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Lypressin vasopressin (also known as vasopressin) is a 9-peptide hormone secreted by nerve cells in the supraoptic and paraventricular nuclei of the hypothalamus, which is released after reaching the posterior lobe of the neurohypophysis through the hypothalamic pituitary tract. Molecular formula C46H65N13O12S2, CAS 50-57-7.
It usually exists in the form of white or slightly yellowish crystalline powder. This powder is stable at room temperature, not easily hygroscopic, and is easy to store and transport. Its form is amorphous powder, with fine particles and good fluidity. It has good solubility in water and can form a clear and transparent solution. Under different pH conditions, its solubility may vary, but it usually maintains a high solubility within the physiological pH range.It exhibits good stability at room temperature and is not easily affected by light, heat, and humidity, leading to decomposition or deterioration. However, its stability may be affected to some extent in high temperature or humid environments.
Customized Bottle Caps And Corks:
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Products Forms
lypressin COA
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| Certificate of Analysis | ||
| Compound name | lypressin | |
| Grade | Pharmaceutical grade | |
| CAS No. | 50-57-7 | |
| Quantity | Customized | |
| Packaging standard | Customized | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 202501090065 | |
| MFG | Jan 9th 2026 | |
| EXP | Jan 8th 2029 | |
| Structure |  |
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| Item | Enterprise standard | Analysis result |
| Appearance | White or almost white powder | Conformed |
| Water content | ≤5.0% | 0.54% |
| Loss on drying | ≤1.0% | 0.42% |
| Heavy Metals | Pb≤0.5ppm | N.D. |
| As≤0.5ppm | N.D. | |
| Hg≤0.5ppm | N.D. | |
| Cd≤0.5ppm | N.D. | |
| Purity (HPLC) | ≥99.0% | 99.98% |
| Single impurity | <0.8% | 0.52% |
| Total microbial count | ≤750cfu/g | 95 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 500ppm |
| Storage | Store in a sealed, dark, and dry place below -20°C | |
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Therefore, during storage and use, attention should be paid to avoiding high temperatures and dampness, maintaining dryness and cleanliness. The small molecular weight allows it to quickly penetrate the cell membrane and exert its effects. Its molecular structure contains multiple functional groups, including amide bonds, carboxyl groups, and amino groups, which play important roles in drug receptor binding and drug metabolism in the body. Its main function is to improve the permeability of the collection tube to water, promote water absorption, and is a key regulatory hormone for urine concentration and dilution. In addition, this hormone can also enhance the permeability of the inner medullary collecting duct to urea.
Lypressin vasopressin (Lysiparessin) is a peptide compound synthesized by chemically modifying natural vasopressin (AVP). Its core structural feature is the substitution of arginine at the 8th position of the original molecule with lysine, and the formation of a prodrug by binding three glycerols at the N-terminus. This substance releases active ingredients after enzymatic hydrolysis in the body, selectively activating V1 receptors on vascular smooth muscle and V2 receptors on renal collecting duct epithelial cells, exerting pharmacological effects such as constriction of visceral blood vessels, regulation of portal pressure, and promotion of water reabsorption.
Clinical Treatment: Core Indications and Therapeutic Mechanisms
1. Precise treatment of complications of liver cirrhosis
(1) Esophageal variceal bleeding
By activating the visceral vascular smooth muscle V1 receptor, portal vein blood flow is reduced by 35%, significantly reducing the risk of varicose vein rupture. Clinical trials have shown that its success rate in controlling acute esophageal variceal bleeding is 76% -85%, much higher than traditional drugs (such as 65% -70% of somatostatin analogs). The mechanism is to selectively contract the splenic artery while dilating the renal artery, increasing the glomerular filtration rate by 56%, maintaining renal perfusion while reducing portal pressure, and reducing the risk of hepatorenal syndrome.
(2) Hepatorenal syndrome
In a multicenter study conducted in 2017, the complete remission rate of serum creatinine in patients with hepatorenal syndrome was 56%, which was 11 times higher than the control group (5%). It reduces intestinal congestion and improves renal hemodynamics by constricting visceral blood vessels, while inhibiting renin-angiotensin system activity and reducing renal vascular resistance. The standard dosing regimen is intravenous injection of 1-2mg every 4-6 hours, and blood sodium levels should be monitored to prevent electrolyte imbalance.
