GRA-Ex-25 - Glucagon Receptor 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGRA Ex-25Cat. No.: HY-50675CAS No.: 307983-31-9分式: CHFNO分量: 563.61作靶点: Glucagon Receptor作通路: GPCR/G Protein储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 32 mg/mL (56.78 mM)* means soluble

2、, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.7743 mL 8.8714 mL 17.7428 mL5 mM 0.3549 mL 1.7743 mL 3.5486 mL10 mM 0.1774 mL 0.8871 mL 1.7743 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，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 GRA Ex-25种 glucagon 受体的抑制剂，抑制和的 glucagon 受体，IC50 值分别为 56 和

3、 55 nM。IC50 & Target IC50: 56 nM (rat glucagon receptor), 55 nM (human glucagon receptor) 2体外研究GRA Ex-25 binds a human glucagon receptor (h-GlucRbind) with Ki of 63 nM and a moderate glucagoninduced adenylate cyclase inhibition (h-GlucRcyclase) with Ki of 254 nM under our assay conditions 1. GRA1/2

4、Master of Small Molecules 您边的抑制剂师www.MedChemEEx-25 has similar affinity to the rat and human glucagon receptors (IC50=56 and 55 nM, respectively) 2.体内研究 GRA Ex-25 (3 mg/kg, i.v.) significantly reduces blood glucose caused by exogenous administration ofglucagon in rat model. GRA Ex-25 is able to inhi

5、bit the rise in blood glucose levels elicited by exogenousadministered glucagon, most likely because of the direct inhibition of glucagon stimulated hepatic glucoseoutput 2.PROTOCOLAnimal Non-fasted male Sprague Dawley rats (200 g) are maintained in the anaesthetized state during the test byAdminist

6、ration 2 s.c. administration of a 1:1 mixture of Hypnorm (fentanyl, 0.05 mg/mL and fluanizone, 2.5 mg/mL) andDormicum (Midazolam, 1.25 mg/mL). Acatheter is inserted in a jugular vein for administration of compounds.Approximately 60 min after initiation of anesthesia, test compounds (0, 1, 3, 10 and

7、30 mg/kg) and glucagon(3 g/kg) are administered in 5 min intervals, respectively. Samples for determination of blood glucoseconcentrations are taken from the tail tip 25 and 5 min prior to administration of the compound to representaverage basal values and again 10 min after administration of glucag

8、on (time for peak response ofglucagon). The results are expressed as delta values calculated as the value obtained 10 min after alucagonadministration minus the average of the two basal values.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1.

9、 Kurukulasuriya R, et al. Biaryl amide glucagon receptor antagonists. Bioorg Med Chem Lett. 2004 May 3;14(9):2047-50.2. Lau J, et al. New beta-alanine derivatives are orally available glucagon receptor antagonists. J Med Chem. 2007 Jan 11;50(1):113-28.McePdfHeightCaution: Product has not been fully validated for medical