GRA-Ex-25 - Glucagon Receptor 抑制劑 - 生命科學(xué)試劑 - 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作靶點: Glucagon Receptor作通路: GPCR/G Protein儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 32 mg/mL (56.78 mM)* means soluble

2、, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 GRA Ex-25種 glucagon 受體的抑制劑，抑制和的 glucagon 受體，IC50 值分別為 56 和

3、 55 nM。IC50 & Target IC50: 56 nM (rat glucagon receptor), 55 nM (human glucagon receptor) 2體外研究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 您邊的抑制劑師www.MedChemEEx-25 has similar affinity to the rat and human glucagon receptors (IC50=56 and 55 nM, respectively) 2.體內(nèi)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