Target: PDE

Cat.No: T19865

Synonym: 3-环戊氧-4-甲氧基苯甲醛,3-(Cyclopentyloxy)-4-methoxybenzaldehyde

Target: PDE

Cat.No: T3987

Synonym: E6005,RVT-501

Target: PDE

Cat.No: T30232

Synonym: GSK 842470,GSK-842470,AWD12-281,AWD-12-281,GW 842470

Target: PDE

Cat.No: T6644

Synonym: SB 95952,ZK 62711,咯利普兰,(R,S)-Rolipram

Target: HIV Protease, Antibacterial, PDE

Cat.No: T27475

Synonym: GSK-356278,GSK 356278

Target: PDE

Cat.No: T4285

Synonym: 克立硼罗,AN-2728,PF-06930164

Target: PDE

Cat.No: T67815

Target: PDE

Cat.No: T12103

Target: PDE

RS-25344 hydrochloride

Cat.No: T23256

Target: PDE

Cat.No: T31792

Synonym: UNII-CDD69JC61J,Way-pda-641,WAY-PDA 641,CDD69JC61J

Target: PDE

Cat.No: T39341

Target: PDE

Cat.No: T9239

Target: PDE

Cat.No: T10201

Target: PDE

Cat.No: T38625

Synonym: CHF-6001

Target: PDE

Cat.No: T16379

Synonym: GRC 3886

Target: PDE

Cat.No: T63056

Cat.No: T1024

Synonym: 罗氟司特,B9302-107,BYK 20869,APTA 2217,BY 217

Target: PDE, RSV

Cat.No: T24382

Synonym: L826141,L826,141,L 826141,L-826,141,L 826,141

Cat.No: T28969

Cat.No: T19824

Synonym: Drotaverine Hydrochloride

Cat.No: T24772

Synonym: SCH351591,SCH 351591,D4396,D 4396,D-4396

MK-0359 besylate

Cat.No: T69399

Apremilast, (+/-)-

Cat.No: T21043

Synonym: Apremilast (+/-)-,

Benafentrine dimaleate

Cat.No: T26767

Synonym: Benafentrine

Cat.No: T26132

Synonym: RS-14203,RS14203

Cat.No: T27557

Synonym: IPL455903,IPL-455903,IPL 455903,HT0712

Cat.No: T11810

Target: Others

Cat.No: T62988

Cat.No: T70925

GSK256066 Trifluoroacetate

Cat.No: T11483

Synonym: GSK 256066 Trifluoroacetate,GSK256066 (2,2,2-trifluoroacetic acid)

Target: PDE

Cat.No: T38944

Synonym: OPC-6535,Tetomilast

Cat.No: T15766

Synonym: BAY 19-8004

Target: PDE

Cat.No: T61208

Cat.No: T62367

Cat.No: T40356

Synonym: PDE4-IN-3

(E/Z)-Ensifentrine

Cat.No: T69491

Cat.No: T60417

Cat.No: T79538

Cat.No: T69223

Cat.No: T71561

Cat.No: T73240

EHNA hydrochloride

Cat.No: T11168

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
TN2159	Robustine 大叶桉亭,8-羟基白鲜碱,4-甲氧基呋喃并[2,3-B]喹啉-8-醇	PDE	Metabolism
	Robustine 是一种从 Dictamnus albus 获得的呋喃喹啉生物碱，在体外对人磷酸二酯酶 5 (hPDE5A) 具有抑制作用。
T4S0792	Pinoresinol 4-O-β-D-glucopyranoside (+)-pinor,(+)-pinoresinol-β-D-glucoside; (+)-pinor,(+)-pinoresinol-β-D-glucoside	Others	Others
	(+)-pinoresinol-β-D-glucoside; (+)-pinor 是连翘中主要的活性呋喃类木脂素。它显示出抗氧化、降血压和环磷酸腺苷 (cAMP) 磷酸二酯酶抑制活性。
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。
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。
TN1950	Moracin M	PDE	Metabolism
	Moracin M 是桑白皮中的一种酚类成分，有效的磷酸二酯酶 4 (PDE4) 抑制剂，对于 PDE4D2，PDE4B2，PDE5A1 和 PDE9A2 的 IC50 分别为 2.9 μM，4.5 μM，> 40 μM 和 > 100 μM。Moracin M 具有抗炎活性。
T28019	(-)-Mesembrine Mesembrin,Mesembrine,Mesembranone
	Mesembrine is a serotonin reuptake inhibitor and is also a weak inhibitor of the enzyme phosphodiesterase 4 (PDE4).
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.
T79957	4'-Methoxyisoagarotetrol
	4'-Methoxyisoagarotetrol 是一种色素衍生物，表现出中等强度的PDE3A抑制活性，其半抑制浓度（IC50）为54 μM。
T4700	1,3,5-Trihydroxy-4-prenylxanthone
	1,3,5-Trihydroxy-4-prenylxanthone is a relatively potent inhibitor of phosphodiesterase type 5 (PDE5), with an IC50 value of 3.0 μM; it shows in vitro inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with IC50 valu
TN3537	Braylin	IL Receptor; TNF; NF-κB	Apoptosis; Immunology/Inflammation; NF-κB
	Braylin has anti-inflammatory, antinociceptive and immunomodulatory effects, which possibly act through the glucocorticoid receptor activation and by inhibition of the transcriptional activity of NF-ÎºB. Braylin is also a phosphodiesterase-4 inhibitor, it could represent an ideal prototype of glucocorticoid receptor ligand, able to induce synergic immunomodulatory effects.
T75486	Toddacoumalone
	Toddacoumalone 是一种天然PDE4 (磷酸二酯酶 4) 抑制剂，效力中等，活性分子特性不完善。具有研究银屑病等炎症性疾病潜力。

天然产物

Cat.No: TN2159

Synonym: 大叶桉亭,8-羟基白鲜碱,4-甲氧基呋喃并[2,3-B]喹啉-8-醇

Target: PDE

Pinoresinol 4-O-β-D-glucopyranoside

Cat.No: T4S0792

Synonym: (+)-pinor,(+)-pinoresinol-β-D-glucoside; (+)-pinor,(+)-pinoresinol-β-D-glucoside

Target: Others

Cat.No: T17199

Synonym: 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

Target: PDE

Drotaverine hydrochloride

Cat.No: T8787

Target: PDE

Cat.No: TN1950

Target: PDE

Cat.No: T28019

Synonym: Mesembrin,Mesembrine,Mesembranone

3-O-Methylquercetin tetraacetate

Cat.No: TN2974

Target: IL Receptor, TNF, PDE

4'-Methoxyisoagarotetrol

Cat.No: T79957

1,3,5-Trihydroxy-4-prenylxanthone

Cat.No: T4700

Cat.No: TN3537

Target: IL Receptor, TNF, NF-κB

Cat.No: T75486

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