化合物 PF8380|T3631

PF-8380
1144035-53-9

￥131 1mg 起订

￥168 2mg 起订

￥248 5mg 起订

上海更新日期：2024-09-14

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 化合物 PF8380

英文名称：: PF-8380

CAS号：: 1144035-53-9

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.45%

产品类别：: 抑制剂

货号：: T3631

Product Introduction

Bioactivity

名称	PF-8380
描述	PF-8380 is an effective and orally available autotaxin inhibitor (IC50: 2.8 nM, in isolated enzyme assay; 101 nM, in the human whole blood). It modulates lysophosphatidic acid (LPA) levels in vivo/vitro by directly inhibiting autotaxin; reduces LPA levels both in plasma and at the site of inflammation.
细胞实验	GL261 or U87-MG cells are plated in triplicate onto 6 cm plates and allowed to grow to 70% confluence. The semi-confluent cell layer is scratched with a sterile 200 μL pipette tip to create a scratch devoid of cells and plates are washed once with PBS to remove non-adherent cells and debris. For radiosensitization drug studies, cells are treated with 1 μM PF-8380 or DMSO for 45 min prior to irradiation with 4 Gy, and then incubated at 37°C in 5% CO2. Control plates are monitored for cell migration (20–24 h). Cells are fixed with 70% ethanol and stained with 1% methylene blue. To quantify migration, cells in three randomly selected high power fields (HPFs) in the scratched area are counted and normalized for surrounding cell density.(Only for Reference)
激酶实验	FS-3 substrate is solubilized in assay buffer at 500 μM and frozen at -20°C in single-use aliquots for up to 4 weeks. Recombinant autotaxin is diluted in Tris-buffered saline (140 mM NaCl, 5 mM KCl, 1 mM CaCl2, 1 mM MgCl2, 50 mM Tris, pH 8.0) and incubated with compound in DMSO or DMSO alone (final 1% DMSO) for 15 min at 37°C, and the reaction is started with the addition of FS-3 at a final concentration of 1 μM. The reaction is allowed to proceed at 37°C for 30 min and monitored at 520 nm until the uninhibited control compared with a no-enzyme control gave a Z′≥0.5. IC50s are determined in triplicate by using a four-parameter fit[1].
体外活性	在放射辐射前,PF-8380预处理可抑制辐射诱导的肿瘤血管内皮细胞血管生成、并延迟神体内经胶质瘤肿瘤生长与发展[2]. 在大鼠气囊炎模型中,PF8380（30 mg/kg,p.o.）可减少炎性痛觉过敏,3 h内可使血浆和炎症组织的LPA水平降低超过95%.
体内活性	PF-8380与FS-3D底物抑制大鼠自毒素（IC50：1.16 nM）。在人体全血中,PF-8380处理2 h可抑制自毒素（IC50：101 nM）[1]。PF-8380可抑制GBM细胞的自毒素,随后使其入侵及迁移减少、并使辐射敏化增强。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : ＜1 mg/mL (insoluble or slightly soluble)
关键字	inhibit \| Phosphodiesterase (PDE) \| PF 8380 \| PF8380 \| PF-8380 \| Inhibitor
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PF-8380|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子