GlpBio

Firuglipel

目录号: GC31508纯度: >99.00%同义词: DS-8500a
Firuglipel(DS-8500a)是高效，选择性，有口服活性的GPR119激动剂。
Firuglipel
Cas No.: 1371591-51-3
规格价格库存数量操作
250mg询价现货
1
500mg询价现货
1
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文献被引

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    641, 529–536 (2025)
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    632, 686–694 (2024)
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    618, 1017–1023 (2023)
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    610, 366–372 (2022)
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    Cell
    187(9):2288-2304 (2024)
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    Cell
    183(7):1867-1883 (2020)
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    388(6745) (2025)
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    387(6739) (2025)
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    387(6734) (2025)
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    33, 273–287 (2023)
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    33, 546–561 (2023)
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    33, 904–922 (2023)
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    31, 1291–1307 (2021)

产品描述 Description

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.

实验参考方法 Experimental Reference Method

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.

产品文档 Product Documents

Purity:>99.00%

化学性质Chemical Properties

CAS 号
1371591-51-3
同义词
DS-8500a
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 g/mol
溶解性
DMSO : 100 mg/mL (213.91 mM; Need ultrasonic)
保存条件
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°C，然后在超声波浴中震荡一段时间。
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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol