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Loxoprofen/洛索洛芬 {[allProObj[0].p_purity_real_show]}

货号:A171140 同义名: Koloxo; Loxoprofeno

Loxoprofen is a non-steroidal anti-inflammatory drug (NSAID) and propionic acid derivative.

Loxoprofen/洛索洛芬 化学结构 CAS号:68767-14-6
Loxoprofen/洛索洛芬 化学结构
CAS号:68767-14-6
Loxoprofen/洛索洛芬 3D分子结构
CAS号:68767-14-6
Loxoprofen/洛索洛芬 化学结构 CAS号:68767-14-6
Loxoprofen/洛索洛芬 3D分子结构 CAS号:68767-14-6
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Loxoprofen/洛索洛芬 纯度/质量文件 产品仅供科研

货号:A171140 标准纯度: {[allProObj[0].p_purity_real_show]}
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全球学术期刊中引用的产品

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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。

Loxoprofen/洛索洛芬 生物活性

描述 Loxoprofen (LOX) is a non-selective cyclooxygenase inhibitor that is widely used for the treatment of pain and inflammation caused by chronic and transitory conditions. In addition, LOX can also be converted into an inactive hydroxylated metabolite (OH-LOXs) by cytochrome P450 (CYP) [3]. Loxoprofen (Loxonin(®), Loxonin(®) Pap, Loxonin(®) Tape) is a prodrug-type NSAID that is available in several formulations, including 60 mg tablets, 100 mg hydrogel patches and 50 or 100 mg tape. Loxoprofen is a useful analgesic option for patients with pain and inflammation, with topical loxoprofen potentially reducing the risk of gastrointestinal, cardiovascular and renal complications associated with oral NSAID use[4]. The uptake of loxoprofen into Caco-2 cells was pH- and concentration-dependent, and was described by a Michaelis-Menten equation with passive diffusion (Km : 4.8 mm, Vmax : 142 nmol/mg protein/30 s, and Kd : 2.2 μl/mg protein/30 s). Transport of loxoprofen in Caco-2 cells is, at least in part, mediated by a proton-dependent transport system[5].

Loxoprofen/洛索洛芬 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02384928 Sciatica Inte... 展开 >>rvertebral Disc Displacement 收起 << Not Applicable Completed - Korea, Republic of ... 展开 >> Jaseng Hospital of Korean Medicine Seoul, Gangnam-Gu, Korea, Republic of, 135-896 收起 <<
NCT03386149 Lumbar Disc Herniation Phase 3 Recruiting September 30, 2018 Korea, Republic of ... 展开 >> Dongguk University Bundang Oriental Hospital Recruiting Seongnam, Gyeonggi, Korea, Republic of, 13601 Contact: Eun-Jung Kim, PhD., KMD    +82317103751    hanijjung@naver.com    Daegu Korean Medicine Hospital of Daegu Haany University Recruiting Daegu, Korea, Republic of, 42158 Contact: I-Rang Choi, B.S    +82537702324    soongood88@dhu.ac.kr    Kyunghee University Medical Center Recruiting Seoul, Korea, Republic of, 02447 Contact: Sae-Rom Jeon, B.S.    +821050478756    sr9213@naver.com    Kyung Hee University Hospital at Gangdong Recruiting Seoul, Korea, Republic of, 05278 Contact: Bonhyuk Goo, M.S., KMD    +8224406099    goobh99@naver.com 收起 <<
NCT02467504 Rheumatoid Arthritis Phase 2 Unknown June 2017 China, Beijing ... 展开 >> Department of Rheumatology and Immunology, Peking University People's Hospital Recruiting Beijing, Beijing, China, 100044 Contact: Xiaoying Zhang, MD    +8613810001444    xiaoying19880307@163.com 收起 <<

Loxoprofen/洛索洛芬 参考文献

[1]Hiroshima Y, Kato T, Tajima K. Regression of diffuse large B-cell lymphoma in sphenoid and ethmoid sinuses following treatment with loxoprofen. Leuk Lymphoma. 2016;57(3):721-3.

[2]Kanda A, Ebihara S, et al. Loxoprofen sodium suppresses mouse tumor growth by inhibiting vascular endothelial growth factor. Acta Oncol. 2003;42(1):62-70.

[3]Paudel S, Shrestha A, Cho P, et al. Assessing Drug Interaction and Pharmacokinetics of Loxoprofen in Mice Treated with CYP3A Modulators. Pharmaceutics. 2019;11(9):479. Published 2019 Sep 16

[4]Greig SL, Garnock-Jones KP. Loxoprofen: A Review in Pain and Inflammation. Clin Drug Investig. 2016;36(9):771-781

[5]Narumi K, Kobayashi M, Kondo A, et al. Characterization of loxoprofen transport in Caco-2 cells: the involvement of a proton-dependent transport system in the intestinal transport of loxoprofen. Biopharm Drug Dispos. 2016;37(8):447-455

Loxoprofen/洛索洛芬 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.06mL

0.81mL

0.41mL

20.30mL

4.06mL

2.03mL

40.60mL

8.12mL

4.06mL

Loxoprofen/洛索洛芬 技术信息

CAS号68767-14-6
分子式C15H18O3
分子量 246.3
SMILES Code CC(C1=CC=C(CC2C(CCC2)=O)C=C1)C(O)=O
MDL No. MFCD00864331
别名 Koloxo; Loxoprofeno; Loxoprofene
运输蓝冰
InChI Key YMBXTVYHTMGZDW-UHFFFAOYSA-N
Pubchem ID 3965
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, room temperature

溶解方案 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
方案一
方案二
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