- Additional information
|Synonyms:||Linacllotide;Linaclotide;Linaelotide Acetate;Linaelotide;CY-14;Liclotide;Argpessin;L-Tyrosine, L-cysteinyl-L-cysteinyl-L-α-glutamyl-L-tyrosyl-L-cysteinyl-L-cysteinyl-L-asparaginyl-L-prolyl-L-alanyl-L-cysteinyl-L-threonylglycyl-L-cysteinyl-, cyclic (1→6),(2→10),(5→13)-tris(disulfide)|
|Boiling point:||2045.0±65.0 °C(Predicted)|
|Purity:||>98% (or refer to the Certificate of Analysis)|
|Shipping Condition:||Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.|
|Storage Condition:||Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).|
|Solubility:||Soluble in DMSO.|
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.
Linaclotide is an effective and selective guanylate cyclase C agonist; it was developed to treat constipation-type irritable bowel syndrome (IBS-C) and chronic constipation.
The US label has a black box warning to not use linaclotide in children less than 6 years old and to avoid in people from 6 to 18 years old, due to the risk of serious dehydration.
More than 10% of people taking linaclotide have diarrhea. Between 1% and 10% of people have decreased appetite, dehydration, low potassium, dizziness when standing up too quickly, nausea, vomiting, urgent need to defecate, fecal incontinence, and bleeding in their colon, rectum, and anus.
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