pde1-in-1

PDE1-IN-1can enhance levels of the second messengers cAMP cGMP leading to the expression of neuronal plasticity-related genes, neurotrophic factors, and neuroprotective molecules. These neuronal plasticity enhancement properties make PDE1 inhibitors good candidates as therapeutic agents in many neurological conditions.

PDE1-IN-2 is an PDE1 inhibitor(PDE1C, PDE1B and PDE1A with IC50 values of 6, 140 and 164 nM, respectvely).

PDE1-IN-3 is a selective inhibitor of human phosphodiesterase 1 (PDE1).

PDE1-IN-9 (Compound 7a) 为磷酸二酯酶 1 (PDE1) 的选择性抑制剂，其可抑制PDE1C，IC50为11 nM。PDE1-IN-9 能降低IL-1β、IL-6、TNF-α 和 iNOS的mRNA表达，并抑制一氧化氮 (NO) 和活性氧 (ROS) 的产生。此外，该化合物在大鼠肝微粒体中显示出良好的代谢稳定性。

ENPP1 Inhibitor C 是一种外核苷酸焦磷酸酶 磷酸二酯酶 1（ENPP1）抑制剂，具有潜在的抗癌活性，可用于研究三阴乳腺癌。

DSR-141562 is a new compound that can be taken orally and has a specific ability to inhibit phosphodiesterase 1 (PDE1) in the brain. This compound exhibits a preference for inhibiting human PDE1B, with an IC50 value of 43.9 nM. It also shows moderate inhibition of human PDE1A (IC50 = 97.6 nM) and PDE1C (IC50 = 431.8 nM). DSR-141562 is particularly useful in the study of positive symptoms, negative symptoms, and cognitive impairments associated with schizophrenia.

Olprinone (Loprinone) Hydrochloride 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 Hydrochloride 由于具有正性肌力和血管扩张作用而被用于心力衰竭的研究。Olprinone Hydrochloride 具有抗炎活性。

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)。

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......

Phosphodiesterase(PDE) 是一种可以催化环核苷酸3 '环磷酸键水解的酶，常用于生化研究。Phosphodiesterase 可作为第二信使分子 cAMP 和 cGMP 介导的信号转导的重要调节因子。根据其对环核苷酸的特异性也可以分别不同类型，如 PDE1-PDE11，在多种疾病方面也具有一定的潜力。

PDE1-IN-5 (Compound 10c) 是一种PDE1C选择性抑制剂，IC50为15 nM。该化合物显示出抗炎活性，能够抑制LPS诱导的iNOS、TNF-α、IL-1α、IL-1β和IL-6表达。在DSS诱导的结肠炎小鼠模型中，PDE1-IN-5对抗炎性肠病(IBD)表现出治疗潜力，并可用于IBD相关研究。

PDE11A4-IN-1 (compound 23b) 是一种选择性的 PDE11A4 抑制剂，具有 12 nM 的 IC50。该化合物相对于 PDE1、PDE2、PDE7、PDE8 和 PDE9 显示出较高的选择性。

PDE1-IN-6 (compound 6c)，一种具有7.5 nM IC50值的选择性PDE1抑制剂，能显著抑制急性髓性白血病细胞的增殖并诱导凋亡 (cellapoptosis)。

PDE1-IN-7 (Compound 13h) 作为bPDE1的选择性抑制剂（IC50=10 nM），在BDL诱导的肝纤维化大鼠模型中展现了显著的抗纤维化活性。该化合物主要用于研究肝纤维化的治疗潜力。