Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MBX2982 是口服具有活力的、选择性的 G 蛋白偶联受体 119 (GPR119) 激动剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 476 | 现货 | ||
2 mg | ¥ 689 | 现货 | ||
5 mg | ¥ 1,120 | 现货 | ||
10 mg | ¥ 1,890 | 现货 | ||
25 mg | ¥ 3,490 | 现货 | ||
50 mg | ¥ 4,960 | 现货 | ||
100 mg | ¥ 7,190 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,230 | 现货 |
产品描述 | MBX-2982 is a selective, orally-available GPR119 agonist, used for the treatment of diabetes. |
体外活性 | In cells pre-treated with MBX-2982 (1 μM) in “chronic incubation/washout” experiments, cAMP accumulation captured by IBMX inclusion is significantly increased compared to control cells (P<0.01; ANOVA; n=3-6) despite extensive washing to remove excess agonist. AR-231,453 produces sustained responses in a similar concentration range to those observed with acute stimulation (a small 1.82 fold shift), with pEC50s of 8.67±0.11 and 8.93±0.17, respectively. In addition, a large but less severe shift in concentration responses (57.54 fold) is observed for MBX-2982 with respective sustained and acute pEC50s of 7.03±0.13 and 8.79±0.12[1]. |
体内活性 | To examine whether the observations in GLUTag and the primary intestinal cells has physiological relevance, C57BL/6 mice are treated with the GPR119 agonist MBX-2982 at a dose of 10 mg/kg. Note that no DPP-IV inhibitor is co-administered in this experiment to examine a direct GPR119 effect, however, a DPP-IV inhibitor is used to preserve active GLP-1 in the blood samples. The plasma GLP-1 levels from the mice dosed with MBX-2982 are increased without a glucose load, indicating that GPR119-mediated GLP-1 secretion is not dependent on glucose[2]. |
激酶实验 | HEK-GPR119 cells are transfected with GloSensor 22F plasmid and used for dynamic cAMP measurements 24-30 h later. Cell suspensions are made by dislodging the cells using PBS wash and Accutase treatment followed by resuspension in culture media. Cells are then washed twice by pelleting through centrifugation (300 g, 5 min) and resuspension in assay buffer (Hank's Balanced Salt Solution supplemented with 20 mM HEPES and 0.01% fatty acid free BSA, pH 7.4). Cells are then counted and diluted to 600,000 cells/mL in buffer, before GloSensor cAMP reagent is added (2% v/v) and equilibrated with the cells for 2 h at 20°C with periodic mixing. 50 μl/well of cells are added to white-bottomed 384 well plates (30,000 cells/well) in triplicate and baseline luminescence is measuring using an Envision plate-reader. 5 μL of MBX-2982 (serially diluted in DMSO and then diluted 1:100 in assay buffer to obtain ×10 concentrated solution) is manually added to the assay wells to achieve the stated final concentration. Plates are incubated at 20°C with luminescence read at regular intervals to detect dynamic cAMP changes over time within the same wells. cAMP responses at each time-point are expressed as fold over control (vehicle-treated cells)[1]. |
细胞实验 | MBX-2982 is serially diluted in DMSO and then diluted 1:100 in assay buffer to obtain ×10 concentrated solutionis[1]. HEK-GPR119 cells are grown to confluency in flasks, and cell suspensions are made by dislodging cells using PBS wash and accutase treatment followed by resuspension in culture media. Cells are then washed twice by pelleting through centrifugation (227 g, 7 min, 20°C) and resuspension in warm assay buffer (Hank's Balanced Salt Solution supplemented with 20 mM HEPES and 0.01% fatty acid free BSA, pH 7.4), with a 5 min incubation at 37°C after the second wash. Cells are then counted and diluted to 200,000 cells/mL in warm assay buffer[1]. |
分子量 | 448.54 |
分子式 | C22H24N8OS |
CAS No. | 1037792-44-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (111.47 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2295 mL | 11.1473 mL | 22.2946 mL | 55.7364 mL |
5 mM | 0.4459 mL | 2.2295 mL | 4.4589 mL | 11.1473 mL | |
10 mM | 0.2229 mL | 1.1147 mL | 2.2295 mL | 5.5736 mL | |
20 mM | 0.1115 mL | 0.5574 mL | 1.1147 mL | 2.7868 mL | |
50 mM | 0.0446 mL | 0.2229 mL | 0.4459 mL | 1.1147 mL | |
100 mM | 0.0223 mL | 0.1115 mL | 0.2229 mL | 0.5574 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
MBX-2982 1037792-44-1 Endocrinology/Hormones GPCR/G Protein GPR Inhibitor G Protein-Coupled Receptor 119 MBX 2982 GPR119 MBX2982 inhibit inhibitor