降糖，减重，脂肪肝！三合一代谢治疗药物在华正式开售

2024年12月23日，首款GIP和GLP-1双重激动剂礼来替尔泊肽注射剂Mounjaro^®在中国大陆地区正式上市，引发市场强烈关注。作为每周注射一次的GIP和GLP-1双重激动剂，Mounjaro^®以卓越的控糖和显著的减重效果，开启中国市场减肥治疗新篇章。

过去两年，司美格鲁肽凭借长效GLP-1类产品的卓越表现迅速走红，埃隆马斯克等名人效应更助推其成为减重市场的“神坛”药物。受其影响，GLP-1药物成为制药巨头争相布局的热门赛道。巴克莱银行预计，到2030年，全球减重药物市场规模将达1500亿美元。

替尔泊肽已在美团平台开售，美团自营价格与减重版司美格鲁肽相近

2024年6月8日，礼来公司（Eli Lilly）公布重磅药物替尔泊肽（Tirzepatide）在治疗MASH患者的2期临床试验SYNERGY-NASH的详细结果。试验数据最初于欧洲肝病学会（EASL）年会公布，并同步发表在《新英格兰医学杂志》（The New England Journal of Medicine, NEJM），题为“Tirzepatide for Metabolic Dysfunction–Associated Steatohepatitis with Liver Fibrosis”。

研究显示替尔泊肽对MASH缓解和防治肝纤维化具有积极作用¹

研究显示，试验达到主要终点。在52周治疗中，接受替尔泊肽5 mg、10 mg、15 mg治疗的患者中，分别有51.8%、62.8%和73.3%的患者实现MASH缓解且无肝纤维化恶化，而安慰剂组仅为13.2%（所有剂量p<0.001）。

Cell surface staining was performed on Human GLP-1R (Luc) HEK293 Reporter Cell (Cat. No. CHEK-ATF096) or negative control cell using PE-labeled anti-human GLP-1R antibody.

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This reporter cell (Cat. No. CHEK-ATF104) was incubated with serial dilutions of Tirzepatide (a dual GLP-1R and GIPR agonist). The EC50 of Tirzepatide was approximately 0.042 nM.

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This reporter cell (Cat. No. CHEK-ATF103) was incubated with serial dilutions of Retatrutide (a triple agonist peptide of GCGR, GIPR and GLP-1R). The max induction fold was approximately 79.93.

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• THRB激动剂选择性筛选应用案例-RLU

Bioactivity analysis of THR-β-selective agonist (RLU).
The Human THRA (Luc) HEK293 Reporter Cell (Cat. No. CHEK-ATF180) and Human THRB (Luc) HEK293 Reporter Cell (Cat. No. CHEK-ATF181) were incubated with serial dilutions of Resmetirom (a THR-β-selective agonist), respectively. The EC50 of Resmetirom determined on Human THRB (Luc) HEK293 Reporter Cell was approximately 4.4 μM.

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Passage stability analysis of receptors expression by FACS.
Flow cytometry surface staining of human GLP-1R on HEK293/Human GLP-1R Stable Cell Line (High Expression) (Cat. No. CHEK-ATP160) demonstrates consistent mean fluorescent intensity across passage 7-22.

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参考资料：

1. Loomba R, Hartman ML, Lawitz EJ, Vuppalanchi R, Boursier J, Bugianesi E, Yoneda M, Behling C, Cummings OW, Tang Y, Brouwers B, Robins DA, Nikooie A, Bunck MC, Haupt A, Sanyal AJ; SYNERGY-NASH Investigators. Tirzepatide for Metabolic Dysfunction-Associated Steatohepatitis with Liver Fibrosis. N Engl J Med. 2024 Jul 25;391(4):299-310. doi: 10.1056/NEJMoa2401943. Epub 2024 Jun 8. PMID: 38856224.