1. GPCR/G Protein Neuronal Signaling
  2. CGRP Receptor
  3. Fremanezumab

Fremanezumab  (Synonyms: 瑞玛奈珠单抗; TEV-48125; LBR-101; PF-04427429; RN-307)

目录号: HY-P99019 纯度: 95.00%
COA 技术支持

Fremanezumab (TEV-48125) 是一种人源化 IgG2a 单克隆抗体,选择性地且强效地结合降钙素基因相关肽 (CGRP) (IC50 值为 7.943 nM)。Fremanezumab 结合小鼠 CGRPIC50 值为 19.6 nM。Fremanezumab 在体外对抗 CGRP 的抗炎作用,包括 CGRP 介导的对 LPS (HY-D1056) 诱导的小胶质细胞激活的抑制。Fremanezumab 选择性地抑制大鼠皮质扩散抑制 (CSD) 引起的 Aδ 脑膜痛觉神经元激活。Fremanezumab 可用于炎症和慢性偏头痛的研究。

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CAS No. : 1655501-53-3

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Fremanezumab (TEV-48125) is a humanized lgG2a monoclonal antibody that selectively and potently binds to calcitonin gene related peptide (CGRp) (IC50 values = 7.943 nM). Fremanezumab binds to mouse CGRP with an IC50 value of 19.6 nM. Fremanezumab counteracts anti-inflammatory effects of CGRP in vitro, including CGRP-mediated inhibition of LPS (HY-D1056)-induced microglial activation. Fremanezumab selectively inhibits the activation of Aδ meningeal nociceptors by cortical spreading depression (CSD) in rats. Fremanezumab can be used for the study of inflammation and chronic migraine[1][2][3].

IC50 & Target

CALCA/CGRP

体外研究
(In Vitro)

Fremanez Raimab (10 μM,6 小时) 对抗小鼠 CGRP 对 C57Bl 小鼠小胶质细胞原代培养中 LPS (HY-D1056) 诱导的 IL1β、IL6 和 IL12 转录本增加的浓度依赖性抑制作用,但单独在 LPS 孵育时不改变小胶质细胞的激活[1]
Fremanezumab (72 小时) 阻止小鼠 CGRP 对第 30 天 MOG35-55 免疫的 NOD 衍生脾细胞增殖的浓度依赖性抑制,但单独不改变淋巴细胞增殖[1]
Fremanezumab (1-100 ng,1 小时) 降低对人和小鼠 CGRP 的免疫检测,IC50 值分别为 7.94 nM 和 19.6 nM[1]
Fremanezumab (0.00001-1 μM) 显著抑制人 αCGRP、鼠 αCGRP 以及代谢稳定的 CGRP 类似物 SAX 在大鼠大脑基底动脉段中诱导的血管舒张效应,并降低 CGRP (pEC50 从 8.0 降至 6.3) 和 SAX (pEC50 从 7.2 降至 6.3) 的效力[2]

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

体内研究
(In Vivo)

Fremanezumab (100 mg/kg, 皮下注射, 每 2 周一次) 在 NOD 小鼠中对疾病进展、存活率、脊髓神经退行性变或先天/适应性免疫反应无影响[1]
Fremanezumab (30 mg/kg,静脉注射,一次) 在麻醉雄性大鼠中选择性地抑制皮质扩散抑制 (CSD) 引起的 Aδ 脑膜痛觉感受器的激活[3]

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

Animal Model: Male Sprague-Dawley rats (225-325 g)[3]
Dosage: 30 mg/kg
Administration: i.v., once
Result: Achieved a significantly lower activation rate of Aδ meningeal nociceptors by CSD.
Showed a significant increase in the firing rate of activated C-fiber meningeal nociceptors.
Clinical Trial
分子量

145.5 kDa

CAS 号
性状

液体

颜色

Colorless to light yellow

中文名称

瑞玛奈珠单抗

储存方式

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

Format
  • Human IgG2 kappa
纯度 & 产品资料

纯度: 95.00%

参考文献
  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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