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PF-04457845

PF-04457845

产品编号 T4323   CAS 1020315-31-4
别名: PF04457845, PF 04457845

PF-04457845 是一种非常有效的选择性 FAAH 抑制剂,作用于 rFAAH 和 hFAAH,IC50分别为 7.4±0.62 nM 和 7.2±0.63 nM。

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PF-04457845 Chemical Structure
PF-04457845, CAS 1020315-31-4
规格 价格/CNY 货期 数量
2 mg ¥ 283 现货
5 mg ¥ 455 现货
10 mg ¥ 788 现货
25 mg ¥ 1,660 现货
50 mg ¥ 2,480 现货
100 mg ¥ 3,680 现货
200 mg ¥ 5,330 待询
1 mL * 10 mM (in DMSO) ¥ 493 现货
产品目录号及名称: PF-04457845 (T4323)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 PF-04457845 is a greatly and effctive FAAH inhibitor, and for hFAAH(IC50=7.2±0.63 nM) and rFAAH(IC50=7.4±0.62 nM).
靶点活性 hFAAH:7.2±0.63 nM, rFAAH:7.4±0.62 nM
体外活性 PF-04457845 inhibits FAAH by a covalent, irreversible mechanism involving carbamylation of the active-site serine nucleophile of FAAH with high in vitro potency (kinact/Ki and IC50 values of 40300 M-1s-1 and 7.2 nM, respectively, for human FAAH).
体内活性 In a rat model, oral administration of PF-04457845 causes a significant inhibition of mechanical allodynia measured after 4 h with a minimum effective dose (MED) of 0.1 mg/kg. FAAH is confirmed to be completely inhibited in mice treated with PF-04457845(1 and 10 mg/kg p.o.).
激酶实验 The IC50 values for the inhibition of hFAAH and rFAAH by PF-04457845 is determined. PF-04457845 is preincubated with FAAH for 60 min before initiating the reaction by the addition of the substrate oleamide. Mouse and human tissues are prepared and inhibitor selectivity is assessed by competitive activity-based protein profiling.
细胞实验 PF-04457845 is formulated as a nanocrystalline suspension in 2% polyvinylpyrrolidone and 0.15% sodium dodecyl sulfate in H2O (Rats). PF-04457845 is prepared in polyethyleneglycol 300 (Mice).RatsPF-04457845 is administered orally to male Sprague-Dawley rats (200 g-250 g) at the indicated dose (mg/kg) as a nanocrystalline suspension in 2% polyvinylpyrrolidone and 0.15% sodium dodecyl sulfate in H2O. The dose volume is 10 mL/kg. The Paw Withdrawal Threshold (PWT) is evaluated at 4 h post dose. PWT measurements are averaged and statistical comparisons between groups are made using analysis of variance and unpaired T-tests.Mice Male C57BL6/J mice (7 weeks old; n=8) are treated with PF-04457845 (1 or 10 mg/kg in polyethyleneglycol 300 vehicle by oral administration in a volume of 4 mL/kg), the synthetic cannabinoid agonist WIN 55,212-2 (1 or 10 mg/kg in 18:1:1 saline/Emulphor/ethanol vehicle by intraperitoneal administration in a volume of 10 mL/kg), or the corresponding vehicle. Mice are evaluated for hypomotility, hypothermia, antinociceptive, and cataleptic effects at 4 h or 30 min after PF-04457845 or WIN 55,212-2 administration, respectively, using the tetrad tests except that catalepsy is assessed for 60 s instead of 10 s. Statistical analysis is performed using the Student's t test comparing each treatment group with vehicle.
动物实验 Male C57BL6/J mice (7 weeks old) are treated with PF-04457845 (1 or 10 mg/kg in polyethyleneglycol 300 vehicle by oral administration in a volume of 4 mL/kg).
别名 PF04457845, PF 04457845
分子量 455.43
分子式 C23H20F3N5O2
CAS No. 1020315-31-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (109.78 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1957 mL 10.9786 mL 21.9573 mL 54.8932 mL
5 mM 0.4391 mL 2.1957 mL 4.3915 mL 10.9786 mL
10 mM 0.2196 mL 1.0979 mL 2.1957 mL 5.4893 mL
20 mM 0.1098 mL 0.5489 mL 1.0979 mL 2.7447 mL
50 mM 0.0439 mL 0.2196 mL 0.4391 mL 1.0979 mL
100 mM 0.022 mL 0.1098 mL 0.2196 mL 0.5489 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Johnson DS, et al. Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. ACS Med Chem Lett. 2011 Feb 10;2(2):91-96. 2. Ahn K, et al. Mechanistic and pharmacological characterization of PF-04457845: a highly potent and selective fatty acid amide hydrolase inhibitor that reduces inflammatory and noninflammatory pain. J Pharmacol Exp Ther. 2011 Jul;338(1):114-24. 3. Buntyn RW, et al. Inhibition of Endocannabinoid-Metabolizing Enzymes in Peripheral Tissues Following Developmental Chlorpyrifos Exposure in Rats. Int J Toxicol. 2017 Sep/Oct;36(5):395-402.
Peiminine Glucosamine TPEN Cryptotanshinone (R)-BPO-27 Sinomenine hydrochloride ROC-325 Sulfisoxazole

相关化合物库

该产品包含在如下化合物库中:
神经退行性疾病化合物库 自噬库 代谢化合物库 临床期小分子药物库 抗代谢疾病化合物库 神经信号分子库 NO PAINS 化合物库 药物功能重定位化合物库 已知活性化合物库 抑制剂库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

PF-04457845 1020315-31-4 Autophagy Metabolism Neuroscience FAAH Fatty acid amide hydrolase PF04457845 inhibit Inhibitor PF 04457845 inhibitor

 

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