Details of the Drug Formulation (DFM)

General Information of DFM (ID: F13211)
Name
Metformin 500 mg tablet
Company
UDL Laboratories
Active Pharmaceutical Ingredient (API) Metformin API Info click to show the detail info of this API
Diabetes mellitus ICD-11: 5A10 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E0PE9M DIG Info Crospovidone Disintegrant
E01UTP DIG Info Magnesium stearate lubricant
E0Q7IF DIG Info Povidone Binding agent ...
E0F9TP DIG Info Sodium lauryl sulfate Emulsifying agent ...
E05BSD DIG Info Titanium dioxide Coating agent ...
E0T2AJ DIG Info Triacetin Humectant ...
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      G-protein coupled receptor (GPCR)
            DBT Name: Adenosine receptor A3 (AA3R) 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 Sodium lauryl sulfate
                    Biological Activity IC50 = 15 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID AA3R_HUMAN
            DBT Name: Muscarinic receptor M1 (ACM1) 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 Sodium lauryl sulfate
                    Biological Activity IC50 = 29 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ACM1_HUMAN
            DBT Name: Serotonin receptor 1A (5HT1A) 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 Sodium lauryl sulfate
                    Biological Activity IC50 = 15 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID 5HT1A_HUMAN
            DBT Name: Alpha-1A adrenoceptor (ADA1A) 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 Sodium lauryl sulfate
                    Biological Activity IC50 = 15 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ADA1A_HUMAN
            DBT Name: Dopamine D3 receptor (DRD3) 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 Sodium lauryl sulfate
                    Biological Activity IC50 = 18 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID DRD3_HUMAN
            DBT Name: Thromboxane A2 receptor (TBXA2R) 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 Sodium lauryl sulfate
                    Biological Activity IC50 > 10 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID TA2R_HUMAN
      Oxidoreductase (ORase)
            DBT Name: Albendazole monooxygenase (CYP3A4) 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 Magnesium stearate
                    Biological Activity Protein expression downregulation (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Crospovidone
                    Biological Activity Protein expression downregulation (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
               Experiment (3) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Povidone
                    Biological Activity IC50 = 107 uM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
               Experiment (4) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Povidone
                    Biological Activity Protein expression upregulation (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
      Hydrolase (HDase)
            DBT Name: Soluble epoxide hydrolase (EPHX2) 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 Sodium lauryl sulfate
                    Biological Activity IC50 = 5500 nM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID HYES_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 Sodium lauryl sulfate
                    Biological Activity IC50 = 23 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PDE4D_HUMAN
      Lyase/isomerase/ligase (L/I/G)
            DBT Name: Cholesterol 25-hydroxylase (CYP1A2) 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 Povidone
                    Biological Activity IC50 = 78.3 uM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP1A2_HUMAN
      Potential-driven transporter (PDT)
            DBT Name: Solute carrier SLCO1B1 (OATP-C) 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 Sodium lauryl sulfate
                    Biological Activity Ki = 2.9 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO1B1_HUMAN
            DBT Name: Solute carrier SLCO2B1 (OATPB) 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 Sodium lauryl sulfate
                    Biological Activity Inhibition ratio = 88.6 % (tested by experiment) [5]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Sodium lauryl sulfate
                    Biological Activity Ki = 1.98 uM (tested by experiment) [5]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
               Experiment (3) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Sodium lauryl sulfate
                    Biological Activity Ki = 2.8 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
      Nuclear receptor (NR)
            DBT Name: Progesterone receptor (PGR) 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 Sodium lauryl sulfate
                    Biological Activity IC50 = 15 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PRGR_HUMAN
      Cell line (CELL)
            DBT Name: Colon cancer HCT-116 cells (HCT-116) 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 Sodium lauryl sulfate
                    Biological Activity IC50 > 100000 nM (tested by experiment) [6]
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0291
            DBT Name: Leukemia RAW264.7 cells (RAW264.7) 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 Sodium lauryl sulfate
                    Biological Activity IC50 > 100000 nM (tested by experiment) [6]
                    Tested Species Mus musculus (Mouse)
                    Cellosaurus ID CVCL_0493
References
1 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
2 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
3 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
4 Discovery of the First in Vivo Active Inhibitors of the Soluble Epoxide Hydrolase Phosphatase Domain. J Med Chem. 2019 Sep 26; 62(18):8443-8460.
5 Bacterial metabolism rescues the inhibition of intestinal drug absorption by food and drug additives. Proc Natl Acad Sci U S A. 2020 Jul 7;117(27):16009-16018.
6 Synthesis of amphiphilic, chalcogen-based redox modulators with in vitro cytotoxic activity against cancer cells, macrophages and microbes. Med Chem Comm. (2014) 5:25-31.

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