GLP-1 (7-37) is a hormone secreted by glucagon cells that promotes glycogen breakdown and gluconeogenesis. It is a polypeptide composed of 30 amino acids, with a molecular weight of approximately 3700 Daltons. Under physiological conditions, Human glucagon like peptide-1 exists in monomeric form and has two important amino acid sequences: the A-chain composed of the 1st to 20th amino acids and the B-chain composed of the 21st to 30th amino acids. Easy to dissolve in water, its solubility in water is 2 mg/mL. In addition, Human glucagon like peptide-1 can also be dissolved in phosphate buffer with a pH of 7.4. Phosphate buffer has good stability and can remain stable for several days at room temperature. However, under acidic conditions, Human glucagon like peptide-1 is easily degraded by enzymes. In its natural state, it is a linear peptide. But under certain conditions, circular structures can be formed through disulfide bonds.
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Customized Bottle Caps And Corks:
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C.F |
C151H228N40O47 |
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E.M |
3354 |
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M.W |
3356 |
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m/z |
3355 (100.0%), 3356 (81.1%), 3354 (61.2%), 3357 (36.4%), 3356 (14.8%), 3357 (12.0%), 3358 (10.6%), 3357 (9.7%), 3355 (9.0%), 3358 (7.8%), 3357 (7.2%), 3358 (6.8%), 3356 (5.9%), 3358 (5.4%), 3359 (3.5%), 3359 (3.3%), 3356 (2.6%), 3359 (2.2%), 3357 (2.1%), 3356 (1.8%), 3355 (1.6%), 3359 (1.6%), 3357 (1.5%), 3358 (1.4%), 3359 (1.2%), 3355 (1.1%), 3360 (1.1%), 3357 (1.1%), 3358 (1.1%), 3360 (1.0%), 3359 (1.0%) |
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E.A |
C, 54.05; H, 6.85; N, 16.70; O, 22.41 |
GLP-1 (7-37) is a skin chain composed of 31 amino acids, hydrolyzed from pancreatic glucagon secreted by L-cells in the gastrointestinal tract. It is stimulated by the physical stimulation of food on the intestine and the secretion of neurotransmitters/plant nerves during feeding. It has the function of promoting insulin secretion, inhibiting pancreatic glucagon secretion, and regulating feeding.
Glucagon-like Peptide-1 (GLP-1), an endogenous intestinal hormone, plays a key role in regulating body weight through a multi-targeted mechanism. It mainly acts on the hypothalamus to modulate appetite signals and inhibits gastrointestinal functions like gastric emptying and gastric acid secretion, which synergistically reduce food intake and achieve weight loss. Below is an overview of its core regulatory mechanisms.
Hypothalamic Regulation: Balancing Satiety and Hunger
The hypothalamus is the central hub for energy homeostasis. GLP-1 crosses the blood-brain barrier and targets key hypothalamic nuclei, regulating two opposing neuron populations. It activates POMC neurons to secrete α-MSH, which transmits strong satiety signals; simultaneously, it inhibits NPY/AgRP neurons, reducing hunger-promoting signals. This dual regulation rebalances the appetite system, lowering the motivation to eat.
Gastrointestinal Regulation: Inhibiting Gastric Functions
GLP-1 significantly slows gastric emptying by regulating gastric smooth muscle, keeping food in the stomach longer to maintain a persistent feeling of fullness. This reinforces satiety and reduces between-meal snacking. It also reduces gastric acid secretion by inhibiting gastrin release and parietal cell activity, moderately slowing nutrient absorption and reducing total energy intake.
Synergistic Effect for Weight Loss
GLP-1's weight-reducing effect relies on the synergy of hypothalamic appetite regulation and gastrointestinal inhibition. These mechanisms collectively reduce food intake and energy absorption. Clinical trials confirm that long-term use of GLP-1 analogs achieves significant and sustainable weight loss (5-10% of baseline weight) in obese individuals, with concurrent improvements in metabolic indicators like blood glucose, highlighting its clinical value in obesity management.
The effect of Human glucagon like peptide-1 on blood pressure: Atrial Urinary Skin (ANP) dependent pathway.
GLP-1 acts on the GLP-1 (7-37) receptor on atrial myocardial cells, increasing CAMP levels and promoting Epac2 membrane translocation, thereby mediating the release of ANP. ANP mediates smooth muscle cell relaxation and vasodilation through CGMP, promotes renal excretion of sodium in urine, and ultimately leads to a decrease in blood pressure. The impact of Human glucagon like peptide-1 on blood lipids:
Acting on the liver
increasing liver B oxidation, reducing fat formation and fatty acid intake, thereby reducing liver steatosis, increasing macrophage activity, increasing cholesterol clearance, and ultimately reducing VLDL formation.
