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Phosphodiesterase (PDE)

Phosphodiesterase (PDE)相关产品（60）
货号 产品名 中文名称 产品描述
SJ-MX1034 Ibudilast 异丁司特

Ibudilast (KC-404, AV411, MN166) 是一种可穿过血脑屏障的、环腺苷酸磷酸二酯酶 (phosphodiesterase, PDE) 抑制剂。Ibudilast 具有抗血小板聚集作用。Ibudilast 抑制气管平滑肌收缩性，可用于哮喘的研究。Ibudilast 可能是一种有效的神经保护和抗痴呆药物，可对抗活化小胶质细胞的神经毒性。
SJ-MX0582 PF-8380

PF-8380是一种有效的、口服生物可利用的自毒素 (autotaxin, ATX)抑制剂，体外酶实验和人类全血细胞实验中，IC50 分别为 2.8 nM 和 101 nM。
SJ-MX2834 Udenafil (DA8159) 乌地那非 Udenafil (formerly known as DA8159) is a novel and potent PDE5 inhibitor used in urology to treat erectile dysfunction. It is available for use in Korea, Russia, and Philippines but not in the United States.
SJ-MX3552 ITI-214 ITI-214 is an orally bioavailable, potent and Selective Inhibitors of Phosphodiesterase 1 for the Treatment of Cognitive Impairment Associated with Neurodegenerative and Neuropsychiatric Diseases. ITI-214 exhibited picomolar inhibitory potency for PDE1, demonstrated excellent selectivity against all other PDE families, and showed good efficacy in vivo. Currently, this investigational new drug is in Phase I clinical development and being considered for the treatment of several indications including cognitive deficits associated with schizophrenia and Alzheimer's disease, movement disorders, attention deficit and hyperactivity disorders, and other CNS and non-CNS disorders.
SJ-MX3659 Ziritaxestat (GLPG1690) Ziritaxestat (GLPG1690) is a selective autotaxin inhibitor with potential application in idiopathic pulmonary disease (IPF).
SJ-MX3773 BRL-50481 BRL-50481 is a novel, potent and selective inhibitor of phosphodiesterase 7 (PDE7) with IC50s of 0.15, 12.1, 62 and 490 μM for PDE7A, PDE7B, PDE4 and PDE3, respectively.  BRL 50481 inhibited the activity of hrPDE7A1 expressed in baculovirus-infected Spodoptera frugiperda 9 cells in a competitive manner (Ki value of 180 nM) and was 416 and 1884 times less potent against PDE3 and 38 and 238 times less potent against PDE4 at a substrate concentration of 1 microM and 50 nM cAMP, respectively. Western blotting identified HSPDE7A1 but not HSPDE7A2 in three human cell types that are implicated in the pathogenesis of chronic obstructive lung disease, namely, CD8+ T-lymphocytes, monocytes, and lung macrophages. 
SJ-MX2472 Olprinone 奥普力农 Olprinone (Loprinone) 是一种有效的磷酸二酯酶 (PDE) 3 抑制剂，对 PDE1，PDE2，PDE3，PDE4 的 IC50 分别为 150、100、0.35 和 14 µM。Olprinone 因其正性肌力和血管扩张作用而被用于心力衰竭的研究。Olprinone 具有抗炎活性。
SJ-MX2690 Pimobendan 匹莫苯丹 Pimobendan (UD-CG115) is a calcium sensitizer and a selective inhibitor of phosphodiesterase III (PDE3) with positive inotropic and vasodilator effects. Pimobendan has been studied for treating heart failure and cardiomyopathy, primarily for veterinary uses.
SJ-MX2448 Zatolmilast Zatolmilast(BPN14770)是一种选择性磷酸二酯酶4D(PDE4D)变构抑制剂，对于PDE4D7与PDE4D3的IC50值分别为7.8 nM和7.4 nM.
SJ-MX1598 CP671305 CP671305 是一种有效的，可口服的，选择性的 phosphodiesterase-4-D 抑制剂，具有很高的活性。
SJ-MX4061 BAY 2666605 BAY 2666605是一种具有口服活性的磷酸二酯酶3A (phosphodiesterase 3A, PDE3A)和磷酸二酯酶3B (phosphodiesterase 3B, PDE3B)抑制剂，IC50分别为87 nM和50 nM。
SJ-MX2506 Aminophylline 氨茶碱 Aminophylline (also known as Phyllocontin; Euphyllin; Truphylline), a bronchodilator composed of theophyllineand ethylenediamine in 2:1 ratio, is a novel, potent, competitive nonselective phosphodiesterase/PDE inhibitor with an IC50 of 0.12 mM. It is also a nonselective adenosine receptor antagonist. Aminophylline is used to treat wheezing, shortness of breath, and difficulty breathing caused by asthma, chronic bronchitis, emphysema.
SJ-MX2591 Doxofylline 多索茶碱 Doxofylline (also known as Neothylline; Ansimar; ABC-1213; ALT-07; Lufyllin; DO-309; Diprophylline; Corphyllin; ABC-12-3), a xanthine derivative, is a novel and potent PDE (phosphodiesterase) inhibitor with the potential for treating asthma. Doxofylline's mechanism of action is related to the inhibition of phosphodiesterase activities, but it appears to have decreased affinities towards adenosine A1 and A2 receptors, which may account for its better safety profile.
SJ-MX2603 Amrinone 氨力农 Amrinone is a potent phosphodiesterase 3 (PDE3) inhibitor (IC50 = 19.5 µM). It increases developed tension and contractile force in isolated cat papillary muscle. It also displays positive inotropic effects, increasing the rate and force of heart contraction in anesthetized and unanesthetized dogs.
SJ-MX2852 Crisaborole (AN-2728) 克立硼罗 Crisaborole (AN-2728) is a boron-based, topical anti-inflammatory agent that acts as a phosphodiesterase 4 (PDE4) inhibitor (IC50 = 0.11 µM). It is less potent against PDE1A, PDE3A, and PDE7A (IC50s = 6.12, 6.41, and 0.73 µM, respectively). AN-2728 suppresses the release of the proinflammatory cytokines TNF-α, IL-2, INF-γ, IL-5, and IL-10 with IC50 values of 0.50, 0.59, 0.72, 2.25, and 2.58 µM, respectively.
SJ-MX2912 Avanafil(TA-1790) 阿伐那非 Avanafil (also known as TA 1790; TA1790; TA-1790; trade name: Stendra; Spedra) is a highly potent and selective PDE5 inhibitor with potential vasodilating effects. It inhibits PDE5 with an IC50 of 5.2 nM, and shows >121-fold selectivity for PDE5 over other isoforms of PDE.
SJ-MX3367 Irsogladine 伊索拉定 Irsogladine (MN1695; MN 1695; Gaslon; MN-1695; Dicloguamine), a mucosal protective drug, is a novel and potent PDE4 inhibitor and muscarinic acetylcholine receptor binder with anti-ulceric activity. It is used as an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding. Irsogladine treatment (300 and 500 mg/kg/day) resulted in a dose-dependent reduction of angiogenesis in wild-type mice by 21 and 45.3%.
SJ-MX3840 Enoximone 烯氟酮 Enoximone 是一种正性肌力血管舒张剂，也是一种选择性的，具有口服活性的磷酸二酯酶 III (PDE3) 抑制剂，IC50 为 5.9 μM。Enoximone 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。Enoximone 还表现出 PDE4 抑制作用，对心肌 PDE4A 的 IC50 为 21.1 μM。Enoximone 可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。
SJ-MX2146 Deltarasin Deltarasin 是一种 KRAS-PDEδ 相互作用的抑制剂，能够与 PDEδ 结合，Kd 值为 38 nM。
SJ-MN0199 Butein 紫铆因 Butein，一种从漆树中分离的植物多酚，可以抑制酪氨酸激酶，NF-κB，STAT3和EGFR活化。
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