胰高血糖素作用机制 - Medchemexpress - MCE中国

1、Product Data SheetGlucagonCat. No.: HY-P0082CAS No.: 16941-32-5分式: CHNOS分量: 3482.75Sequence: His-Ser-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Lys-Tyr-Leu-Asp-Ser-Arg-Arg-Ala-Gln-Asp-Phe-Val-Gln-Trp-Leu-Met-Asn-ThrSequence Shortening: HSQGTFTSDYSKYLDSRRAQDFVQWLMNT作靶点: Glucagon Receptor作通路: GPCR/G Protein储

2、存式: Protect from lightPowder -80C 2 years-20C 1 yearIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (14.36 mM; Need ultrasonic)H2O : 20 mg/mL (5.74 mM; ultrasonic and adjust pH to 2 with HCl)H2O : 0.1 mg/mL (insoluble)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 0.2871 mL 1.4356 mL

3、 2.8713 mL5 mM 0.0574 mL 0.2871 mL 0.5743 mL10 mM 0.0287 mL 0.1436 mL 0.2871 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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month (protect from light)。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实

4、验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (0.72 mM); Suspended solution; Need ultrasonicPage 1 of 2 www.MedChemE此案可获得 2.5 mg/mL (0.72 mM) 的均匀悬浊液，悬浊液可于服和腹腔注射。

5、以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (0.72 mM); Precipitated solution; Need ultrasonic此案可获得 2.5 mg/mL (0.72 mM)以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合

6、均匀。BIOLOGICAL ACTIVITY物活性 Glucagon (Porcine glucagon) 由胰腺 细胞产的种多肽激素。Glucagon 促进糖异1。Glucagon 降低 HNF-4 活性2。Glucagon 可促进 HNF4 磷酸化3。体外研究 Upon binding to its receptor Gcgr, Glucagon activates cAMP-PKA signaling to stimulate hepatic glucose production(HGP) and cause hyperglycemia1.Glucagon stimulates both

7、 hepatic kisspeptin1 production and gluconeogenesis1.Glucagon (100 nM) represses CYP7A1 mRNA expression in human primary hepatocytes3.Glucagon (100 nM) increases phosphorylayion of HNF43.Western Blot Analysis3Cell Line: Human primary hepatocytes (H1211, HH1215)Concentration: 100 nMIncubation Time:Re

8、sult: Resulted in a marked increase in the amount of phosphorylated HNF4.体内研究 Low-dose (20 g/kg) Glucagon increases glycemia and does not stimulate insulin secretion in ambient-fed mice.High-dose (1 mg/kg) Glucagon lowers glycemia compared with PBS control and stimulates insulin secretion inambient-

9、fed mice4.Animal Model: C57BL/6J mice (12- to 24-week-old)4Dosage: 20 g/kg and 1 mg/kgAdministration: Administered by i.p. injection; 45 minutesResult: Low-dose (20 g/kg) increased glycemia and did not stimulate insulin secretion.High-dose (1 mg/kg) lowered glycemia and stimulated insulin secretion.

10、户使本产品发表的科研献 Proc Natl Acad Sci U S A. 2020 Feb 11;117(6):3144-3149.See more customer validations on HYPERLINK www.MedChemE www.MedChemEPage 2 of 3 www.MedChemEREFERENCES1. Song WJ, et al. Glucagon regulates hepatic kisspeptin to impair insulin secretion. Cell Metab. 2014 Apr 1;19(4):667-81.2. Hirota

11、 K, et al. Hepatocyte nuclear factor-4 is a novel downstream target of insulin via FKHR as a signal-regulated transcriptional inhibitor. J Biol Chem.2003 Apr 11;278(15):13056-60.3. Song KH, et al. Glucagon and cAMP inhibit cholesterol 7alpha-hydroxylase (CYP7A1) gene expression in humanhepatocytes: discordant regulation of bileacid synthesis and gluconeogenesis. Hepatology. 2006 Jan;43(1):117-25.4. Capozzi ME, et al. Glucagon lowers glycemia when -cells are active. JCI Insight. 2019 Jul 23;5. pii: 129954.McePdfHeightCaution: Product has not been full