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Postion:Product Catalog >PF-04859989 HCl
PF-04859989 HCl
  • PF-04859989 HCl

PF-04859989 HCl NEW

Price $60 $98 $189
Package 5mg 10mg 25mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-12

Product Details

Product Name: PF-04859989 HCl CAS No.: 177943-33-8
Purity: 99.3% Supply Ability: 10g
Release date: 2024/11/12

Product Introduction

Bioactivity

名稱PF-04859989 HCl
描述PF-04859989 HCl is a brain-penetrable and irreversible inhibitor of kynurenine amino transferase II (KAT II), which is the enzyme responsible for most of the brain synthesis of kynurenic acid.
體外活性The IC50s values are 23 and 263 nM for hKAT II and rKAT II. PF-04859989 HCl is selective for KAT II over human KAT I, KAT III, and KAT IV (IC50s of 22, 11, and >50 μM, respectively)[3].
體內(nèi)活性Acute administration of the KAT II inhibitor PF-04859989 (5 or 10 mg/kg) was associated with a short-onset, time-dependent decrease in firing rate and burst activity of DA neurons, both parameters reaching a 50% reduction within 45 min. Furthermore, PF-04859989 reduced the number of spontaneously active DA cells as measured 4-6 after administration. Pretreatment with d-cycloserine (30 mg/kg) or CGP-52432 (10 mg/kg) prevented the inhibitory action of PF-04859989 (5 mg/kg) on firing rate and burst firing activity. In contrast, pretreatment with methyllycaconitine (MLA, 4 mg/kg) did not change the response, whereas picrotoxin (4.5 mg/kg) partially prevented the inhibitory effects of PF-04859989 (5 mg/kg, i.v.)[2].
存儲(chǔ)條件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 100 mg/mL (465.87 mM)
H2O : 100 mg/mL (465.87 mM)
關(guān)鍵字disorders | schizophrenia | Inhibitor | inhibit | PF04859989 HCl | midbrain | psychiatric | PF 04859989 HCl | dopamine | neurons | PF-04859989 HCl | cognitive ,impairment
相關(guān)庫(kù)經(jīng)典已知活性庫(kù) | 抑制劑庫(kù) | 已知活性化合物庫(kù)

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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