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Search Results for " phosphodiesterase 4 inhibitor "

57

抑制剂 & 化合物

9

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。
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)。
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。
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。
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。
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。
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。
T63056	Dovramilast CC-11050	PDE	Metabolism
	Dovramilast (CC-11050) 是一种具有口服活性的磷酸二酯酶4(PDE4)抑制剂，，可以减少促炎介质和细胞因子的产生。Dovramilast 可用于研究结核分枝杆菌感染和红斑狼疮。
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。
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.
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.
T26132	RS 14203 RS-14203,RS14203
	RS 14203 is a selective type 4 phosphodiesterase (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.
T11810	L791943	Others	Others
	L791943 is a selective, potent) inhibitor of Phosphodiesterase-4 (PDE4,IC50 of 4.2 nM).
T27557	HT-0712 IPL455903,IPL-455903,IPL 455903,HT0712
	HT-0712是一种磷酸二酯酶4 （PDE4）抑制剂。
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.
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).
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.
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].
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.
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。
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).
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。
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.
T79624	PDE4-IN-14
	PDE4-IN-14 (化合物1)是PDE4抑制剂，适用于研究与PDE4关联的疾病（例如炎症性和免疫性疾病、癌症及代谢性疾病等）。
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, ...
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.
TMIH-0190	Difamilast-d5
	Difamilast-d5 是 Difamilast 的氘代化合物。Difamilast 的 CAS 号为 937782-05-3。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。
T60920	PDE4-IN-8
	PDE4-IN-8 (Example 5) 是磷酸二酯酶4(PDE4)的有效抑制剂。PDE4-IN-8 对 PDE4B2 的 IC50值为 0.93 nM。然而，PDE4-IN-8 对 IL13、IL4、IFNy 的抑制作用微弱，IC50值分别为 4.04 nM, 36.33 nM, 2394 nM。
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...

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: T4285

Synonym: 克立硼罗,AN-2728,PF-06930164

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: T67815

Target: PDE

Cat.No: T31792

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

Target: PDE

RS-25344 hydrochloride

Cat.No: T23256

Target: PDE

Cat.No: T39341

Target: PDE

Cat.No: T9239

Target: PDE

Cat.No: T10201

Target: PDE

Cat.No: T63056

Synonym: CC-11050

Target: PDE

Cat.No: T38625

Synonym: CHF-6001

Target: PDE

Cat.No: T16379

Synonym: GRC 3886

Target: PDE

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: T19824

Synonym: Drotaverine Hydrochloride

Cat.No: T24772

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

MK-0359 besylate

Cat.No: T69399

Cat.No: T26132

Synonym: RS-14203,RS14203

Apremilast, (+/-)-

Cat.No: T21043

Synonym: Apremilast (+/-)-,

Cat.No: T11810

Target: Others

Cat.No: T27557

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

Cat.No: T62988

Cat.No: T70925

Cat.No: T38944

Synonym: OPC-6535,Tetomilast

GSK256066 Trifluoroacetate

Cat.No: T11483

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

Target: PDE

Cat.No: T15766

Synonym: BAY 19-8004

Target: PDE

Cat.No: T61208

Cat.No: T40356

Synonym: PDE4-IN-3

(E/Z)-Ensifentrine

Cat.No: T69491

Cat.No: T62367

Cat.No: T79538

Cat.No: T73240

Cat.No: T71561

Cat.No: T79624

3,3'-((2-Chlorophenyl)methylene)bis(4-hydroxy-2H-chromen-2-one)

Cat.No: T36133

EHNA hydrochloride

Cat.No: T11168

Target: Others

Cat.No: TMIH-0190

Cat.No: T60920

Cat.No: T69262

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。
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.
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.
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
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: T28019

Synonym: Mesembrin,Mesembrine,Mesembranone

3-O-Methylquercetin tetraacetate

Cat.No: TN2974

Target: IL Receptor, TNF, PDE

Cat.No: TN3537

Target: IL Receptor, TNF, NF-κB

1,3,5-Trihydroxy-4-prenylxanthone

Cat.No: T4700

Cat.No: T75486

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