PDE1-IN-4

PDE1-IN-4 是有效的、选择性的 PDE1 (磷酸二酯酶 -1) 抑制剂，能够作用于 PDE1C (IC50: 10 nM)、PDE1A (IC50: 145 nM) 和 PDE1B (IC50: 354 nM)。PDE1-IN-4 能够调控 cAMP (3′,5′- 环磷酸腺苷) 和 cGMP (3′,5′- 环磷酸鸟苷)，表现出抗纤维化效果。PDE1-IN-4 能够抑制 TGF-β1 诱导的人肺成纤维细胞分化。PDE1-IN-4 能够用于研究特发性肺纤维化 (IPF)。

GPD-1116 是一种口服活性的PDE4和PDE1磷酸二酯酶抑制剂，能有效减少烟雾导致的肺细胞凋亡。此化合物在多种动物疾病模型中显示出疗效，如肺气肿、急性肺损伤、慢性阻塞性肺病 (COPD)、哮喘及肺动脉高压。

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 patients with lung cancer). It is selective for these phosphodiesterases over PDE1 and PDE2, where it provides less than 25% inhibition. Fenspiride potentiates the airway relaxant effects of isoproterenol and sodium nitroprusside indicating an effect on cAMP and cGMP phosphodiesterases, respectively. Aerosolized fenspiride (1 mg ml) reverses bronchoconstriction induced by capsaicin and, when used at aerosolized concentrations ranging from 1-10 mg ml, reduces cough induced by citric aci......

Vardenafil-d5 是 Vardenafil 的氘代化合物。Vardenafil 的 CAS 号为 224785-90-4。Vardenafil 是选择性、高效的、具有口服活性的磷酸二酯酶5抑制剂，IC50=0.7 nM。它能够非竞争性地抑制环磷酸鸟苷水解，从而提高 cGMP 水平。它对 PDE1 (180 nM)，PDE6 (11 nM)，PDE2，PDE3，PDE4 (>1000 nM) 具有选择性。它可用于研究勃起功能障碍。