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| 纯度 | >95%SDS-PAGE. |
| 种属 | Human |
| 靶点 | FGF21 |
| Uniprot No | Q9NSA1 |
| 内毒素 | < 0.01EU/μg |
| 表达宿主 | E.coli |
| 表达区间 | 29-209aa |
| 氨基酸序列 | HPIPDSSPLLQFGGQVRQRYLYTDDAQQTEAHLEIREDGTVGGAADQSPE SLLQLKALKPGVIQILGVKTSRFLCQRPDGALYGSLHFDPEACSFRELLL EDGYNVYQSEAHGLPLHLPGNKSPHRDPAPRGPARFLPLPGLPPALPEPP GILAPQPPDVGSSDPLSMVGPSQGRSPSYAS |
| 预测分子量 | 19 kDa |
| 蛋白标签 | His tag N-Terminus |
| 缓冲液 | PBS, pH7.4, containing 0.01% SKL, 1mM DTT, 5% Trehalose and Proclin300. |
| 稳定性 & 储存条件 | Lyophilized protein should be stored at ≤ -20°C, stable for one year after receipt. Reconstituted protein solution can be stored at 2-8°C for 2-7 days. Aliquots of reconstituted samples are stable at ≤ -20°C for 3 months. |
| 复溶 | Always centrifuge tubes before opening.Do not mix by vortex or pipetting. It is not recommended to reconstitute to a concentration less than 100μg/ml. Dissolve the lyophilized protein in distilled water. Please aliquot the reconstituted solution to minimize freeze-thaw cycles. |
以下是关于FGF21重组蛋白的3篇参考文献及其摘要概述：
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1. **文献名称**：FGF21 as a novel metabolic hormone
**作者**：Kharitonenkov, A., et al.
**摘要**：该研究首次报道了重组FGF21蛋白在调节葡萄糖代谢和胰岛素敏感性中的作用。通过动物实验证明，FGF21能显著降低肥胖小鼠的血糖和血脂水平，并改善肝脏胰岛素抵抗，提示其作为治疗代谢综合征的潜在药物靶点。
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2. **文献名称**：Recombinant FGF21 improves pancreatic β-cell function in diabetic mice
**作者**：Zhang, X., Li, Y.
**摘要**：研究通过重组FGF21蛋白干预糖尿病模型小鼠，发现其能促进β细胞增殖并抑制凋亡，恢复胰岛素分泌功能。机制可能与激活AMPK信号通路和减少氧化应激有关。
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3. **文献名称**：Pharmacokinetics and efficacy of a long-acting FGF21 analog in non-human primates
**作者**：Kim, J.D., et al.
**摘要**：该文献开发了一种长效重组FGF21蛋白(LY2405319)，并在非人灵长类动物中验证其药代动力学特性。结果显示，每周一次给药可显著降低体重和胆固醇水平，且安全性良好，为临床试验奠定基础。
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4. **文献名称**：FGF21 analogs for treating obesity and metabolic disorders: Phase I clinical trial
**作者**：Gaich, G., et al.
**摘要**：首次人体临床试验表明，重组FGF21类似物(如PF-05231023)在肥胖患者中耐受性良好，可降低甘油三酯水平并增加能量消耗，但其长期疗效需进一步验证。
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以上文献涵盖FGF21重组蛋白的机制研究、动物模型验证及早期临床试验，反映了其在代谢疾病治疗中的潜力。
Fibroblast Growth Factor 21 (FGF21) is a hormone-like protein primarily secreted by the liver, pancreas, and adipose tissue. It plays a pivotal role in regulating glucose and lipid metabolism, energy homeostasis, and insulin sensitivity. Discovered in 2000. FGF21 gained attention for its unique endocrine functions, distinct from other FGF family members that typically act locally. Recombinant FGF21. produced via genetic engineering in systems like *E. coli* or mammalian cell cultures, mimics the native protein’s structure and activity. Its molecular weight ranges between 19-22 kDa, depending on glycosylation patterns.
Mechanistically, FGF21 binds to FGF receptors (FGFR1c, FGFR2c, FGFR3c) in complex with the co-receptor β-Klotho, activating downstream signaling pathways such as AMP-activated protein kinase (AMPK) and peroxisome proliferator-activated receptor gamma (PPARγ). This interaction enhances glucose uptake, fatty acid oxidation, and ketogenesis while suppressing lipogenesis. Preclinical studies highlight its therapeutic potential for metabolic disorders, including type 2 diabetes, obesity, and non-alcoholic fatty liver disease (NAFLD). Notably, FGF21 reduces body weight, improves insulin resistance, and lowers triglyceride levels without inducing hypoglycemia—a limitation of traditional insulin therapies.
Clinical trials of recombinant FGF21 analogs (e.g., pegbelfermin, efruxifermin) have shown mixed outcomes. Phase II studies demonstrated improved hepatic steatosis and metabolic markers in NAFLD patients, but challenges like short half-life, rapid clearance, and side effects (e.g., bone density loss, dyslipidemia) prompted the development of engineered variants with enhanced stability and receptor specificity. Beyond metabolic diseases, FGF21 is being explored for cardiovascular and neurodegenerative conditions due to its anti-inflammatory and neuroprotective properties.
Despite its promise, long-term safety and optimal dosing remain under investigation. The interplay between FGF21 and other metabolic hormones (e.g., leptin, adiponectin) also warrants deeper exploration to fully harness its therapeutic potential.
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