Details of the Drug Formulation (DFM)

General Information of DFM (ID: F13402)
Name
Methenamine 1000 mg tablet
Company
Winthrop
Active Pharmaceutical Ingredient (API) Methenamine API Info click to show the detail info of this API
Urinary tract infection ICD-11: GC08 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E08XEK DIG Info Hydrazine yellow Colorant
E01UTP DIG Info Magnesium stearate lubricant
E0Q7IF DIG Info Povidone Binding agent ...
E0BG7D DIG Info Saccharin sodium dihydrate Flavoring agent
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      G-protein coupled receptor (GPCR)
            DBT Name: Opioid receptor mu (OPRM1) 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 Hydrazine yellow
                    Biological Activity IC50 = 16 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID OPRM_HUMAN
            DBT Name: Dopamine D1 receptor (DRD1) 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 Hydrazine yellow
                    Biological Activity IC50 = 23 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID DRD1_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 Povidone
                    Biological Activity IC50 = 107 uM (tested by experiment) [3]
                    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 Protein expression upregulation (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
      Hydrolase (HDase)
            DBT Name: Tyrosyl-DNA phosphodiesterase 2 (TDP2) 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 Hydrazine yellow
                    Biological Activity IC50 = 3500 nM (estimated based on the structural similarity with CHEMBL3813826 ) [4]
                    Structural Similarity Tanimoto coefficient = 0.777777778
                    Tested Species Homo sapiens (Human)
                    UniProt ID TYDP2_HUMAN
      Lyase/isomerase/ligase (L/I/G)
            DBT Name: Carbonic anhydrase XII (CA12) 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 Saccharin sodium dihydrate
                    Biological Activity Ki = 633 nM (estimated based on the structural similarity with CHEMBL310671 ) [5]
                    Structural Similarity Tanimoto coefficient = 0.962264151
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH12_HUMAN
            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
      Transmembrane channel/porin (TC/P)
            DBT Name: GABA(A) receptor alpha-1 (GABRA1) 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 Hydrazine yellow
                    Biological Activity IC50 = 13 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID GBRA1_HUMAN
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 selective inhibitors of tyrosyl-DNA phosphodiesterase 2 by targeting the enzyme DNA-binding cleft. Bioorg Med Chem Lett. 2016 Jul 15; 26(14):3232-3236.
5 Carbonic anhydrase inhibitors: copper(II) complexes of polyamino-polycarboxylamido aromatic/heterocyclic sulfonamides are very potent inhibitors of the tumor-associated isoforms IX and XII. Bioorg Med Chem Lett. 2008 Jan 15; 18(2):836-41.

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