Name | glucagon |
Synonyms | glucagon GLUCAGON 37 GLUCAGON 1-37 Glucagon 1-29 GLUCAGON ACETATE Glucagon(1-29) Human HCl GLUCAGON (1-37) (PORCINE) Glucagon, human recombinant Glucagon Hydrochloride(Human) HSQGTFTSDYSKYLDSRRAQDFVQWLMNTKRNKNNIA Glucagon (1-29) (human, bovine, porcine) H-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-Thr-OH H-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-THR-LYS-ARG-ASN-LYS-ASN-ASN-ILE-ALA-OH L-histidyl-L-seryl-L-glutaminylglycyl-L-threonyl-L-phenylalanyl-L-threonyl-L-seryl-L-alpha-aspartyl-L-tyrosyl-L-seryl-L-lysyl-L-tyrosyl-L-leucyl-L-alpha-aspartyl-L-seryl-L-arginyl-L-arginyl-L-alanyl-L-glutaminyl-L-alpha-aspartyl-L-phenylalanyl-L-valyl-L-glutaminyl-L-tryptophyl-L-leucyl-L-methionyl-L-asparaginyl-L-threonine |
CAS | 16941-32-5 9007-92-5 |
EINECS | 685-611-6 |
InChI | InChI=1/C153H225N43O49S/c1-72(2)52-97(133(226)176-96(47-51-246-11)132(225)184-104(60-115(159)209)143(236)196-123(78(10)203)151(244)245)179-137(230)103(58-83-64-167-89-29-19-18-28-87(83)89)183-131(224)95(43-46-114(158)208)177-148(241)120(74(5)6)194-141(234)101(54-79-24-14-12-15-25-79)182-138(231)105(61-117(211)212)185-130(223)94(42-45-113(157)207)171-124(217)75(7)170-127(220)91(31-22-49-165-152(160)161)172-128(221)92(32-23-50-166-153(162)163)174-146(239)110(69-199)191-140(233)107(63-119(215)216)186-134(227)98(53-73(3)4)178-135(228)99(56-81-33-37-85(204)38-34-81)180-129(222)90(30-20-21-48-154)173-145(238)109(68-198)190-136(229)100(57-82-35-39-86(205)40-36-82)181-139(232)106(62-118(213)214)187-147(240)111(70-200)192-150(243)122(77(9)202)195-142(235)102(55-80-26-16-13-17-27-80)188-149(242)121(76(8)201)193-116(210)66-168-126(219)93(41-44-112(156)206)175-144(237)108(67-197)189-125(218)88(155)59-84-65-164-71-169-84/h12-19,24-29,33-40,64-65,71-78,88,90-111,120-123,167,197-205H,20-23,30-32,41-63,66-70,154-155H2,1-11H3,(H2,156,206)(H2,157,207)(H2,158,208)(H2,159,209)(H,164,169)(H,168,219)(H,170,220)(H,171,217)(H,172,221)(H,173,238)(H,174,239)(H,175,237)(H,176,226)(H,177,241)(H,178,228)(H,179,230)(H,180,222)(H,181,232)(H,182,231)(H,183,224)(H,184,225)(H,185,223)(H,186,227)(H,187,240)(H,188,242)(H,189,218)(H,190,229)(H,191,233)(H,192,243)(H,193,210)(H,194,234)(H,195,235)(H,196,236)(H,211,212)(H,213,214)(H,215,216)(H,244,245)(H4,160,161,165)(H4,162,163,166)/t75-,76+,77+,78+,88-,90-,91-,92-,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,107-,108-,109-,110-,111-,120-,121-,122-,123-/m0/s1 |
Molecular Formula | C153H225N43O49S |
Molar Mass | 3482.75 |
Density | 1.53±0.1 g/cm3(Predicted) |
Solubility | Practically insoluble in water and in most organic solvents. It is soluble in dilute mineral acids and in dilute solutions of alkali hydroxides. |
Appearance | powder |
Storage Condition | Keep in dark place,Sealed in dry,2-8°C |
WGK Germany | 3 |
FLUKA BRAND F CODES | 3-10-21 |
HS Code | 2937190000 |
This product is twenty-nine peptide. Secreted by insulin A cells. When hypoglycemia, its secretion is normal, and the plasma half-life is about 3~6min. It is mainly inactivated in the liver, followed by the kidney and blood. Zinc-containing glucagon has a longer duration of action. The release of glucagon in the human body during severe stress is undoubtedly a physiological self-protective effect. Such as large area Burns, acute myocardial infarction with cardiogenic Shock, acute pancreatitis and after surgery, plasma concentrations increased significantly. Pancreatic Islet A- cell hyperplasia or tumor also releases large amounts of glucagon.
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 0.287 ml | 1.436 ml | 2.871 ml |
5 mM | 0.057 ml | 0.287 ml | 0.574 ml |
10 mM | 0.029 ml | 0.144 ml | 0.287 ml |
5 mM | 0.006 ml | 0.029 ml | 0.057 ml |
Straight chain peptide hormone | Glucagon, also known as glucagon and glucagon, is a straight chain peptide hormone secreted by islet alpha cells, containing 29 amino acids, molecular formula and relative molecular mass are C153H225N43O49S = 3482.8. Our country has artificially synthesized this hormone. White fine crystalline powder at room temperature, odorless and tasteless. It is almost insoluble in water and most organic solvents, soluble in dilute acid and dilute lye. The preparation mostly uses its hydrochloride, which is soluble in water. It is now known that glucagon must maintain molecular integrity in order to exert its physiological activity. The structure of glucagon in humans and mammals (rabbits, cattle, pigs, rats, etc.) may be the same, but slightly different in birds. It is an important hormone to maintain normal blood sugar. Its main function is to activate phosphorylase in the myocardium, promote glycogen decomposition and have a catecholamine-like effect. Therefore, it has a heart-strengthening effect on the heart, increasing heart rate and myocardial contractility. Increased coronary blood flow. The cardiotonic effect is not accompanied by an increase in the excitability of the heart, but increases the calcium ions entering the cardiomyocytes, and can activate the adenosine cyclase on the liver cell membrane, and promote the synthesis of cyclic adenosine phosphate in the cell. It is reported that glucagon has a certain effect on some cases of heart failure. In addition, in the case of diabetes, liver disease, kidney disease, glucagonoma and stress, the plasma level also increases to varying degrees. Glucagon has four physiological functions of promoting liver glycogen decomposition, liver glycogen heterogenesis, lipolysis and ketone body formation. It can promote the uptake of amino acids by liver cells, accelerate the deamination and oxidation process of amino acids in the liver, reduce the concentration of plasma amino acids, reduce protein synthesis, and promote liver glycogen eogenesis. In addition, it can also activate the lipase ability of lipid storage cells in the liver, increase the release of free fatty acids, accelerate the lipid acid oxidation process of liver cells, and also increase the production of liver glycogen and ketone bodies. At the same time, glucagon can also inhibit the tension and peristalsis of the stomach, small intestine, and colon, reduce the tension of the gallbladder, inhibit pancreatic exocrine, and inhibit the absorption of water and salt by the intestinal mucosa. High doses of glucagon can also increase the concentration of cAMP in myocardial cells, increase heart rate and increase myocardial contractility. |
Pharmacological effects | The main role of glucagon is to promote glycogenolysis and produce glucose to increase blood sugar; secondly, it can also increase the level of cyclic adenosine phosphate (cAMP) through adenylate cyclase, thereby activating protein kinase, activating lipase in adipose tissue, and promoting lipolysis; activating myocardial adenylate cyclase system, promote the activity of myocardial phosphorylase, increase the accumulation of calcium in the myocardium, thereby enhancing myocardial contractility, increasing cardiac output and raising blood pressure; it can also promote the secretion of insulin, somatostatin, thyroxine and calcitonin; Promote the release of catecholamines from sympathetic nerves and chromaffin cells. Glucagon, insulin and somatostatin regulate each other to maintain blood sugar in the normal range. The secretion of glucagon is inversely proportional to the concentration of blood glucose. At the same time, the secretion of glucagon is also affected by the content of amino acids, plasma free fatty acids, α-adrenergic receptor stimulators (norepinephrine), Auxin release inhibitory hormones, etc. glucagon is a single-chain polypeptide hormone synthesized and secreted by islet α2 cells. It is a physiological antagonist of insulin. The effect on metabolism is similar to that of epinephrine, which has the following effects: 1. Elevating blood sugar: It can activate liver phosphorylase, promote liver glycogen decomposition and glycogen xenogenesis, and increase blood sugar. 2. Positive inotropic effect: It can increase the content of cAMP in cells, enhance myocardial contractility, and increase cardiac output and stroke work. Its positive inotropic effect can still be exerted after the application of sufficient cardiac glycosides, and is not blocked by propranolol. Although it can increase heart rate and increase blood pressure, it will not cause arrhythmia. Its production mechanism is: ①Activate adenylate cyclase to convert adenosine triphosphate into cyclized adenosine monophosphate, which enhances myocardial contractility; ②Promote liver glycogen decomposition and increase blood sugar levels; ③Promote insulin release and improve myocardial glucose Utilization, and promote anaerobic glycolysis of the myocardium, thereby improving the energy metabolism of the myocardium. In combination with digitalis cardiac glycosides, can increase the efficacy. 3. Effect on kidney: dilate renal blood vessels, improve renal blood flow, and promote the excretion of sodium, potassium and calcium. 4. Effect on the digestive system: It can cause the smooth muscle relaxation of the stomach, duodenum, small intestine and colon, inhibit the peristalsis of the stomach, small intestine and colon, and increase the secretion of bile and intestinal fluid. 5. The effect on the secretory system: excites the adrenal medulla and promotes the release of catecholamines. It can also promote the secretion of insulin, thyroid hormone, calcitonin and growth hormone. |
indications | this product is invalid for oral administration, and more injections are given. The body effect is short, it takes effect 5 minutes after intravenous injection, blood sugar can increase by 50% within 30 minutes, and the effect can last for about 1 hour. Mainly inactivated in liver, kidney and plasma, plasma half-life of 3~6 minutes. It is clinically used in insulin-dependent diabetic patients with severe hypoglycemia and coma and cannot be eaten. It is also used to measure pancreatic function and assist in the diagnosis of islet tumors and pheochromocytoma. The circulatory system is mainly used for acute heart failure, heart failure that is ineffective in digitalis treatment, and heart failure with cardiogenic shock. The effect of glucagon on chronic heart failure is poor. The main indications are as follows: ① Acute low emission syndrome. ② Acute heart failure or cardiogenic shock caused by coronary heart disease and cardiomyopathy. ③ combined with propranolum to treat arrhythmia caused by digitalis poisoning. |
usage and dosage | 3~5mg is given for the first time, and glucose solution is added for intravenous injection. if there is no adverse reaction after 2~5min, intravenous drip at a speed of 2.5~10 mg/h can be used. Intravenous medication took effect for 1~3min, reached a peak in 10min, disappeared in 30min, and could be applied continuously for 24 hours depending on the condition. intramuscular injection, subcutaneous injection or intravenous injection: hypoglycemic coma, 0.5~1mg each time, give medicine every 20 minutes when necessary. 5~20 minutes can be effective. If it is still ineffective after 1 hour, glucose should be used as soon as possible. 25 μg/kg for children. intravenous drip: dilute with 5% glucose injection and then drip. Congestive heart failure, 2.5~7.5mg per hour. Cardiogenic shock, 1~12mg per hour, if the condition requires, 24 hours of intravenous drip. |
adverse reactions | excessive dosage or too fast injection can cause nausea and vomiting. It can also cause hypokalemia, hyperglycemia and bleeding tendency. |