Acting on intestinal cells
Regulating lipid absorption and chylomicron synthesis at the intestinal cell level by regulating genes related to cholesterol and fatty acid uptake and transport.
Indirect effects
Human glucagon like peptide-1 stimulates insulin secretion in the pancreas, which can inhibit adipocyte lipolysis, leading to a decrease in free fatty acid levels and a decrease in intestinal chylomicron production. Human glucagon like peptide-1 inhibits gastric emptying and reduces intestinal glycerol absorption, thereby reducing chylomicron production.
Human glucagon like peptide-1 inhibits the absorption of glycerol by acting on intestinal sympathetic nervous system signals, interferes with the expression of genes involved in fat generation and glycerol storage, and reduces the formation of chylomicrons.Human glucagon like peptide-1 has a positive effect on cardiovascular function: through the kidneys, it increases sodium excretion and diuresis when sodium overload and volume expansion occur, reducing water and sodium retention in pigs.
Endogenous GLP-1 is rapidly degraded by DPP-IV enzyme (dikinase) in the body, with a half-cycle of only about 2 minutes, requiring continuous infusion for 24 hours to meet clinical treatment needs.
To overcome this drawback, the GLP-1 analogue (Liraglutide) underwent two modifications based on the endogenous structure of GLP-1: one added a 16 carbon palmitic acid side chain at position 26, and the other replaced arginine with lysine at position 34. This structural change causes slow absorption of its subcutaneous tissue, making it less susceptible to degradation by DPP-V enzymes. The half-life is extended to 13 hours, and the hypoglycemic effect can last for 24 hours, Meanwhile, due to the 97% homology between Liraglutide and human GLP-1, it rarely produces antibodies and has been widely used in clinical practice.
The mechanism of GLP-1 (7-37) blood glucose concentration dependent hypoglycemia is related to the dependence of protein kinase A (PKA) on glucose concentration by closing ion channels.
Human glucagon like peptide-1 binds to the GLP-1 receptor coupled with G protein on the B cell membrane, activating adenosine cyclase (AC) by stimulating G protein. After activation, adenylate cyclase (AC) can catalyze ATP to generate cyclic adenosine monophosphate (CAMP). CAMP is the second messenger that stimulates the release of insulin from B cells by GLP-1, and when the concentration of AMP increases, it activates protein kinase A (PKA).
The closure of potassium ion channels by PKA depends on glucose concentration, and only when ATP/ADP levels reach a certain level can potassium ion channels be closed, thereby assisting in triggering the initiation pathway. After triggering the activation pathway, cell membrane depolarization triggers the amplification pathway. GLP-1 can further act on the amplification pathway, slow down the inactivation of calcium ion channels, prolong the peak time of calcium ion concentration, increase calcium ion concentration, promote insulin containing vesicle exocytosis, and assist in lowering blood sugar. When glucose concentration decreases, the ratio of ATP to ADP decreases, making it insufficient to close potassium channels. The low ratio of ATP to ADP also prevents PKA from effectively acting on potassium channels. The initiation pathway of potassium channels cannot be triggered, therefore insulin cannot be released. So, GLP-1's ability to perceive changes in glucose concentration is a true glucose concentration dependent promotion of insulin secretion.
GLP-1(7-37) is a 31-amino-acid intestinal incretin hormone (officially known as human glucagon-like peptide-1). Its chemical properties cover multiple aspects such as molecular structure, physical state, solubility, stability, and reactivity. The following analysis will focus on the core chemical characteristics.
Molecular Structure and Composition
Amino Acid Sequence
The amino acid sequence of GLP-1(7-37) is:
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG (single-letter abbreviation) Or
His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-Gly-Arg-Gly (three-letter abbreviation).
This sequence is connected through amide bonds, forming a linear polypeptide chain, which contains multiple polar (such as Ser, Thr) and non-polar (such as Leu, Val) amino acids, giving it amphipathic characteristics.
Molecular formula and molecular weight
Molecular formula: C₁₅₁H₂₂₈N₄₀O₄₇
Molecular weight: 3355.72 Da (exact mass is 3355.666 Da, different sources may vary slightly due to calculation methods).
