SJ-MX2878
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Fasiglifam
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Fasiglifam (also known as TAK-875) is a novel, long-acting, selective and orally bioavailable and selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line, it is 400-fold more potent than oleic acid. TAK-875 has a favorable pharmacokinetic profile which enables long-acting drug efficacy. TAK-875 exhibited potent agonistic activity and high binding affinity to the human GPR40 receptor. In addition, TAK-875 showed excellent agonist potency and selectivity for GPR40 receptor over other members of the FFA receptor family (e.g. EC50>10 μM for others).
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SJ-MX2782
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GW9508
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GW9508 is a potent and selective agonist for the free fatty acid receptor FFA1 (GPR40).
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SJ-MN1202
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Vincamine
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长春胺 |
Vincamine 是从马达加斯加长春花中提取的一种单萜类吲哚生物碱。Vincamine 可以作为一种外周血管扩张剂 (Vasodilator),对脑微血管循环有选择性的血管调节作用。Vincamine 是一种 GPR40 激动剂,通过改善β细胞功能障碍和促进葡萄糖刺激型胰岛素分泌 (GSIS) 发挥β细胞保护作用。Vincamine 可改善体内葡萄糖稳态,对 2 型糖尿病 (T2DM) 的研究具有潜力。
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SJ-MX1702
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Fasiglifam (TAK-875)
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Fasiglifam (TAK-875)是一种选择性GPR40激动剂,在表达人GPR40的CHO细胞系中EC50为14 nM,比油酸有效400倍。
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SJ-MX1182
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DC260126
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DC260126 是一种有效的 GPR40 (FFAR1) 拮抗剂。DC260126 剂量依赖性地抑制亚油酸、油酸、棕榈油酸和月桂酸刺激的 GPR40 介导的 Ca2+ 升高 (IC50 分别 6.28, 5.96, 7.07, 4.58 μM)。DC260126 对棕榈酸酯诱导的内质网应激和凋亡 (apoptosis) 有保护作用。
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SJ-MX5656
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Fezagepras sodium
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