Linaclotide CAS 851199-59-2

Shaanxi BLOOM Tech Co., Ltd. is one of the most experienced manufacturers and suppliers of linaclotide cas 851199-59-2 in China. Welcome to wholesale bulk high quality linaclotide cas 851199-59-2 for sale here from our factory. Good service and reasonable price are available.

Linaclotide, with the chemical formula C₂₁H₂₉N₃O₅ and CAS Registry Number 851199-59-2, is a structurally defined synthetic peptide therapeutic agent. Its characteristic amino acid sequence is recorded as: H‑Thr‑Lys‑Pro‑Ser‑Leu‑Gly‑Leu‑Met‑Pal‑He‑Eu‑Gly‑Leu‑Met‑Pal‑He‑Eu‑Gly‑Leu‑Met‑Pal‑He‑OH.

Linaclotide typically appears as a white to grayish‑white crystalline or amorphous powder with distinct physicochemical properties. It is almost insoluble in water under normal conditions, but shows appreciable solubility in polar aprotic solvents such as formic acid and dimethyl sulfoxide (DMSO). In terms of chemical stability, linaclotide remains relatively stable within the pH range of 1 to 7, making it compatible with a variety of weakly acidic to neutral formulation environments. Although it exhibits a certain degree of solubility under strongly alkaline conditions at high pH values, its overall aqueous solubility remains extremely low. Under physiological pH conditions approximating the human intestinal environment, the water solubility of the product is generally less than 1 mg/mL, a property that influences its formulation design, dissolution behavior, and oral absorption characteristics.

Pharmacologically, linaclotide is classified as a synthetic 14‑amino‑acid peptide agonist that acts locally within the gastrointestinal tract. It is primarily indicated for the treatment of certain subtypes of chronic idiopathic constipation and irritable bowel syndrome with constipation (IBS‑C), providing relief by increasing intestinal fluid secretion and accelerating gastrointestinal transit without significant systemic absorption.

Beyond its clinical applications, linaclotide also serves as a valuable reference standard and chemical identification material in pharmaceutical research and development. It can be used to characterize and confirm the structure, purity, and physicochemical properties of related synthetic compounds or drug substances. By comparing and analyzing spectral data-including infrared spectroscopy (IR), nuclear magnetic resonance (NMR), and mass spectrometry (MS)-between the reference standard and test samples, researchers can accurately identify unknown compounds, verify structural consistency, and ensure batch‑to‑batch uniformity of drug products.

In addition, linaclotide is widely employed in bioanalytical detection and quantitative analysis, enabling sensitive and selective measurement of its concentration and distribution in various biological matrices such as plasma, feces, and intestinal tissues. These analytical applications are critical for evaluating key pharmacokinetic and pharmacodynamic profiles, including drug absorption, distribution, metabolism, and excretion (ADME), as well as for assessing local efficacy, safety margins, and potential drug‑drug interactions in preclinical and clinical studies.

Linaclotide COA

Linaclotide is an effective and selective agonist of guanylate cyclase-C (GC-C), developed for the treatment of constipated irritable bowel syndrome (IBS-C) and chronic constipation.

Treatment of Constipated Irritable Bowel Syndrome (IBS-C): By binding to GC-C receptors in the enteric epithelium, GC-C is activated, which increases enteric fluid secretion, accelerates food delivery, and reduces enteric pain nerve activation. For patients with Constipated Irritable Bowel Syndrome (IBS-C), it can help improve enteric function and alleviate constipation symptoms.

Treatment of Chronic Constipation (CIC): Chronic constipation (CIC) is a common digestive system disease that patients suffer from long-term constipation. Another important use of it is for the treatment of adult patients with chronic idiopathic constipation (CIC). By regulating intestenteric nal function, it helps to restore normal bowel habits and alleviate chronic constipation symptoms.

 

Scientific research and pharmacological experiments: In addition to clinical therapeutic purposes, it is also widely used in scientific research and pharmacological experiments. As an agonist of guanylate cyclase C (GC-C), it provides an important tool for studying enteric physiology and pathology. Researchers can further understand the pathogenesis of enteric diseases by studying their mechanisms and effects, providing a basis for developing more effective treatment methods.

 

Research experiment: As an agonist of guanylate cyclase C (GC-C), it has high selectivity and specificity. It is widely used in scientific research experiments to study the physiological and pathological mechanisms of the intestine, especially in areas such as constipation and irritable bowel syndrome (IBS-C). Through drug administration experiments, researchers can observe the impact on enteric function, further understand its mechanism of action and potential therapeutic applications.

 

5. Drug metabolism and kinetics research: Understanding the metabolism and kinetics of this substance in vivo can help evaluate its efficacy and safety. Through pharmacokinetic experiments, its absorption, distribution, metabolism, and excretion (ADME) characteristics in organisms can be determined, providing scientific basis for clinical medication plans.

6. Drug synthesis and optimization: As an effective GC-C agonist, it has potential value in drug synthesis. By studying its molecular structure and pharmacological activity, it is possible to further explore synthesis methods and optimization strategies for similar compounds, in order to develop more efficient, safe, and low toxicity drugs.

 

7. Drug design and modification: Based on the mechanism of action and structure-activity relationship research of product, chemists can design and modify drug molecules with similar or improved mechanisms of action. Through computer-aided drug design and experimental verification, the properties and activities of new drug molecules can be predicted, and their binding ability and efficacy with targets can be optimized.

