RinalodipineAcetate , ≥98% , 851199-59-2

CAS NO.：851199-59-2

Empirical Formula: C59H79N15O21S6

Molecular Weight: 1526.74

MDL number: MFCD20526656

PRODUCT Properties

• 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

Description and Uses

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 a guanylate cyclase-C agonist currently being studied in Phase 3 trials for the treatment of irritable bowel syndrome with constipation.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302
• Precautionary statements: P264-P270-P301+P312-P330-P501