GLP-1R Agonist DMB
目录号 : KCM13119 CAS No. : 281209-71-0 纯度 : ≥98%
GLP-1R agonist DMB is an agonist of glucagon-like peptide 1 receptor (GLP-1R; K = 26.3 nM for the recombinant human receptor). It inhibits forskolin-induced cAMP accumulation in BHK cells expressing the recombinant human receptor with an EC value of 101 nM. GLP-1R (100 and 1,000 nM) increases insulin levels induced by D-(+)-glucose in pancreatic islets isolated from wild-type, but not Glp1r knockout, mice. It reduces fasting plasma glucose levels in mice when administered at a dose of 5 µmol/kg.
规格 价格 是否有货 数量
1mg
In-stock
5mg
In-stock
10mg
In-stock
25mg
In-stock

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生物活性

GLP-1R Agonist DMB  is an effective GLP-1R agonist that exerts its activating effect by forming hydrogen bonds with the Tyr42, Cys71, and Ser84 residues of GLP-1R. GLP-1R Agonist DMB has the potential for research in metabolic diseases such as type 2 diabetes and obesity.

体外研究

GLP-1R Agonist DMB (100 nM, 1000 nM) can activate GLP-1 receptor-mediated cAMP production, with an EC50 of 101 nM, but exhibits a self limiting effect at high concentrations .

GLP-1R Agonist DMB (100 nM) enhances the binding of GLP-1 to GLP-1 receptors and reduces the Kd value of GLP-1 (from 0.51 nM to 0.19 nM).

GLP-1R Agonist DMB (100 nM, 1000 nM) promotes glucose dependent insulin secretion in CD1 mouse islets, and this effect depends on the GLP-1 receptor. At concentrations of 100 nM and 1000 nM, GLP-1R Agonist DMB significantly enhances 10 mM glucose induced insulin secretion, similar to GLP-1, and this effect disappears in the islets of GLP-1 receptor knockout mice.

分子式
C13H15Cl2N3O2S
分子量
348.25
CAS号
281209-71-0
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro:

DMSO :25 mg/mL (71.79 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8715 mL 14.3575 mL 28.7150 mL
5 mM 0.5743 mL 2.8715 mL 5.7430 mL
10 mM 0.2872 mL 1.4358 mL 2.8715 mL
*

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, 6 months; -20°C, 1 month。-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。

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