化合物 Fasiglifam|T2351|TargetMol

Fasiglifam
1000413-72-8

￥462 1mg 起订

￥928 5mg 起订

￥1759 10mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

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联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 化合物 Fasiglifam

英文名称：: Fasiglifam

CAS号：: 1000413-72-8

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.82%

产品类别：: 抑制剂

货号：: T2351

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.
溶解度	DMSO : 50 mg/mL (95.31 mM)
关键字	TAK 875 \| inhibit \| FFAR \| Fasiglifam \| Inhibitor \| TAK-875 \| Free Fatty Acid Receptor
相关产品	Benzyl nicotinate \| CRTh2 antagonist 2 \| CAY10595 \| Azathioprine \| Questiomycin A \| TUG-1375 \| NF-56-EJ40 \| Monomethyl fumarate \| 3-Hydroxyoctanoic Acid \| Fezagepras sodium \| Timapiprant \| Vincamine
相关库	经典已知活性库 \| 已知活性化合物库 \| 抗糖尿病库 \| NO PAINS 化合物库 \| 抗肥胖化合物库 \| GPCR靶点分子库 \| 膜蛋白靶向化合物库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库 \| 抗癌药物库

TAK875|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子