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- CAS号：
1000413-72-8
- 规格：
1mLx10mM(inDMSO)/1mg/5mg/10mg/25mg/50mg/100mg/200mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥735.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥351.0 |
| 规格： | 5mg | 产品价格： | ￥705.0 |
| 规格： | 10mg | 产品价格： | ￥1104.0 |
| 规格： | 25mg | 产品价格： | ￥1904.0 |
| 规格： | 50mg | 产品价格： | ￥2864.0 |
| 规格： | 100mg | 产品价格： | ￥3976.0 |
| 规格： | 200mg | 产品价格： | ￥5512.0 |
Product Introduction
Bioactivity
| 名称 | Fasiglifam |
| 描述 | Fasiglifam (TAK875) is a potent, selective and orally bioavailable GPR40 agonist. |
| 细胞实验 | TAK-875 is dissolved in 1% BSA and 0.1% DMSO.? INS-1 832/13 cells are suspended in RPMI medium and seeded in a 96-well plate at a density of 2×104 cells/well; 1% BSA and 0.1% DMSO alone (control), palmitic acid (10, 100, and 1000 μM), oleic acid (10, 100, and 1000 μM), or TAK-875 (1, 10, and 100 μM) is added to the plate. After 72-h culture, medium is discarded, and cells are preincubated for 2 h with KRBH containing 1 mM glucose and 0.2% BSA at 37°C. After discarding of the preincubation buffer, KRBH containing 1 or 20 mM glucose and 0.2% BSA is added, and the plate is further incubated for 2 h. The insulin concentration in the supernatant is measured as described above. To measure intracellular insulin content, INS-1 832/13 cells are exposed to 1% BSA and 0.1% DMSO alone (control), palmitic acid (1000 μM), oleic acid (1000 μM), or TAK-875 (100 μM) with 1% BSA and 0.1% DMSO. After incubation, cells are washed once with phosphate-buffered saline, and acid-ethanol solution is added to each well, followed by sonication on ice. Intracellular insulin is extracted by overnight incubation at ?30°C, followed by separation of supernatant by centrifugation at 12,000 rpm×5 min at 4°C. |
| 激酶实验 | INS-1 832/13 cells are suspended in RPMI medium containing 11 mM glucose and the supplements described above. These cells are seeded at a density of 2×104?cells/well in a 96-well black plate coated with poly-D-lysine, and 1% BSA and 0.1% DMSO alone (control), palmitic acid (62.5, 125, 250, 500, and 1000 μM), oleic acid (62.5, 125, 250, 500, and 1000 μM), or TAK-875 (6.25, 12.5, 25, 50, and 100 μM) is added to the plate with 1% BSA and 0.1% DMSO, followed by culture for 72 h. After the culture, caspase 3/7 activity is measured with the Apo-one homogeneous caspase 3/7 assay according to the manufacturer's instructions. Fluorescence intensity is measured at an excitation of 485 nm and an emission at 535 nm. |
| 体外活性 | Fasiglifam在CHO-hGPR40細胞中以濃度依賴的方式增加細胞內IP產量，其EC50值為0.072 μM。在CHO細胞中，Fasiglifam以濃度範圍0.1-10 μM呈濃度依賴性提高細胞內IP產量[1]。此外，Fasiglifam在3-30 μM的濃度範圍內，依賴於濃度地增加[Ca2+]i。在10 mM葡萄糖存在的環境下，Fasiglifam以0.001-10 μM的濃度範圍內，依賴於濃度地促進INS-1 833/15細胞中胰島素的分泌[2]。 |
| 体内活性 | Fasiglifam（10 mg/kg，p.o.）在ZDF大鼠中提高了血浆胰岛素水平。Fasiglifam（30 mg/kg，p.o.）改善了空腹高血糖，而不影响空腹正常血糖。与改善糖尿病大鼠葡萄糖耐量的剂量相比，Fasiglifam在30 mg/kg的剂量，即3至10倍较高剂量，不会改变具有正常葡萄糖稳态的SD大鼠的空腹血糖水平。同样，Fasiglifam在具有正常空腹血糖水平的SD大鼠中并未显著改变胰岛素分泌[1]。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.81 mM), Sonication is recommended. 10% DMSO+90% Saline : 10 mg/mL (19.06 mM), Suspension. DMSO : 150 mg/mL (285.92 mM), Sonication is recommended. |
| 关键字 | TAK-875 | TAK 875 | Inhibitor | inhibit | GPR40(FFA1) | GPR40 | Free Fatty Acid Receptor | FFAR | Fasiglifam |
| 相关产品 | Benzyl nicotinate | TUG-424 | CRTh2 antagonist 2 | CAY10595 | 1-methoxycyclopropanecarboxylic acid | Azathioprine | Kynurenic acid | TUG-1375 | Monomethyl fumarate | Fezagepras sodium | Timapiprant | Pamoic acid disodium |
| 相关库 | Bioactive Compound Library | Bioactive Compounds Library Max | Failed Clinical Trials Compound Library | Endocrinology-Hormone Compound Library | Anti-Obesity Compound Library | GPCR Compound Library | Membrane Protein-targeted Compound Library | Orally Active Compound Library | Drug Repurposing Compound Library | Anti-Metabolism Disease Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |
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网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 Fasiglifam【1000413-72-8】
￥351 - 5512
