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FPL 62064 {[allProObj[0].p_purity_real_show]}

货号:A268943

FPL 62064是一种强效的 5-脂氧合酶(5-LOX)和 COX-2 双重抑制剂,具有强效的抗炎作用。

FPL 62064 化学结构 CAS号:103141-09-9
FPL 62064 化学结构
CAS号:103141-09-9
FPL 62064 3D分子结构
CAS号:103141-09-9
FPL 62064 化学结构 CAS号:103141-09-9
FPL 62064 3D分子结构 CAS号:103141-09-9
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FPL 62064 纯度/质量文件 产品仅供科研

货号:A268943 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 lipoxygenase 其他靶点 纯度
Zileuton 97%
Nordihydroguaiaretic acid 99%+
MK-886 99%+
Esculetin 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 COX COX-1 COX-2 其他靶点 纯度
Piroxicam 98%
Salicylic acid 98%
Phenacetin 98%
Etodolac 99%
Flunixin meglumine 98%
Ibuprofen L-lysine 99%
Nabumetone 98%
Acemetacin 98%
Diflunisal 98%
Pranoprofen 98%
Ampiroxicam 98%
Meloxicam 98%
Sulindac 98%
Ketoprofen 98%
Mefenamic Acid 95%
Bromfenac sodium 98%
Oxaprozin 99%
Aspirin 99%
Nepafenac 98%
Zaltoprofen 99%
Salicin 98%
Suprofen 99%+
Xanthohumol 99%
Parecoxib 98%
Tolfenamic Acid +++

COX-2, IC50: 0.2 μM

98%
Etoricoxib 99%
Niflumic Acid 98%
Valdecoxib ++++

COX-2, IC50: 5 nM

99+%
Ibuprofen +

COX-1, IC50: 13 μM

+

COX-2, IC50: 370 μM

98%
Indomethacin ++

COX1, IC50: 0.28 μM

+

COX-2, IC50: 14 μM

97%
Lornoxicam ++++

COX-1, IC50: 5 nM

++++

COX-2, IC50: 8 nM

98%
Meclofenamic acid sodium ++++

COX-1, IC50: 40 nM

+++

COX-2, IC50: 50 nM

99%
Rofecoxib ++++

COX-2, IC50: 18 nM

98%
Asaraldehyde 98%
Naproxen +

COX-1, IC50: 8.7 μM

+

COX-2, IC50: 5.2 μM

98%
Diclofenac Sodium Salt +++

COX-1, IC50: 60 nM

+++

COX-2, IC50: 200 nM

98%
NS-398 ++

COX-2, IC50: 3.8 μM

95%
Amfenac Sodium Hydrate ++

COX-1, IC50: 250 nM

+++

COX-2, IC50: 150 nM

98%+
Nimesulide +

COX-2, IC50: 26 μM

98%
Lumiracoxib ++

COX-1, Ki: 3 μM

+++

COX-2, Ki: 60 nM

99%
Rutaecarpine 95%
Celecoxib ++++

COX-2, IC50: 40 nM

98%
Carprofen ++++

canine COX2, IC50: 30 nM

98%
Ketorolac ++

COX-1 (human), IC50: 1.23 μM

++

COX-2 (human), IC50: 3.50 μM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

FPL 62064 生物活性

描述 Prostaglandins (PGs) from the cyclooxygenase pathway and leukotrienes (LTs) from the lipoxygenase pathway are both mediators of the inflammatory process generated from the same arachidonic acid (AA) cascade[1]. FLP 62064 is a dual inhibitor of prostaglandin synthetase and 5-lipoxygenase with IC50s of 3.6 and 3.1 μM, respectively. In vivo, FPL 62064 inhibited all three parameters with the following order of potency: PGE2 (prostaglandin E2)>LTC4 (leukotriene C4)>oedema, corresponding to ID50 values of 3.7, 28.3 and 40.8 μg of FPL 62064 per ear, respectively. Furthermore, FPL 62064 (1, 3, 10 μg/site) inhibited production of all three metabolites in a dose-dependent manner. The increase in plasma protein extravasation observed 2 hr after injection of arachidonic acid (range 22-64 μl plasma/site, n = 10) was also dose dependently inhibited by FPL 62064. Moreover, FPL 62064 (250-1000 μg per ear) dose-dependently inhibited oedema, PMN (polymorphonuclear granulocytes) infiltration and the proliferative response to TPA (12-O-tetradecanoylphorbol 13-acetate). In guinea-pigs, FPL 62064 applied topically to irradiated skin produced dose-related inhibition of PGE2 formation with an IC50 of 11 μg[2].

FPL 62064 参考文献

[1]Shabaan MA, Kamal AM, Faggal SI, Elsahar AE, Mohamed KO. Synthesis and biological evaluation of pyrazolone analogues as potential anti-inflammatory agents targeting cyclooxygenases and 5-lipoxygenase. Arch Pharm (Weinheim). 2020;353(4):e1900308

[2]Blackham A, Griffiths RJ, Hallam C, et al. FPL 62064, a topically active 5-lipoxygenase/cyclooxygenase inhibitor. Agents Actions. 1990;30(3-4):432-442

FPL 62064 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.77mL

0.75mL

0.38mL

18.85mL

3.77mL

1.88mL

37.69mL

7.54mL

3.77mL

FPL 62064 技术信息

CAS号103141-09-9
分子式C16H15N3O
分子量 265.31
SMILES Code COC1=CC=C(NC2=NN(C3=CC=CC=C3)C=C2)C=C1
MDL No. MFCD00877802
别名
运输蓝冰
InChI Key WKLGNFJHVJIZPK-UHFFFAOYSA-N
Pubchem ID 128268
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, sealed in dry, room temperature

溶解方案

DMSO: 250 mg/mL(942.29 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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