标签归档：licofelone

Licofelone-d4

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Licofelone-d4 

Licofelone-d4 是 Licofelone 的氘代物。Licofelone (ML-3000) 是双 COX/5-LOX 抑制剂 (IC50 分别为 0.21，0.18 μM)，有潜力用于骨关节炎的研究。Licofelone 具有抗炎和抗增殖作用。Licofelone 诱导细胞凋亡，减少促炎性白三烯和前列腺素的产生。

Licofelone-d4

Licofelone-d4 Chemical Structure

CAS No. : 1189427-04-0

规格 是否有货
5 mg Check price and availability

* Please select Quantity before adding items.

生物活性

Licofelone-d4 (ML-3000-d4) is the deuterium labeled Licofelone. Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins[1][2][3].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

383.90

Formula

C23H18D4ClNO2
CAS 号

1189427-04-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Tavolari S, et al. Licofelone, a dual COX/5-LOX inhibitor, induces apoptosis in HCA-7 colon cancer cells through the mitochondrial pathway independently from its ability to affect the arachidonic acid cascade. Carcinogenesis. 2008 Feb;29(2):371-80.

    [3]. Alvaro-Gracia JM, et al. Licofelone–clinical update on a novel LOX/COX inhibitor for the treatment of osteoarthritis. Rheumatology (Oxford). 2004 Feb;43 Suppl 1:i21-5.

    [4]. Laufer SA, et al. (6,7-Diaryldihydropyrrolizin-5-yl)acetic acids, a novel class of potent dual inhibitors of both cyclooxygenase and 5-lipoxygenase. J Med Chem. 1994 Jun 10;37(12):1894-7.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Licofelone(Synonyms: ML-3000)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Licofelone (Synonyms: ML-3000) 纯度: 98.04%

Licofelone (ML-3000) 是双 COX/5-LOX 抑制剂 (IC50 分别为 0.21，0.18 μM)，有潜力用于骨关节炎的研究。Licofelone 具有抗炎和抗增殖作用。Licofelone 诱导细胞凋亡，减少促炎性白三烯和前列腺素的产生。

Licofelone(Synonyms: ML-3000)

Licofelone Chemical Structure

CAS No. : 156897-06-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥550 In-stock
1 mg ￥500 In-stock
5 mg ￥600 In-stock
10 mg ￥1100 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Licofelone 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Ferroptosis Compound Library
  • Lipid Metabolism Compound Library

生物活性

Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins[1][2][3].

IC50 & Target

COX

0.21 μM (IC50)

5-LOX

0.18 μM (IC50)

体外研究
(In Vitro)

The IC50s of human thrombocyte COX and human 5-LO are 0.16 µM and 0.23 µM, respectively[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

379.88

Formula

C23H22ClNO2
CAS 号

156897-06-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (65.81 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6324 mL 13.1621 mL 26.3241 mL
5 mM 0.5265 mL 2.6324 mL 5.2648 mL
10 mM 0.2632 mL 1.3162 mL 2.6324 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.58 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.58 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Tavolari S, et al. Licofelone, a dual COX/5-LOX inhibitor, induces apoptosis in HCA-7 colon cancer cells through the mitochondrial pathway independently from its ability to affect the arachidonic acid cascade. Carcinogenesis. 2008 Feb;29(2):371-80.

    [2]. Alvaro-Gracia JM, et al. Licofelone–clinical update on a novel LOX/COX inhibitor for the treatment of osteoarthritis. Rheumatology (Oxford). 2004 Feb;43 Suppl 1:i21-5.

    [3]. Laufer SA, et al. (6,7-Diaryldihydropyrrolizin-5-yl)acetic acids, a novel class of potent dual inhibitors of both cyclooxygenase and 5-lipoxygenase. J Med Chem. 1994 Jun 10;37(12):1894-7.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务