Firuglipel
(Synonyms: DS-8500a) 目录号 : GC31508
Firuglipel(DS-8500a)是高效，选择性，有口服活性的GPR119激动剂。
Cas No.:1371591-51-3
Sample solution is provided at 25 µL, 10mM.
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Firuglipel (DS-8500a) is an orally available, potent and selective GPR119 agonist.
Firuglipel (DS-8500a) increases intracellular cAMP in a concentration-dependent manner in human, rat, and mouse GPR119-expressing Chinese hamster ovary (CHO)-K1 cells, with EC50 values of 51.5, 98.4, and 108.1 nM, respectively. DS-8500a has no effect on intracellular cAMP in pcDNA3.1/CHO-K1 cells[1].
Firuglipel (DS-8500a) (1-30 mg/kg) upregulates glucagon-like peptide-1 and enhances glucose-dependent insulin secretion and improves glucose homeostasis in type 2 diabetic rats[1].
[1]. Matsumoto K, et al. DS-8500a, an Orally Available G Protein-Coupled Receptor 119 Agonist, Upregulates Glucagon-Like Peptide-1 and Enhances Glucose-Dependent Insulin Secretion and Improves Glucose Homeostasis in Type 2 Diabetic Rats. J Pharmacol Exp Ther. 2018 Dec;367(3):509-517.
Animal experiment: | Rats[1]Male SD rats (8 weeks) are fasted overnight and orally given vehicle (0.5% MC), DS-8500a (0.1, 1, 3 and 10 mg/kg), or glimepiride (10 mg/kg). Thirty minutes later, all animals received a 50% glucose solution intravenously (glucose load: 0.5 g/kg). Blood collection is performed from the tail vein 35 minutes before, 5 minutes before, and 5 minutes after the glucose load. The plasma insulin concentration is measured using ELISA kits. |
References: [1]. Matsumoto K, et al. DS-8500a, an Orally Available G Protein-Coupled Receptor 119 Agonist, Upregulates Glucagon-Like Peptide-1 and Enhances Glucose-Dependent Insulin Secretion and Improves Glucose Homeostasis in Type 2 Diabetic Rats. J Pharmacol Exp Ther. 2018 Dec;367(3):509-517. | |
| Cas No. | 1371591-51-3 | SDF | |
| 别名 | DS-8500a | ||
| Canonical SMILES | CC[C@H](C1=NC(C2=CC(F)=C(C(N[C@H](C)CO)=O)C=C2)=NO1)OC3=CC=C(C(C4CC4)=O)C=C3 | ||
| 分子式 | C25H26FN3O5 | 分子量 | 467.49 |
| 溶解度 | DMSO : 100 mg/mL (213.91 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1391 mL | 10.6954 mL | 21.3908 mL |
| 5 mM | 0.4278 mL | 2.1391 mL | 4.2782 mL |
| 10 mM | 0.2139 mL | 1.0695 mL | 2.1391 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
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 saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet