Sitagliptin phosphate monohydrate

- Overview
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    Background
    
    Sitagliptin phosphate monohydrate is the phosphate salt of its active component, sitagliptin, with one molecule of water. Sitagliptin is a potent inhibitor of dipeptidyl peptidase 4 (DPP-4), an enzyme catalyzing the cleavage of peptides with an N-terminal alanine or proline amino acid residue, that selectively inhibits DPP-4 with 50% inhibition concentration IC50 value of 18 nM and shows no affinity towards other DDP enzymes (such as DDP-8 and DDP-9). The inhibition of DPP4 by sitagliptin has been found to be mediated by increasing levels of two DPP-4 substrates, including glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP). Sitagliptin is currently being investigated in the treatment of type II diabetes.
- Properties
  - Alternative Name
    
    Tesavel, MK-0431,MK0431; (3R)-3-amino-1-[3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one;phosphoric acid;hydrate
    
    CAS Number
    
    654671-77-9
    
    Molecular Formula
    
    C16H15F6N5O·H3PO4·H2O
    
    Molecular Weight
    
    523.3
    
    Appearance
    
    A solid
    
    Purity
    
    97.01%
    
    Solubility
    
    ≥23.8 mg/mL in DMSO; insoluble in EtOH; ≥30.6 mg/mL in H2O with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. McCloskey AG, Miskelly MG, et al. "Pharmacological potential of novel agonists for FFAR4 on islet and enteroendocrine cell function and glucose homeostasis." Eur J Pharm Sci. 2020;142:105104. PMID:31669388
    2. Mansur SA, Mieczkowska A, et al. "Sitagliptin Alters Bone Composition in High-Fat-Fed Mice." Calcif Tissue Int. 2018 Dec 18. PMID:30564859
    3. Ghorpade DS, Ozcan L, et al. "Hepatocyte-secreted DPP4 in obesity promotes adipose inflammation and insulin resistance." Nature. 2018 Mar 29;555(7698):673-677. PMID:29562231
    4. Mroz PA, Perez-Tilve D, et al. "Native Design of Soluble, Aggregation-Resistant Bioactive Peptides: Chemical Evolution of Human Glucagon." ACS Chem Biol. 2016 Dec 16;11(12):3412-3420. PMID:27797473
    5. Khan D, Vasu S, et al. "Islet distribution of Peptide YY and its regulatory role in primary mouse islets and immortalised rodent and human beta-cell function and survival." Mol Cell Endocrinol. 2016 Jul 25;436:102-113. PMID:27465830
    6. Gault, V. A., R. Lennox, and P. R. Flatt. "Sitagliptin, a DPP‐4 inhibitor, improves recognition memory, oxidative stress, hippocampal neurogenesis and up‐regulates key genes involved in cognitive decline." Diabetes, Obesity and Metabolism (2015). PMID:25580570

Sitagliptin phosphate monohydrate

Sitagliptin phosphate monohydrate

Background

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