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Cat. No. | Product Name | Target | Signaling Pathways |
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T39210 |
PDE4-IN-4
PDE4-IN-4 |
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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 |
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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. | |||
T79618 |
M3/PDE4 modulator-1
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M3/PDE4 modulator-1 (10f) 为多功能化合物,具备M3mAChR拮抗和PDE4抑制作用。于OVA大鼠模型中,M3/PDE4 modulator-1 (10-1000 nM/kg;iv) 能降低半胱氨酸嗜酸性粒细胞内流。 | |||
T10201 |
PDE IV-IN-1
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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 |
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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
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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
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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
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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
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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
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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
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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
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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 ... |
Cat. No. | Product Name | Target | Signaling Pathways |
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TN1950 |
Moracin M
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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
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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。 |