Loxoprofen Sodium|80382-23-6|(洛索洛芬钠)-陌孚医药/Medlife

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Loxoprofen Sodium (Synonyms: 洛索洛芬钠)

目录号: PC19110 纯度: ≥98%

CAS No. :80382-23-6

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中文名称	Loxoprofen Sodium
中文别名	洛索洛芬钠;2-[4-(2-氧代环戊烷-1-基甲基)苯基]丙酸钠二水合物;洛索洛芬钠二水;镰叶芹醇;氯洛索洛芬钠;洛索洛芬钠原药;洛索洛酚钠;马来酸二甲酯;洛索洛芬钠，医药级,纯度:>99%
英文名称	Loxoprofen Sodium
英文别名	Loxoprofen Sodium;Loxoprofen Sodium (Mixture of diastereomers);LOXOPROFENE SODIUM;cs-600;Loxonin;LOXOPROFEN NA;Loxoprofen sodiuM hydrate;loxoprofensodiumdihydrate;SodiuM Loxoprofen;sodium salt of Loxoprofen;Unastin;benzeneacetic acid, alpha-methyl-4-((2-oxocyclopentyl)methyl)-, sodium salt, di alpha-methyl-4-((2-oxocyclopentyl)methyl)benzeneacetate sodium salt dihydrate;Sodium 2-[4-(2-Oxocyclopentyl-1-methyl)phenyl]propionate dihydrate;Loxoprofen sodium salt;Sodium 2-(4-((2-oxocyclopentyl)methyl)phenyl)propanoate;LX-A;AK189220;Sodium 2-[4-[(2-Oxocyclopentyl)methyl]phenyl]propionate;Sodium 2-(4-(2-oxocyclopentylmethyl)phenyl)propionate dihydrate;CS 600;sodium 2-{4-[(2-oxocyclopentyl)methyl]phenyl}propanoate;Benzeneacetic acid, alpha-methyl-4-((2-oxocyclopentyl)
Cas No.	80382-23-6
分子式	C₁₅H₁₇NaO₃
分子量	268.28
包装储存	4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

生物活性

Loxoprofen sodium is a non-steroidal, orally active anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen sodium is a nonselective COX inhibitor with IC₅₀s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively. Loxoprofen sodium can reduce atherosclerosis and shows antitumor activity.

性状

Solid

IC50 & Target[1][2]

COX-1

6.5 μM (IC₅₀)

COX-2

13.5 μM (IC₅₀)

体外研究(In Vitro)

Loxoprofen sodium, an anti-inflammatory prodrug (NSAID), is a nonselective COX inhibitor with IC₅₀s of 6.5 and 13.5μM for COX-1 and COX-2 in human whole blood assays, respectively.
Loxoprofen (LOX) sodium is a non-selective cyclooxygenase inhibitor that is widely used for the reasearch of pain and inflammation caused by chronic and transitory conditions. Its alcoholic metabolites are formed by carbonyl reductase (CR) and they consist of trans-LOX, which is active, and cis-LOX, which is inactive. In addition, LOX sodium can also be converted into an inactive hydroxylated metabolite (OH-LOXs) by cytochrome P450 (CYP).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Loxoprofen sodium (4 mg/kg/day; p.o.; 1 or 8 weeks) reduces atherosclerosis in mice by reducing inflammation. Loxoprofen sodium (60 μg/mL; p.o.; 24 days) suppresses mouse tumor growth by inhibiting VEGF.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	ApoE mice (C57BL/6J-Apoe) with high-fat diet (0.2% cholesterol, 21% saturated fat) from 8 to 16 weeks of age
Dosage:	4 mg/kg/day in drinking water
Administration:	Oral dosing from 8 to 16 weeks of age or from 15 to 16 weeks of age
Result:	Inhibited platelet thromboxane production and platelet aggregation. Reduced extent of atherosclerosis. Suppressed the production of PGE₂, TxB₂ and PGI₂.

Animal Model:	6-week-old male C57BL/6 and BDF1 mice, 100 μL suspensions (2 × 10 cells/mL) of LLC cells and KLN205 cells were injected subcutaneously into C57BL/6 and BDF1 mice, respectively.
Dosage:	60 μg/mL
Administration:	Oral dosing in drinking water, every day for 24 days
Result:	Suppressed tumor growth and angiogenesis, suppressed expression of VEGF in mice with LLC tumor, inhibited tubular formation of HUVECs.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

ClinicalTrial

参考文献

[1]. Riendeau D, et al. Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2. Bioorg Med Chem Lett. 2004;14(5):1201-1203. [Information]

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

[3]. Hamaguchi M, et al. Loxoprofen Sodium, a Non-Selective NSAID, Reduces Atherosclerosis in Mice by Reducing Inflammation. J Clin Biochem Nutr. 2010 Sep;47(2):138-47. [Information]

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

溶解度数据

体外研究:

H₂O : 100 mg/mL (372.74 mM; Need ultrasonic)

DMSO : 19.23 mg/mL (71.68 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.7274 mL	18.6372 mL	37.2745 mL
5 mM	0.7455 mL	3.7274 mL	7.4549 mL
10 mM	0.3727 mL	1.8637 mL	3.7274 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制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

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1.92 mg/mL (7.16 mM); Clear solution

此方案可获得 ≥ 1.92 mg/mL (7.16 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 19.2 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.92 mg/mL (7.16 mM); Clear solution

此方案可获得 ≥ 1.92 mg/mL (7.16 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 19.2 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1.92 mg/mL (7.16 mM); Clear solution

此方案可获得 ≥ 1.92 mg/mL (7.16 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 19.2 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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