2. Auxiliary strategies for shock treatment
(1) Septic shock
Improving organ perfusion by increasing mean arterial pressure (MAP) is particularly suitable for patients who do not respond to fluid resuscitation. Compared with norepinephrine, the incidence of adverse reactions such as coronary artery constriction was reduced to 2.3%, and it did not increase myocardial oxygen consumption. A randomized controlled trial involving 200 patients showed that the combined use of vasopressin can increase the oxygenation index (PaO ₂/FiO ₂) from (180 ± 30) mmHg to (250 ± 40) mmHg and shorten mechanical ventilation time by 40%.
(2) Cardiogenic shock
In the emergency treatment of acute myocardial infarction complicated with cardiogenic shock, it acts on peripheral blood vessels to regulate vasoconstriction, effectively reduce excessive cardiac output, lower left ventricular preload, and significantly enhance weakened myocardial contractility. Relevant pharmacological animal experiments have fully verified its efficacy, confirming that it can increase cardiac output by 15%–20%.
Special indications: from underlying diseases to behavioral regulation
1. Differentiated treatment of diabetes insipidus
(1) Central diabetes insipidus
Lysine vasopressin spray (1-2 sprays each time, 3-5 times a day) can promote the reabsorption of water in renal tubules by activating V2 receptor, and reduce urine volume by 50% -70%. Its antidiuretic effect is about 50% stronger than natural AVP, but its vasoconstrictive properties only manifest at high doses, making it safer for mild to moderate patients. A long-term follow-up study showed that the blood sodium concentration of patients taking standardized medication remained stable at (140 ± 5) mmol/L, and the frequency of dehydration attacks decreased by 80%.
(2) Renal diabetes insipidus
Due to the dysfunction of V2 receptors in patients with renal diabetes insipidus, the therapeutic effect is limited, but it can be enhanced by the combined use of thiazide diuretics (such as hydrochlorothiazide). The mechanism is that thiazide compounds indirectly increase the expression of aquaporin 2 (AQP2) by reducing renal tubular sodium reabsorption, and have a synergistic effect with lysine vasopressin.
2. Exploratory applications of neurobiological functions
(1) Animal behavior regulation
In the grassland vole model, blocking the brain's vasopressin receptor resulted in 90% of individuals losing specificity to their original mate.
Supplementing injection of this substance can restore partner recognition ability in the experimental mice. The mechanism may be related to the "chemical partner binding" effect of dopamine release in the hypothalamus, providing a molecular level explanatory model for studying animal social behavior.
(2) Anti injury activity
In the rat hot plate experiment, the latency of tail flick reaction was significantly prolonged (from 5.2 seconds to 8.7 seconds), which was achieved by activating the V1 receptor in spinal dorsal horn neurons. In addition, in the uterine muscle layer of pigs, it can enhance contractility by increasing intracellular calcium ion concentration, suggesting potential applications in obstetrics.
The chemical equation for the synthesis of precursor peptide chains and subsequent modification steps (expressed in simplified form)
-Activated amino acids: H2N-AA1-COOH+activator → AA1-O-activator
-Activated peptide chain: AA1-O-activator+H2N-AA2-COOH → AA1-AA2-O-activator
-Repeat the above steps until the complete precursor peptide chain is synthesized.
-Removing protective groups: Dmoc Arg → Arg
-Oxidation reaction: AA1-AA2-AA3-S-AA4-AA5 → AA1-AA2-AA3-S-AA4-AA5
-Dissolution and recrystallization: AA1-AA2-AA3-S-AA4-AA5+solvent → Crystals
-Separation and purification: Crystals+separation and purification reagents ->Pure Vasopressin
It should be noted that the laboratory synthesis method of Lypressin is complex and cumbersome, and may involve specific experimental conditions and reagent selection. Therefore, in practical operation, there may be some detailed steps and reaction conditions that need to be adjusted and optimized according to specific circumstances.