8. Research on synthesis methods: Exploring the synthesis methods of product helps to understand its chemical structure and properties, while also providing reliable process conditions for drug production. Chemists will study different synthesis routes and methods to improve the yield, purity, and stability of product.

The common synthesis methods of Linaclotide involve multiple steps, among which the following are the key steps:

3. Remove Acm protective group and form remaining disulfide bond:

We can successfully use Trt and Acm, two orthogonal protected cysteine protection groups, for the synthesis of linalopide. The use of these protective groups helps to avoid unnecessary side reactions during the synthesis process, thereby improving the efficiency of synthesis and the purity of the product. Please note that PhS(O)Ph/CH₃SiCl₃ has a pungent odor and should be operated under good ventilation conditions, wearing appropriate personal protective equipment.

Reaction conditions:

Use PhS(O)Ph/CH₃SiCl₃ as the deprotection reagent.

Objective:

To remove the Acm protective group of cysteine and promote the formation of residual disulfide bonds.

The above steps are only one possible method for synthesizing Linaclotide, and may involve more details and precautions in actual operation. In addition, synthesizing peptides or protein drugs with high molecular weight and complexity requires high experimental skills and experience, and it is recommended to do so under the guidance of professional laboratories and professionals.

Linaclotide is a guanylate cyclase-C (GC-C) agonist, and its mechanism of action mainly involves multiple aspects. The following is a detailed introduction for you:

After Linaclotide binds to the GC-C receptor on the surface of enteric epithelial cells, it activates the receptor and increases the concentration of cyclic guanosine monophosphate (cGMP) within the cells. cGMP, as an important cellular signaling molecule, can stimulate enteric epithelial cells to secrete chloride ions and bicarbonate into the enteric lumen.

Increase the secretion of intestinal fluid

Meanwhile, cGMP can also inhibit the absorption of sodium ions, resulting in an increase in osmotic pressure within the enteric lumen. To maintain osmotic pressure balance, water enters the enteric lumen from the cells, thereby increasing the volume of enteric contents and the secretion of fluid, making the stool soft and easy to excrete, effectively improving constipation symptoms.

Enhance intestinal peristalsis

The increase in cGMP concentration not only affects the secretion of enteric fluid, but also has an effect on enteric smooth muscle. It can enhance the contraction of enteric smooth muscle, promote enteric peristalsis, accelerate the movement of feces in the intestines, reduce the retention time of feces in the intestines, and further relieve constipation.

Reduce visceral hypersensitivity

Patients with constipation-induced irritable bowel syndrome often have visceral hypersensitivity, being overly sensitive to stimuli such as enteric dilation and contraction, and are prone to discomfort symptoms such as abdominal pain and abdominal distension. 

Improve intestinal barrier function

Linaclotide can increase the secretion of the enteric mucus layer. The mucus layer is a viscous liquid secreted by intestienteric al epithelial cells. It can cover the surface of the intestine, forming a protective barrier that shields enteric epithelial cells from damage by harmful substances and maintains the normal function and structure of the intestine. 

Potential anti-tumor effect

Recent studies have shown that the GC-C receptor may play an important role in the suppression of enteric tumors. As a GC-C agonist, Linaclotide may have the potential to inhibit enteric inflammation and prevent tumors by activating GC-C receptors and regulating processes such as proliferation, differentiation and apoptosis of enteric cells.

Linaclotide (product name: Linzess ®) It is a medication used to treat constipation predominant irritable bowel syndrome (IBS-C) and chronic idiopathic constipation (CIC). As a guanylate cyclase C (GC-C) receptor agonist, it improves symptoms by increasing the secretion of enteric fluid and accelerating enteric peristalsis. Since obtaining FDA approval in 2012, Linaclotide has become one of the important treatment options in the field of gastroenterology. The mechanism of action of Linaclotide is closely related to its activation of GC-C receptors. GC-C receptor is a transmembrane protein located on the top membrane of enteric epithelial cells, and its endogenous ligands are guanylin and uroguanylin.

These peptide hormones activate GC-C receptors under physiological conditions, causing an increase in intracellular cyclic guanosine monophosphate (cGMP) levels, which in turn activates downstream CFTR (cystic fibrosis transmembrane conductance regulator) channels, leading to increased secretion of chloride ions and bicarbonate, accompanied by water entering the enteric lumen, softening feces and promoting enteric peristalsis. In the 1990s, scientists began studying the physiological functions of GC-C receptors and their roles in gastrointestinal diseases. Research has found that abnormalities in the GC-C signaling pathway are associated with diseases such as constipation and IBS-C, providing a theoretical basis for the development of drugs targeting GC-C receptors.

 

 

The inspiration for Linaclotide's development was partly derived from bacterial heat stable enterotoxin (STa). STa is a toxin secreted by certain pathogenic Escherichia coli that can overactivate GC-C receptors, leading to severe secretory diarrhea. Scientists have realized that if a synthetic peptide can be designed to selectively activate GC-C receptors without causing excessive stimulation, it may be used to treat constipation. Based on this idea, researchers have begun to structurally modify natural GC-C agonists, such as guanosine protein and uridine protein, to improve their stability and selectivity.

Hot Tags: linaclotide cas 851199-59-2, suppliers, manufacturers, factory, wholesale, buy, price, bulk, for sale, dermorphin peptide, DERMORPHIN, Cosmetic, dermorphin in humans, Melanotan ii powder