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M5275335

RinalodipineAcetate , ≥98% , 851199-59-2

CAS NO.:851199-59-2

Empirical Formula: C59H79N15O21S6

Molecular Weight: 1526.74

MDL number: MFCD20526656

Pack Size Price Stock Quantity
1mg RMB284.80 In Stock
5mg RMB1254.40 In Stock
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Update time: 2022-07-08

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
Hazardous Substances Data 851199-59-2(Hazardous Substances Data)

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