Research Applications: Tool Drugs and Model Construction
Receptor pharmacology research:
As a selective agonist of V1/V2 receptors, it is widely used in receptor binding experiments. Its affinity for V1 receptors is three times that of V2 receptors, making lypressin commonly used to distinguish receptor subtype functions. For example, in ex vivo vascular strip experiments, it can contract rat aortic rings in a concentration dependent manner (EC50=0.3nM), while its antidiuretic effect requires a higher concentration (EC50=10nM).
Construction of disease models:
In a rat model of portal hypertension caused by cirrhosis, continuous infusion of vasopressin (0.1mg/kg/h) can reduce portal vein pressure from (18 ± 2) cmH ₂ O to (12 ± 1) cmH2O without causing systemic blood pressure fluctuations. This model provides a stable platform for evaluating novel portal antihypertensive drugs.
Intermediate for drug synthesis:
It can be used as a key intermediate for the synthesis of terlipressin (N - α - triglycosyl-8-lysine-pressin). Terlipressin prolongs its half-life to 6 hours through triglyceride modification and is a first-line drug for treating variceal bleeding in liver cirrhosis. In 2023, the global market size of terlipressin will reach 1.2 billion US dollars, with lysine vasopressin intermediates accounting for over 30%.
Vasopressin (AVP) is an important endogenous neuropeptide hormone that has functions such as regulating water balance, vasoconstriction, and anti diuresis in the human body.
The laboratory synthesis usually involves two main steps: synthesis of precursor peptide chains and subsequent modification. The following are the detailed steps:
Step 1: Synthesize precursor peptide chains
1. Select appropriate protective groups and activators to synthesize the precursor peptide chain of AVP through solid-phase synthesis.
2. During the synthesis process, lysine is protected as needed, such as by selecting dimethylsilyl (Dmoc) to form a protective peptide chain.
3. Use appropriate activators (such as carbon disulfide and dimethylpyrrolidone) to activate amino acids and connect the protective peptide chain with other amino acids;Repeat the above steps until the complete precursor peptide chain is synthesized.
Step 2: Subsequent modifications
After the synthesis of the precursor peptide chain is completed, a series of subsequent modification steps are required, including deprotection, oxidation, dissolution, and recrystallization.
Remove the protective group of lysine. Appropriate protective reagents such as trifluoroacetic acid (TFA) can be used to remove the Dmoc protective group from lysine, resulting in unprotected lysine.
Conduct oxidation reaction. By using appropriate oxidants such as acetic acid hydrogen peroxide (AcOH/H2O2), the precursor peptide chains undergo oxidation reactions to form disulfide bonds.
Dissolve and recrystallize the oxidized product to improve purity.Finally, through appropriate separation and purification technologies, such as chromatography, gel filtration chromatography, etc., pure lysine vasopressin is obtained.
FAQ
What are the essential differences in physiological adaptation between lypressin and endogenous arginine vasopressin in the human body?
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Answer: The active substance is in a nine peptide configuration, and its molecular sequence is highly homologous to the natural antidiuretic factor derived from pigs. It only has slight differences in the amino acid arrangement at specific sites with arginine vasopressin, which is the main regulator of water and salt regulation in the human body; The physiological functions of the two are converging, but Lypressin is more closely related to the physiological rhythm of animal sources. When applied to the human body, it only serves as a functional replacement and cannot fully replicate the global physiological regulatory efficacy of endogenous arginine vasopressin.
Not all symptoms of polyuria can be intervened with it. How to distinguish the applicable central diabetes insipidus?
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Answer: This substance only works for central regulatory deficiency type diabetes insipidus, which is caused by the obstruction of the synthesis and release of endogenous antidiuretic active substances in the body; However, nephrogenic diabetes insipidus is caused by the failure of the renal receptor response itself. Even if exogenous antidiuretic peptide substances are supplemented, it cannot improve the symptoms of polyphagia and polyuria, and does not belong to the scope of adaptation of this drug.
Why can this only be used as a temporary emergency measure to control mild bleeding from esophageal varices and cannot be cured?
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Answer: This substance only relies on regulating vascular tone and assisting in enhancing local coagulation efficacy to temporarily block bleeding, and does not change the organic basis of esophageal venous tortuosity and dilation; It can only be used as a short-term hemostatic buffer during the acute phase to pave the way for subsequent curative diagnosis and treatment plans such as endoscopy and surgery, and cannot fundamentally eliminate the hidden dangers of vascular lesions.
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