Linaclotide
- CAS No.
- 851199-59-2
- Chemical Name:
- Linaclotide
- Synonyms
- Linacllotide;Rinalodipine Acetate;CY-14;Argpessin;Liclotide;inaclotide;Linaclotide;Linaelotide;Linaelotide Acetate;Linaclotide USP/EP/BP
- CBNumber:
- CB82498818
- Molecular Formula:
- C59H79N15O21S6
- Molecular Weight:
- 1526.74
- MOL File:
- 851199-59-2.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/8/15 16:24:08
| Melting point | 231-235°C (dec.) |
|---|---|
| Boiling point | 2045.0±65.0 °C(Predicted) |
| Density | 1.60 |
| storage temp. | Hygroscopic, Refrigerator, under inert atmosphere |
| solubility | DMSO (Slightly, Heated), Methanol ((Slightly, Heated)), Water (Slightly, Heated) |
| pka | 3.05±0.10(Predicted) |
| form | Solid |
| color | White |
| Stability | Hygroscopic |
| InChIKey | KXGCNMMJRFDFNR-VRMHCMCOSA-N |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302 | |||||||||
| Precautionary statements | P264-P270-P301+P312-P330-P501 | |||||||||
| NFPA 704 |
|
Linaclotide Chemical Properties,Uses,Production
Description
In August 2012, the US FDA approved linaclotide (also referred to as MD-1100), a first-in-class, orally administered 14-amino acid peptide as a therapy for patients suffering from chronic idiopathic constipation (CIC) and irritable bowel syndrome with constipation (IBS-C). Linaclotide and its active metabolite MM-419447, which results from the cleavage of the C-terminal tyrosine residue by carboxypeptidase A, mimic the actions of the endogenous intestinal peptides guanylin (15 amino acids) and uroguanylin (16 amino acids) by activating guanylyl cyclase C (GC-C) on the intestinal epithelium. Activation of GC-C leads to increased intra- and extracellular levels of cGMP and activation of the CFTR ion channel, resulting in increased levels of HCO3-, Cl-, and water in the intestinal lumen and accelerated gastrointestinal transit. Based on an in vitro assaymeasuring the accumulation of cGMP in T84 cell exposed to an agonist, the EC50 of linaclotide at pH 7.0 was 99±17.5 nM. In preclinical studies in mice using the transit of activated charcoal as ameasure of efficacy, linaclotide at 100 μg/kg significantly accelerated transit compared to wild-type mice treated with charcoal only or GC-Cnullmice treatedwith and without linaclotide.118 Efficacy was also seen in rats treatedwith linaclotide atdoses of 5, 10, and 20 μg/kg. Linaclotide has been synthesized using conventional solid-phase peptide technology.
Uses
Linaclotide is a guanylate cyclase-C agonist currently being studied in Phase 3 trials for the treatment of irritable bowel syndrome with constipation.
Biological Functions
Linaclotide works by increasing fluid in your intestines and helping speed up movement of food through the gut. Linaclotide may improve stool texture and lessen symptoms such as bloating, abdominal pain/discomfort, straining, and feelings of incomplete bowel movements.
Side effects
Side effects include:Diarrhea, abdominal pain, flatulence, abdominal distension, viral gastroenteritis, headache, upper respiratory tract infection, sinusitis
Linaclotide Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| Jigs Chemical ltd | +919099003427 | Gujarat, India | 239 | 58 | Inquiry |
| Anthem Biosciences Pvt Ltd | +91-8066724000 +91-9900044575 | Karnataka, India | 38 | 58 | Inquiry |
| Apicore Pharmaceuticals Pvt Ltd | +91-2662267177 +91-2662267166 | Gujarat, India | 181 | 58 | Inquiry |
| Pharmaffiliates Analytics and Synthetics P. Ltd | +91-172-5066494 | Haryana, India | 6773 | 58 | Inquiry |
| SynZeal Research Pvt Ltd | +1 226-802-2078 | Gujarat, India | 6522 | 58 | Inquiry |
| SUN PHARMACEUTICAL INDUSTRIES LTD | (+91 22) 4324 4324 | New Delhi, India | 175 | 58 | Inquiry |
| MSN LIFE SCIENCES PRIVATE LTD | +91 84523 34200 | New Delhi, India | 104 | 58 | Inquiry |
| AURO PEPTIDES LTD | +91 (40) 6672 1200 | New Delhi, India | 10 | 58 | Inquiry |
| CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
| AFINE CHEMICALS LIMITED | +86-0571-85134551 | China | 15395 | 58 | Inquiry |
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