Fenoprofen Calcium  (Synonyms: 非诺洛芬钙; LILLY-53858 Calcium)

Fenoprofen (LILLY-53858) Calcium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen Calcium is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen Calcium also increases ERK1/2 activation in HEK293T cells. Fenoprofen Calcium has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis^[1][2].

在 HEK293T 细胞中，Fenoprofen Calcium 以双相方式刺激 MC3-5R 上的 ERK1/2 活化，其中 MC3R 浓度为 3 和 10 µM 时，MC4R 浓度为 1 µM时，MC5R 浓度为 3 µM 时，ERK1/2 活化最强。在转染空载体 pcDNA3.1 和 MC1R 的细胞中，Fenoprofen Calcium 诱导的 pERK1/2 水平无显著差异。Fenoprofen Calcium 诱导 MC3-5R 上的偏向信号传导，因为它选择性地激活 ERK1/2 级联，但不激活典型的 cAMP 信号传导^[1]。

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

Fenoprofen (10 mg/kg；腹腔注射；从第 2 天起，每日两次；连续 7 天) Calcium 对软骨完整性和滑膜炎具有抗关节炎作用，但在 Mc3r^-/- 小鼠中，该作用显著减弱^[2]。

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

262.31

C₁₅H₁₄O₃.1/2Ca

34597-40-5

非诺洛芬钙

Room temperature in continental US; may vary elsewhere.

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

• [1]. Yuan XC, et al. Fenoprofen-An Old Drug Rediscovered as a Biased Allosteric Enhancer for Melanocortin Receptors. ACS Chem Neurosci. 2019 Mar 20;10(3):1066-1074.  [Content Brief]

  [2]. Montero-Melendez T, et al. Old drugs with new skills: fenoprofen as an allosteric enhancer at melanocortin receptor 3. Cell Mol Life Sci. 2017 Apr;74(7):1335-1345.  [Content Brief]