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。