Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8462 |
Enoximone
依诺昔酮,烯氟酮 |
PDE | Metabolism |
Enoximone 是一种选择性的,具有口服活性的磷酸二酯酶 III 抑制剂,也是正性肌力血管舒张剂。它通过抑制 cGMP 抑制的 PDE 来诱导血管舒张并增加细胞内 cAMP 水平。它还表现出 PDE4抑制作用,对心肌 PDE4A 的 IC50为 21.1 μM。它用于充血性心力衰竭的研究,并具有支气管扩张,抗哮喘和抗炎作用。 | |||
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。 | |||
T5496 |
ML-030
|
PDE | Metabolism |
ML-030 是 PDE4抑制剂,对 PDE4A (IC50=6.7 nM),PDE4A1 (IC50=12.9 nM),PDE4B1 (IC50=48.2 nM),PDE4B2 (IC50=37.2 nM),PDE4C1 (IC50=452 nM) 和 PDE4D2 (IC50=49.2 nM)。 | |||
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。 | |||
T61794 | LASSBio-1632 | ||
LASSBio-1632 is a novel anti-asthmatic lead candidate that selectively inhibits PDE4A and PDE4D isoenzymes, leading to the suppression of airway hyper-reactivity (AHR) and TNF-α production in lung tissue. With high experimental BBB permeability, LASSBio-1632 (7j) efficiently crosses the blood-brain barrier through passive diffusion [1]. | |||
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... | |||
T33947 |
PF-06445974
PF-6445974,PF6445974,PF06445974,PF 6445974 |
||
PF-06445974 has good selectivity for PDE4D, excellent brain permeability, and has a high level of specific binding in the "cold tracer" study. |