PDE

PDE7 inhibitor S14 is a cell-permeable PDE7 inhibitor that acts by targeting the cyclic adenosine monophosphate (cAMP)/cAMP-response element-binding protein (CREB) pathway.

deacetylsclerotiorin is a new chloroazaphilones produced by the fungus Bartalinia robillardoides strain LF550.

ATI-22-107 is a positive cardiac inotropic agent which may affect myocyte calcium cycling and contractility.

CK 3197 is a selective positive inotropic agent for the treatment of congestive heart failure. It has hemodynamic and myocardial energetic effects.

MK-0359 (L454560) is a selective and effective oral PDE4 inhibitor for the treatment of chronic asthma.

β-Carboline-1-carboxylic acid is an alkaloid that has been found in P. quassioides and has diverse biological activities. It reduces LPS-induced increases in MCP-1, TNF-α, IL-6, and IL-1β levels in RAW 264.7 cells when used at a concentration of 15 µg/ml and inhibits the epithelial-to-mesenchymal transition (EMT) induced by TGF-β1 in A549 cells. β-Carboline-1-carboxylic acid induces cytotoxicity in CT26.WT, K562, and SGC-7901 cells (IC50s = 14.96, 22.11, and 19.7 µg/ml, respectively) but not HepG2 or A549 cells (IC50s = 36.41 and 41.51 µg/ml, respectively). It also inhibits cAMP phosphodiesterase with an IC50 value of 96 µM.

SAR156497 is an exquisitely selective Aurora A, B, and C inhibitor with in vitro and in vivo efficacy with IC50 = 0.5 nM (Aurora A); 1 nM (Aurora B / incenp); 3 nM (Aurora C / incenp) respectively SAR156497 combines high in vitro potency with satisfactory metabolic stability and limited CYP 3A4 and PDE3 inhibition. In vitro, SAR156497 displayed high antiproliferative activity on a large panel of tumor cell lines without correlation with any particular genetic signature or Aurora kinases expression. It induced significant modulation of Aurora A and Aurora B biomarkers (p-Aurora A and pHH3, respectively) and cell polyploidy, as expected from Aurora A/B inhibitors.

Davalomilast (Example 100) 是一种PDE4抑制剂，具有抗炎特性。Davalomilast 适用于研究自身免疫性疾病和皮肤病学。

PDE4-IN-29 (Compound 55) 是一种选择性且具口服活性的PDE4抑制剂，能有效作用于PDE4亚型如 PDE4A1、PDE4B2 和 PDE4D3，其对 PDE4D3 的IC50值低于 5 nM。该化合物可以抑制环腺苷酸 (cAMP) 的降解，从而提升细胞内的cAMP水平，抑制如 TNF-α 等炎症因子的释放。PDE4-IN-29 可能用于研究银屑病、特应性皮炎和慢性阻塞性肺疾病等炎症性疾病。

Amentoflavone hexaacetate is a 3,5-cyclic nucleotide phosphodiesterase inhibitor. It has anti-angiogenic and anti-metastatic effects.

5-HT1A/5-HT7受体拮抗剂（5-HT1A Ki=8 nM，Kb=0.04 nM；5-HT7 Ki=451 nM，Kb=460 nM）具有 PDE4B/PDE7A 抑制活性（PDE4BIC50=80.4μM；PDE7AIC50=151.3μM），其抗抑郁样作用强于作为参考活性分子的依西酞普兰。

Cipamfylline is a xanthine, a theophylline analogue, and is a potent and selective inhibitor of phosphodiesterase type 4 (PDE-4). Cipamfylline was tested in patients with a diagnosis of atopic dermatitis and in two human models of acute and chronic irritant contact dermatitis. The outcome of the study revealed that cipamfylline was more effective than vehicle in treating atopic dermatitis, but less effective than a group II steroid, hydrocortisone-17-butyrate both in the treatment of atopic dermatitis and irritant contact dermatitis. The absorption of cipamfylline and the subsequent systemic exposure might be the reason why further clinical studies with higher doses of cipamfylline have not been published.

Inamrinone lactate is a positive inotropic cardiotonic with vasodilator properties, phosphodiesterase inhibitory activity, and the ability to stimulate calcium ion influx into the cardiac cell.

