PF-05180999 - Phosphodiesterase (PDE) 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPF-05180999Cat. No.: HY-111371CAS No.: 1394033-54-5分式: CHFN分量: 414.39作靶点: Phosphodiesterase (PDE)作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (120.

2、66 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.4132 mL 12.0659 mL 24.1319 mL5 mM 0.4826 mL 2.4132 mL 4.8264 mL10 mM 0.2413 mL 1.2066 mL 2.4132 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄

3、清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.58 mg/mL (6.23 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.58 mg/mL (6.23 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.58 m

4、g/mL (6.23 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 PF-05180999种磷酸酯酶 2A (PDE2A) 抑制剂，IC50 值为 1.6 nM。IC50 & Target PDE2A PDE10A1 PDE11A4 PDE7B1.6 nM (IC50) 2.03 M (IC50) 26.969 M (IC50) 50.09 M (IC50)体外研究 PF-05180999 is a phosphodiesterase 2A (PDE2A) i

5、nhibitor, with an IC50 of 1.6 nM. PF-05180999 binds tothe rat, dog and monkey PDE2A, with Kis of 4.2, 8.4, and 5.5 nM and IC50s of 2.6, 5.2, and 3.4 nM,respectively. PF-05180999 shows weak activity against PDE, with IC50s of 2.03 M (PDE10A1), 26.969 M(PDE7B), 50.09 M (PDE11A4), and 56.25 M (PDE1B1,

6、PDE3A1, PDE4D3, PDE5A1, PDE6 (bovine),PDE8B, PDE9A1), respectively. PF-05180999 is also a weak inducer of CYP3A4, and with no directinhibition of human recombinant cytochrome P450 (CYP) enzymes (1A2, 2B6, 2C8, 2C9, 2C19, 2D6, and3A) and no induction of CYP1A2 1.体内研究 PF-05180999 (Compound 30; 0.032-0

7、.32 mg/kg mg/kg, s.c.) dramatically reduces the working memoryerrors produced by ketamine in a working memory radial arm maze (RAM) model in rats. PF-05180999causes acute and exposure-dependent elevation in the accumulation of cGMP bulk levels in the cortex,striatum, and hippocampus, but with no cha

8、nges in cAMP and the associated downstream phospho-cAMPresponse element-binding protein (p-CREB) in mice 1.PROTOCOLAnimal Rats 1Administration 1 Male Sprague-Dawley rats (weighing 250-320 g) under urethane anesthesia at 1.5 g/kg intraperitoneal (ip)are placed in a stereotaxic frame, where craniotomi

9、es are performed above the region of the medialprefrontal cortex (mPFC) and ipsilateral (CA)1/subiculum. Body temperature of the rat is maintained at 37Cwith an electrical heating pad. The femoral vein is cannulated for administration of test drugs (PF-05180999,etc.). After the conclusion of the exp

10、eriments animals are euthanized with an iv bolus of urethane 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Helal CJ, et al. Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate. JMed Chem. 2018 Feb 8;61(3):1001-1018.McePdfHeightCaution: Product has not been fully va