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MBX-2982

MBX-2982

产品编号 T1793   CAS 1037792-44-1

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。

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MBX-2982 Chemical Structure
MBX-2982, CAS 1037792-44-1
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
产品目录号及名称: MBX-2982 (T1793)
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纯度: 99.96%
纯度: 98.83%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (111.47 mM)

溶液配制表

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

计算器

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分子量计算器
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参考文献

1. Hothersall JD, et al. Sustained wash-resistant receptor activation responses of GPR119 agonists. Eur J Pharmacol. 2015 Sep 5;762:430-42. 2. Lan H, et al. Agonists at GPR119 mediate secretion of GLP-1 from mouse enteroendocrine cells through glucose-independent pathways. Br J Pharmacol. 2012 Apr;165(8):2799-807.
AM-1638 AZD1981 FL104 GPR4 antagonist 1 FTBMT ML192 [Orn8]-Urotensin II acetate NF-56-EJ40

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌临床化合物库 已知活性化合物库 神经信号分子库 GPCR靶点分子库 药物功能重定位化合物库 抗糖尿病库 内分泌激素分子库 经典已知活性库 ReFRAME 相关化合物库

剂量换算

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体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
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给药体积
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第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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技术支持

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。

Keywords

MBX-2982 1037792-44-1 Endocrinology/Hormones GPCR/G Protein GPR Inhibitor G Protein-Coupled Receptor 119 MBX 2982 GPR119 MBX2982 inhibit inhibitor

 

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