MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Edelinontrine

CAS No. : 1082744-20-4

MCE 站：Edelinontrine

产品活性：Edelinontrine (PF-04447943) 是一种有效的人重组 PDE9A 抑制剂，IC₅₀ 为 12 nM，比作用于其他PDE家族成员选择性高 78 倍 (IC₅₀>1000 nM)。是是

研究领域：Metabolic Enzyme/Protease

作用靶点：Phosphodiesterase (PDE)

In Vitro: Using recombinant human, rhesus, ａnd rat PDE9A2 in a cell free assay Edelinontrine is shown to have a K_i of 2.8±0.26, 4.5±0.13, ａnd 18.1±1.9 nM (n=4, 11 ａnd 9 respectively). Edelinontrine is found to be highly selective over other PDE enzymes (PDE1, K_i=8600±2121 nM, n = 5; PDE2A3, K_i>99,000 nM; PDE3A, K_i>50,000 nM; PDE4A, K_i>29,000 nM; PDE5A, K_i=14,980±5025 nM, n=5; PDE6C, K_i=5324±2612 nM, n=4; PDE7A2, K_i>75,000 nM; PDE8A, K_i>50,000 nM; PDE10, K_i>51,250±20,056 nM, n=4; PDE11, K_i>80,000 nM) ａnd no other significant activity at ~60 other receptors/enzymes. In HEK whole cells expressing rhesus PDE9A2, Edelinontrine inhibits ANP (0.3 μM) stimulated cGMP with an IC₅₀ of 375±36.9 nM (n=16).

In Vivo: Based on i.v. ａnd p.o. dosing, pharmacokinetic studies with Edelinontrine in the rat indicates a T_max of 0.3 h, T_1/2 of 4.9 h, Cl of 21.7 mL/min/kg ａnd an oral bioavailability of 47%. Thirty minutes following oral administration in rats (1-30 mg/kg), Edelinontrine concentrations dose-dependently increase in blood, brain ａnd cerebrospinal fluid (CSF). The brain:plasma exposure ratios 30 min after dosing range from 0.13 at the 1 mg/kg dose to 0.33 at the 30 mg/kg dose. CSF levels are approximately 50% of brain levels. In mice, Edelinontrine (3, 10, 30 mg/kg p.o.) dose-dependently increases plasma ａnd brain concentrations of Edelinontrine while the brain to plasma ratio ranged from 0.26 to 0.7 although this is not entirely dose dependent. CSF cGMP levels increase in a dose-dependent manner from a basal level of 3 pmol/mL to 13.3 pmol/mL (3.5-fold) at the 30 mg/kg dose. CSF cGMP levels also increase in a dose-dependent manner from a basal level of 3 pmol/mL in vehicle treated animals to 13.3 pmol/mL (3.5-fold) at the 30 mg/kg dose. CSF cGMP levels are elevated at all doses tested with a maximal effect of 3.5 fold increase above controls at 30 mg/kg.

相关产品：Covalent Screening Library Plus  |  Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Metabolism/Protease Compound Library  |  Clinical Compound Library  |  Drug Repurposing Compound Library  |  Covalent Screening Library  |  Anti-COVID-19 Compound Library  |  Anti-Alzheimer＇s Disease Compound Library  |  Neurodegenerative Disease-related Compound Library  |  Targeted Diversity Library  |  Anti-Colorectal Cancer Compound Library   |  Cirsimarin  |  PDE11-IN-1  |  Enpp-1-IN-2  |  PAT-347  |  Vardenafil-d₅  |  Bay 60-7550  |  Enpp-1-IN-17  |  Deltarasin hydrochloride  |  HA155  |  Apremilast  |  Enpp-1-IN-6  |  Roflumilast  |  RS-25344 hydrochloride  |  PDE4-IN-6  |  Sp-cAMPS  |  ITI-214  |  Irsenontrine maleate  |  Lodenafil  |  Osoresnontrine  |  Deltasonamide 2  |  PF-07038124  |  Ziritaxestat  |  ATX inhibitor 22  |  Milri-d₃  |  Avanafil-¹³C,d₃  |  MT-3014  |  ATX inhibitor 19  |  Homo Sildenafil-d₅  |  Furamidine  |  PDE4-IN-12

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物  |  寡核苷酸  |  抗体  |  点击化学

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种全球独家化合物库，我们致力于为全球科研客户提供前沿*全的高品质小分子活性化合物；
•   50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。