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- Ribosomal S6 Kinase (RSK)
- GLP-1R Agonist DMB
GLP-1R Agonist DMB
A GLP-1R agonist
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包装价格促销价数量
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1mg￥412.00330.00- +
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5mg￥1962.001570.00- +
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10mg￥3412.002730.00- +
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25mg￥8200.006560.00- +
- 货号: ajcx20634
- CAS: 281209-71-0
- 别名:
- 分子式: C13H15Cl2N3O2S
- 分子量: 348.2
- 纯度: ＞98%
- 溶解度: Soluble in DMSO
- 储存: Store at -20°C
- 库存: 现货
Background
GLP-1R agonist DMB is an agonist of glucagon-like peptide 1 receptor (GLP-1R; KB = 26.3 nM for the recombinant human receptor).1 It inhibits forskolin-induced cAMP accumulation in BHK cells expressing the recombinant human receptor with an EC50 value of 101 nM.2 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.3
|1. Koole, C., Wootten, D., Simms, J., et al. Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner: Implications for drug screening. Mol. Pharmacol. 78(3), 456-465 (2010).|2. Knudsen, L.B., Kiel, D., Teng, M., et al. Small-molecule agonists for the glucagon-like peptide 1 receptor. Proc. Natl. Acad. Sci. USA 104(3), 937-942 (2007).|3. Irwin, N., Flatt, P.R., Patterson, S., et al. Insulin-releasing and metabolic effects of small molecule GLP-1 receptor agonist 6,7-dichloro-2-methylsulfonyl-3-N-tert-butylaminoquinoxaline. Eur. J. Pharmacol. 628(1-3), 268-273 (2010).
