规格 | 价格 | 库存 | 数量 |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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靶点 |
Human GLP-1 receptor ( EC50 = 0.66 μM ); Rat GLP-1 receptor ( EC50 = 0.755 μM )
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体外研究 (In Vitro) |
BETP 是一种 GLP-1 受体激动剂,对人和大鼠 GLP-1 受体的 EC50 分别为 0.66 和 0.755 μM。 BETP(化合物 B)在表达 GLP-2、GIP、PTH 或胰高血糖素受体的细胞中无活性。 BETP (1-10 μM) 可增强正常和糖尿病人胰岛的胰岛素分泌。此外,BETP 与 GLP-1 组合显示出增加 GLP-1 受体信号传导的相加效应 [1]。 BETP 将胃酸调节素的效力提高 10 倍(EC50 为 80 pM)。 GLP-1 不会改变胃泌酸调节素和胰高血糖素对胰高血糖素受体的效力和功效。 BETP (0-30 μM) 增加胃泌酸调节素与 GLP-1 受体的结合亲和力[2]。
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体内研究 (In Vivo) |
BETP 对 SD 大鼠具有促胰岛素作用。 BETP(10 mg/kg,颈静脉插管)在静脉葡萄糖耐量试验 (IVGTT) 模型中表现出胰岛素促分泌活性。 BETP(10 mg/kg,静脉注射)治疗的大鼠需要增加 20% 的葡萄糖输注速度,并且在 SD 大鼠高血糖钳夹模型中显示出更高的血浆胰岛素水平[1]。 BETP (5 mg/kg) 增强胃泌酸调节素刺激的胰岛素分泌[2]。
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动物实验 |
Rats: The IVGTT research is carried out. Three male SD rats per cage are kept in groups in polycarbonate cages with filter tops. Rats are kept at 21°C on a 12:12 h light-dark cycle (lights come on at 6:00 a.m.), where they are given an unlimited supply of food and deionized water. Rats are fasted for the entire experiment and given 60 mg/kg of pentobarbital to put them to sleep. The jugular vein is punctured with a 0.84 mm catheter to administer glucose and compounds (BETP, etc.). A larger, 1.02 mm-diameter catheter is placed into the carotid artery to collect blood quickly. At times 0, 2, 4, 6, 10, and 20 minutes following intravenous administration of the BETP, blood is drawn for the measurement of glucose and insulin levels. An intravenous glucose bolus of 0.5 g/kg is then administered right away. Insulin and glucose plasma levels are measured[1].
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参考文献 |
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分子式 |
C20H17N2O2F3S
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分子量 |
406.42138
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精确质量 |
406.1
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CAS号 |
1371569-69-5
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外观&性状 |
Light yellow to yellow solid powder
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SMILES |
CCS(=O)C1=NC(=CC(=N1)C(F)(F)F)C2=CC(=CC=C2)OCC3=CC=CC=C3
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InChi Key |
NTDFYGSSDDMNHI-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C20H17F3N2O2S/c1-2-28(26)19-24-17(12-18(25-19)20(21,22)23)15-9-6-10-16(11-15)27-13-14-7-4-3-5-8-14/h3-12H,2,13H2,1H3
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化学名 |
2-ethylsulfinyl-4-(3-phenylmethoxyphenyl)-6-(trifluoromethyl)pyrimidine
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别名 |
BETP
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
DMSO: ~25 mg/mL (~61.5 mM)
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.15 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. 请根据您的实验动物和给药方式选择适当的溶解配方/方案: 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4605 mL | 12.3025 mL | 24.6051 mL | |
5 mM | 0.4921 mL | 2.4605 mL | 4.9210 mL | |
10 mM | 0.2461 mL | 1.2303 mL | 2.4605 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。