Its molecular weight is moderate and belongs to typical peptide compounds.
pH value and charge distribution
GLP-1(7-37) contains multiple acidic (such as Glu, Asp) and basic (such as Arg, Lys) amino acids. The isoelectric point (pI) is expected to be near neutral (the specific value needs to be experimentally determined). Under physiological pH (7.4), the molecule carries a negative charge and may bind to the cell membrane or receptor through electrostatic interactions.
Physical state and appearance
Appearance
GLP-1(7-37) is typically a white to off-white solid powder with a purity of ≥ 95% (detected by HPLC). The high-purity product is in a uniform powder form and contains no visible impurities or lumps.
Density and Refractive Index
Density: Predicted value is 1.48 ± 0.1 g/cm³ (slight fluctuations may occur due to differences in crystal forms from various sources).
Refractive Index: Predicted value is 1.660 (calculated based on molecular structure simulation).
These parameters reflect the degree of close packing in its solid state and its optical properties.
Solubility and Solvent Selection
Water Solubility
The solubility of GLP-1(7-37) in water is low (< 0.1 mg/mL), but it can be significantly improved by adjusting the pH:
Acidic conditions (pH ≈ 1): Solubility ≥ 50 mg/mL (14.90 mM) in 0.1 M HCl. Ultrasound-assisted treatment can further enhance solubility.
Neutral conditions: Solubility significantly decreases. Pure water should not be used for preparation directly.
Solubility in Organic Solvents
80% acetic acid/water solution: Solubility ≥ 10 mg/mL (2.98 mM), suitable for experiments requiring organic solvent assistance.
DMSO: Solubility < 1 mg/mL (almost insoluble or slightly soluble). Use with caution to avoid affecting the activity of the polypeptide.
Solubility Optimization Strategies
pH Adjustment: Acidic conditions (such as HCl) can break intermolecular hydrogen bonds, increasing solubility.
Ultrasound-Assisted Solubilization: Reduces aggregation through physical disruption, improving dissolution efficiency.
Stepwise Dissolution: Dissolve in a small amount of acidic solution first, then dilute to the target concentration.
Stability and Storage Conditions
Thermal stability
GLP-1(7-37) is temperature-sensitive. High temperatures (>25℃) can lead to degradation or aggregation. The recommended storage temperature is -20℃, and repeated freezing and thawing should be avoided.
Light stability
It needs to be stored in the dark (such as using a brown bottle or aluminum foil wrapping). Exposure to light may trigger photo-oxidation reactions, damaging the molecular structure.
Chemical stability
pH influence: It is prone to hydrolysis under extreme pH (such as strong acids or strong bases), losing its biological activity.
Oxidation sensitivity: It contains multiple oxidizable amino acids (such as Met, Trp), and needs to be operated under inert gas (such as nitrogen) protection.
Reaction Activity and Biological Function Correlation
Receptor binding activity
GLP-1(7-37) exerts its effect by activating the GLP-1 receptor (GLP-1R). The N-terminal (His⁷-Glu²¹) and C-terminal (Lys²⁸-Gly³⁷) regions are crucial for receptor binding. Chemical modifications (such as fatty acid chain connection) can prolong its half-life, but the key sites must remain active.
Enzyme hydrolysis sensitivity
It is easily degraded by dipeptidyl peptidase-4 (DPP-4), resulting in inactivation. The natural GLP-1(7-37) has a half-life of only 1-2 minutes and requires structural modification (such as the fatty acid side chain of liraglutide) to increase stability.
Bioactivity verification
Its ability to enhance insulin secretion is verified through cell experiments (such as INS-1 cells) or animal models (such as the hyperglycemic clamp experiment), confirming the direct correlation between chemical properties and biological functions.
FAQ
Who cannot take GLP-1?
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Patients with conditions such as depression or eating disorders may need additional considerations before starting GLP-1 therapy. In some cases, these medications can exacerbate mental health issues, so it is important to address these conditions alongside any weight loss treatment.
What does Ozempic do to your face?
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The rapid weight loss achieved with Ozempic can decrease facial volume, resulting in loose skin, lines and wrinkles, or a hollowed appearance becoming more prominent. There are a few factors to consider on your weight loss journey to help prevent Ozempic face. Dehydration can intensify the negative effects.
What is the cheapest way to get GLP-1?
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With Insurance: If your plan covers GLP-1s, your copay will be your cheapest option. FDA-Approved (Cash Price): Generic liraglutide is currently the cheapest glp 1 agonist that is fully FDA-approved and available for cash-paying patients.
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