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作靶點: Glucagon Receptor作通路: GPCR/G Protein儲

2、存式: Protect from lightPowder -80C 2 years-20C 1 yearIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 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制備儲備液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；旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month (protect from light)。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍浮Ｒ韵氯芙獍付颊埾劝凑?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實

4、驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 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此案可獲得 2.5 mg/mL (0.72 mM) 的均勻懸濁液，懸濁液可于服和腹腔注射。

5、以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (0.72 mM); Precipitated solution; Need ultrasonic此案可獲得 2.5 mg/mL (0.72 mM)以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合

6、均勻。BIOLOGICAL ACTIVITY物活性 Glucagon (Porcine glucagon) 由胰腺 細胞產(chǎn)的種多肽激素。Glucagon 促進糖異1。Glucagon 降低 HNF-4 活性2。Glucagon 可促進 HNF4 磷酸化3。體外研究 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.體內(nèi)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、戶使本產(chǎn)品發(fā)表的科研獻 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