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19

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T39210	PDE4-IN-4 PDE4-IN-4
	PDE4-IN-4 is a compound acting as both a potent M3 antagonist (p IC 50 = 10.2) and a PDE4 inhibitor (p IC 50 = 8.8), designed for inhalation-based treatment of pulmonary diseases.
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.
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。
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）。
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 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。
T6649	(S)-(+)-Rolipram (S)-Rolipram,(+)-Rolipram,盐酸环胞苷,S- (+)-Rolipram	Apoptosis; PDE	Apoptosis; Metabolism
	(S)-(+)-Rolipram ((+)-Rolipram) 是一种 cAMP 依赖性磷酸二酯酶 4 (PDE4) 抑制剂，IC50=1100 nM。它能够抑制人单核细胞产生的肿瘤坏死因子 α (TNFα)。
T50023	ethyl 1-(4-aminophenyl)-5-(trifluoromethyl)-1H-pyrazole-4-carboxylate	Others	Others
	ethyl 1-(4-aminophenyl)-5-(trifluoromethyl)-1H-pyrazole-4-carboxylate 又称 EAPT，是一种有效的选择性 PDE4抑制剂，调节细胞内环腺苷酸(cAMP)水平。它已被用于多种科研应用，包括 cAMP 介导的信号转导通路的研究，并有潜力作为治疗炎症和免疫相关疾病的药物。
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].
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).
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。
T22077	Eggmanone
	Eggmanone (EGM1) 是一种有效的、选择性的磷酸二酯酶 4(PDE4)拮抗剂，对 PDE4D3 的 IC50为 72 nM。Eggmanone 对 PDE4D3 的选择性大约是其他 PDE 的 40-50 倍。Eggmanone 通过选择性拮抗 PDE4 发挥 Hh 抑制作用，导致蛋白激酶 A 激活和随后的 Hh 阻断。
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）。
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).
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...
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.
T69615	AWD12-281 sodium
	AWD 12-281 is a selective phosphodiesterase 4 (PDE4) inhibitor for the treatment of lung inflammation using inhalative administration. AWD 12-281 Is Active in a New Guinea-Pig Model of Allergic Skin Inflammation Predictive of Human Skin Penetration and Suppresses Both Th1 and Th2 Cytokines in Mice. AWD 12-281 is a very promising drug candidate not only for the treatment of lung inflammation using inhalative administration but also for the treatment of atopic dermatitis.
T38002	LEO 39652
	LEO 39652 is a dual-soft PDE4 inhibitor with IC50s of 1.2 nM, 1.2 nM, 3.0 nM and 3.8 nM for PDE4A, PDE4B, PDE4C and PDE4D, respectively. LEO 39652 also inhibits TNF-α with an IC50 value of 6.0 nM. LEO 39652 is used for topical research of Atopic dermatitis (AD) [1]. LEO 39652 shows unbound in vitro potency when measured as LPS induced TNF-α release in human peripheral blood mononuclear cells (PBMC), incubated in serum free medium. LEO 39652 shows a relatively high binding to human serum albumin...
T71141	Fenspiride-d5
	Fenspiride-d5 is intended for use as an internal standard for the quantification of fenspiride by GC- or LC-MS. Fenspiride is an antagonist of histamine H1 receptors and a non-steroidal anti-inflammatory drug (NSAID). It inhibits histamine-induced contraction of isolated guinea pig trachea but not histamine-induced inotropy of isolated guinea pig heart. It also inhibits phosphodiesterase 4 (PDE4), PDE5, and PDE3 (IC50s = 69, ~158, and 363 µM, respectively, in isolated human bronchi derived from ...

化合物

Cat.No: T39210

Synonym: PDE4-IN-4

Cat.No: T40356

Synonym: PDE4-IN-3

Cat.No: T10201

Target: PDE

Cat.No: T30232

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

Target: PDE

Cat.No: T16379

Synonym: GRC 3886

Target: PDE

Cat.No: T63056

Synonym: CC-11050

Target: PDE

(S)-(+)-Rolipram

Cat.No: T6649

Synonym: (S)-Rolipram,(+)-Rolipram,盐酸环胞苷,S- (+)-Rolipram

Target: Apoptosis, PDE

ethyl 1-(4-aminophenyl)-5-(trifluoromethyl)-1H-pyrazole-4-carboxylate

Cat.No: T50023

Target: Others

Cat.No: T61208

Cat.No: T38944

Synonym: OPC-6535,Tetomilast

Cat.No: T60920

Cat.No: T22077

Cat.No: T79624

Cat.No: T79538

O-Demethyl Apremilast

Cat.No: T35929

Cat.No: T71561

AWD12-281 sodium

Cat.No: T69615

Cat.No: T38002

Cat.No: T71141

Cat. No.	Product Name	Target	Signaling Pathways
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。
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: TN1950

Target: PDE

Cat.No: T75486

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