|2-((2-(4-溴苯基)-6-甲基嘧啶-4-基)氨基)乙醇|CsnPharm

CAS No.: 330981-72-1

AS1269574 Catalog No. CSN23765

AS 1269574 is a GPR119 receptor agonist with EC50 of 2.5 μM in HEK293 cells expressing human GPR119.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述GPR119 is a G protein-coupled receptor expressed on intestinal L cells that synthesize and secrete the blood glucose-lowering hormone glucagon-like peptide-1 (GLP-1)^[1]. The GPR119 expression was markedly increased in preosteoclasts and then downregulated in mature osteoclasts. Activation of GPR119 with AS1269574 inhibited the generation of multinuclear osteoclasts from bone marrow-derived macrophages. GPR119 activation attenuated the expression of c-Fos and nuclear factor of activated T cells cytoplasmic 1 (NFATc1) and blocked RANKL-stimulated phosphorylation of IκBα, c-Jun N-terminal protein kinase (JNK), and extracellular signal-regulated kinase (ERK) but not p38^[2]. AS1269574 is a potent, orally available GPR119 agonist. AS1269574 has the potential for the research of type 2 diabetes. AS1269574 had an EC(50) value of 2.5μM in HEK293 cells transiently expressing human GPR119 and enhanced insulin secretion in the mouse pancreatic β-cell line MIN-6 only under high-glucose (16.8mM) conditions. This contrasted with the action of the sulfonylurea glibenclamide, which also induced insulin secretion under low-glucose conditions (2.8mM). AS1269574 had an EC(50) value of 2.5μM in HEK293 cells transiently expressing human GPR119 and enhanced insulin secretion in the mouse pancreatic β-cell line MIN-6 only under high-glucose (16.8mM) conditions. This contrasted with the action of the sulfonylurea glibenclamide, which also induced insulin secretion under low-glucose conditions (2.8mM). In in vivo studies, a single administration of AS1269574 to normal mice reduced blood glucose levels after oral glucose loading based on the observed insulin secretion profiles. Significantly, AS1269574 did not affect fed and fasting plasma glucose levels in normal mice^[3].
参考文献

[1] Oleg G Chepurny,et al. GPR119 Agonist AS1269574 Activates TRPA1 Cation Channels to Stimulate GLP-1 Secretion. Mol Endocrinol. 2016 Jun;30(6):614-29.
[2] Hyun-Ju Kim,et al. G protein-coupled receptor 119 is involved in RANKL-induced osteoclast differentiation and fusion. J Cell Physiol.2019 Jul;234(7):11490-11499.
[3] Yoshida S, et al. Identification of a novel GPR119 agonist, AS1269574, with in vitro and in vivo glucose-stimulated insulin secretion. Biochem Biophys Res Commun. 2010;400(3):437-441.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.2450 mL
- 16.2248 mL
- 32.4496 mL
- 5 mM
- 0.6490 mL
- 3.2450 mL
- 6.4899 mL
- 10 mM
- 0.3245 mL
- 1.6225 mL
- 3.2450 mL

技术信息

CAS号	330981-72-1	储存条件	粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C13H14BrN3O	运输	蓝冰
分子量	308.17	别名

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

AS1269574 Catalog No. CSN23765

靶点选择性

请登录您的专属账户

确认信息