Milrinone-d3是Milrinone的氘代物。Milrinone 是一种PDE3抑制剂，具有强心作用，并能扩张血管。

Apremilast (Standard) 是 Apremilast 的标准品，适用于定量分析、质量控制及生化实验等相关研究。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。

Isomazole 是一种可口服的具有钙敏特性的新型磷酸二酯酶（PDE）抑制剂，对PDE3 和 PDE4 有抑制作用。

UK 088800 是一种生物活性化学品。

2,5-dichloro-4-(difluoromethoxy)-N,N-dimethylbenzene-1-sulfonamide是一种 PDE 抑制剂。

Pterine-6-carboxylic acid (6-Carboxypterin) 是叶酸的光降解产物，可被用作光敏感剂研究UVA 破环DNA 结构的分子机制。

Acetildenafil (Hongdenafil) (Standard) 是 Acetildenafil (Hongdenafil) 的标准品，适用于定量分析、质量控制及生化实验等相关研究。Acetildenafil 是一种 phosphodiesterase 5 抑制剂 Sildenafil 衍生物。

UK 088800 (Standard) 是 UK 088800 的标准品，适用于定量分析、质量控制及生化实验等相关研究。UK 088800 是一种生物活性化学品。

Sildenafil citrate (Standard) 是 Sildenafil citrate 的标准品，适用于定量分析、质量控制及生化实验等相关研究。Sildenafil citrate (UK-92480 citrate) 是一种磷酸二酯酶 5 抑制剂，IC50为 5.22 nM。

Dasantafil (SCH446132) 是一种小分子磷酸二酯酶-5A(PDE5A)抑制剂，可用于治疗泌尿生殖系统疾病和研究勃起功能障碍。

Deltasonamide 2 is a competitive, high affinity PDEδ inhibitor with a Kd of ~385 pM.

PDE5-IN-9对Phosphodiesterase PDE1c 具有抑制作用，可用来治疗高血压、心力衰竭、心肌梗塞、肾衰竭、哮喘、支气管炎和痴呆。

Deltasonamide 2 hydrochloride is a competitive high-affinity PDEδ inhibitor with a Kd of approximately 385 pM.

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。

PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor (IC50= 22 nM).1It is selective for PDE9A over PDE1C (IC50= >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 μM but does inhibit the human dopamine transporter (DAT; Ki= 293 nM). PF-04449613 (0.1-100 mg/kg, s.c.) increases cerebrospinal fluid (CSF) levels of cyclic GMP (cGMP) in rats. Subcutaneous administration of PF-04449613 (10 mg/kg) increases the rate of dendritic spine formation and elimination in mouse primary motor cortex pyramidal neuronsin vivo.2It increases the average running speed of mice in an accelerating rotarod task, indicating improved motor learning, at the same dose. 1.Claffey, M.M., Helal, C.J., Verhoest, P.R., et al.Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitorsJ. Med. Chem.55(21)9055-9068(2012) 2.Lai, B., Li, M., Hu, A., et al.The phosphodiesterase 9 inhibitor PF-04449613 promotes dendritic spine formation and performance improvement after motor learningDev. Neurobiol.78(9)859-872(2018)

PDE5-IN-3 (compound 11j) 是一种 PDE5 的有效抑制剂 (IC50: 1.57 nM)。PDE5-IN-3 对 EGFR 具有中度抑制作用 (IC50: 5.827 μM)。PDE5-IN-3 明显抑制 Wnt/β-catenin 通路，其 IC50 值为 1286.96 ng/mL。PDE5-IN-3 在 HepG2 细胞中诱导内在的凋亡线粒体途径。PDE5-IN-3 表现出显著的抗肿瘤效果。

PAT-347 is a potent Autotaxin Inhibitor. Autotaxin (ATX) is a secreted enzyme responsible for the hydrolysis of lysophosphatidylcholine (LPC) to the bioactive lysophosphatidic acid (LPA) and choline. The ATX-LPA signaling pathway is implicated in cell survival, migration, and proliferation; thus, the inhibition of ATX is a recognized therapeutic target for a number of diseases including fibrotic diseases, cancer, and inflammation, among others.

Furamidine dihydrochloride (DB75 dihydrochloride)是一种选择性的蛋白精氨酸甲基转移酶1（PRMT1）小分子抑制剂，可优先结合DNA小沟中的AT碱基对序列。Furamidine dihydrochloride主要通过与蛋白质底物竞争的方式靶向PRMT1酶活性位点（对辅因子为非竞争性抑制），在不同遗传背景的白血病细胞系中阻断细胞增殖。

C82 acts as an inhibitor of Mycobacterium tuberculosis (Mtb) cyclic dinucleotide phosphodiesterase (CdnP), with an IC50 value of 17.5 µM. This particular enzyme is responsible for breaking down cyclic di-AMP (c-di-AMP) into adenosine 5'-monophosphate (AMP). Notably, C82 demonstrates selectivity for Mtb CdnP over other bacterial cyclic dinucleotide phosphodiesterases (CDN PDEs) such as Yybt, RocR, and Group B Streptococcus (GBS) CdnP, as well as the mammalian CDN PDE ENPP1, and the viral CDN PDE poxin, showing effectiveness at a concentration of 200 µM.

FR-229934 is a bio-active chemical. Detailed information has not been published.

(R)-Apremilast ((R)-CC-10004) 是一种 Apremilast 的异构体。

ONO-8430506 是一种可口服的、具有有效性的 autotaxin (ATX)/ENPP2 抑制剂（ IC90 ：100 nM），能够抑制小鼠血浆中 ATX 活性。