Details of the Drug Formulation (DFM)

General Information of DFM (ID: F03249)
Name
Captopril 12.5 mg tablet
Company
Legacy Pharmaceutical
Active Pharmaceutical Ingredient (API) Captopril API Info click to show the detail info of this API
Essential hypertension ICD-11: BA00 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E0SJ4H DIG Info Beta-D-lactose Diluent ...
E0VR2M DIG Info Palmitic acid Emulsifying agent ...
E01UTV DIG Info Silicon dioxide Anticaking agent ...
E0QY1F DIG Info Talc Anticaking agent ...
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      G-protein coupled receptor (GPCR)
            DBT Name: Olfactory receptor 51E2 (OR51E2) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Palmitic acid
                    Biological Activity EC50 = 9.8 nM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID O51E2_HUMAN
      Oxidoreductase (ORase)
            DBT Name: Prostaglandin G/H synthase 1 (COX-1) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Palmitic acid
                    Biological Activity IC50 > 500000 nM (tested by experiment) [2]
                    Tested Species Bos taurus (Bovine)
                    UniProt ID PGH1_BOVIN
            DBT Name: Prostaglandin G/H synthase 2 (COX-2) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Palmitic acid
                    Biological Activity IC50 > 500000 nM (tested by experiment) [2]
                    Tested Species Ovis aries (Sheep)
                    UniProt ID PGH2_SHEEP
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Palmitic acid
                    Biological Activity IC50 > 3 uM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PGH2_HUMAN
            DBT Name: Albendazole monooxygenase (CYP3A4) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Silicon dioxide
                    Biological Activity Protein expression downregulation (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
      Hydrolase (HDase)
            DBT Name: Toll-like receptor 2 (TLR2) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Palmitic acid
                    Biological Activity IC50 = 5000 nM (tested by experiment) [5]
                    Tested Species Homo sapiens (Human)
                    UniProt ID TLR2_HUMAN
            DBT Name: Phosphodiesterase 3A (PDE3A) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Palmitic acid
                    Biological Activity IC50 = 4.1 uM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PDE3A_HUMAN
            DBT Name: Phosphodiesterase 4D (PDE4D) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Palmitic acid
                    Biological Activity IC50 = 6.6 uM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PDE4D_HUMAN
      Potential-driven transporter (PDT)
            DBT Name: Monoamine transporter VAT2 (VMAT2) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Palmitic acid
                    Biological Activity Ki = 4.4 uM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID VMAT2_HUMAN
      Transmembrane channel/porin (TC/P)
            DBT Name: Vanilloid receptor 2 (TrpV2) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Palmitic acid
                    Biological Activity IC50 > 10000 nM (tested by experiment) [6]
                    Tested Species Rattus norvegicus (Rat)
                    UniProt ID TRPV2_RAT
      Nuclear receptor (NR)
            DBT Name: PPAR-alpha (PPARA) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Palmitic acid
                    Biological Activity IC50 = 1500 nM (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PPARA_HUMAN
            DBT Name: PPAR-delta (PPARD) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Palmitic acid
                    Biological Activity IC50 = 7400 nM (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PPARD_HUMAN
            DBT Name: PPAR-gamma (PPARG) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Palmitic acid
                    Biological Activity IC50 = 30000 nM (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PPARG_HUMAN
      Other protein families (OPF)
            DBT Name: Adipocyte lipid-binding protein (ALBP) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Palmitic acid
                    Biological Activity IC50 = 930 nM (tested by experiment) [8]
                    Tested Species Homo sapiens (Human)
                    UniProt ID FABP4_HUMAN
            DBT Name: Epidermal lipid-binding protein (E-FABP) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Palmitic acid
                    Biological Activity IC50 = 1200 nM (tested by experiment) [8]
                    Tested Species Homo sapiens (Human)
                    UniProt ID FABP5_HUMAN
            DBT Name: Heart lipid-binding protein (H-FABP) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Palmitic acid
                    Biological Activity IC50 = 2600 nM (tested by experiment) [8]
                    Tested Species Homo sapiens (Human)
                    UniProt ID FABPH_HUMAN
            DBT Name: Intestinal lipid-binding protein (I-FABP) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Palmitic acid
                    Biological Activity IC50 = 1700 nM (tested by experiment) [8]
                    Tested Species Homo sapiens (Human)
                    UniProt ID FABPI_HUMAN
      Cell line (CELL)
            DBT Name: Lung cancer A-549 cells (A-549) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Palmitic acid
                    Biological Activity IC50 = 150000 nM (tested by experiment) [9]
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0023
            DBT Name: Myoblast L6 cells (L6) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Palmitic acid
                    Biological Activity IC50 = 52.7 ug.mL-1 (tested by experiment) [10]
                    Tested Species Rattus norvegicus (Rat)
                    Cellosaurus ID CVCL_0385
            DBT Name: Lymphoma S49 cells (S49) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Palmitic acid
                    Biological Activity EC50 = 500000 nM (tested by experiment) [11]
                    Tested Species Mus musculus (Mouse)
                    Cellosaurus ID CVCL_D198
References
1 US patent application no. 20180116992A1, Modulators of Prostate-Specific G-Protein Receptor (PSGR/OR51E2) and Methods of Using Same.
2 Cox-2 inhibitory effects of naturally occurring and modified fatty acids. J Nat Prod. 2001 Jun; 64(6):745-9.
3 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
4 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
5 Lipolanthionine peptides act as inhibitors of TLR2-mediated IL-8 secretion. Synthesis and structure-activity relationships. J Med Chem. 2006 Mar 9; 49(5):1754-65.
6 Elongation of the Hydrophobic Chain as a Molecular Switch: Discovery of Capsaicin Derivatives and Endogenous Lipids as Potent Transient Receptor Potential Vanilloid Channel 2 Antagonists. J Med Chem. 2018 Sep 27; 61(18):8255-8281.
7 Molecular properties of fatty acids related to PPAR binding and metabolic diseases. Med Chem Res (2013) 22:3126-3133.
8 Discovery of inhibitors of human adipocyte fatty acid-binding protein, a potential type 2 diabetes target. Bioorg Med Chem Lett. 2004 Sep 6; 14(17):4445-8.
9 A comprehensive review of topoisomerase inhibitors as anticancer agents in the past decade. Eur J Med Chem. 2019 Jun 1; 171:129-168.
10 2-Hexadecynoic acid inhibits plasmodial FAS-II enzymes and arrests erythrocytic and liver stage Plasmodium infections. Bioorg Med Chem. 2010 Nov 1; 18(21):7475-85.
11 2'-O-Acyl-6-thioinosine cyclic 3',5'-phosphates as prodrugs of thioinosinic acid. J Med Chem. 1979 Jul; 22(7):811-5.

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