Details of the Drug Formulation (DFM)

General Information of DFM (ID: F20300)
Name
Sodium fluoride 1.1 mg tablet
Company
Mayne Pharma
Active Pharmaceutical Ingredient (API) Sodium fluoride API Info click to show the detail info of this API
Periodontal disease ICD-11: DA0C Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E0PJ5J DIG Info Benzosulfimide Flavoring agent
E0SJ4H DIG Info Beta-D-lactose Diluent ...
E01UTP DIG Info Magnesium stearate lubricant
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      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 for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Magnesium stearate
                    Biological Activity Protein expression downregulation (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
      Hydrolase (HDase)
            DBT Name: Cholinesterase (BCHE) 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 Benzosulfimide
                    Biological Activity IC50 = 3600 nM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CHLE_HUMAN
      Lyase/isomerase/ligase (L/I/G)
            DBT Name: Carbonic anhydrase VA (CA5A) 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 Benzosulfimide
                    Biological Activity Ki = 10060 nM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH5A_HUMAN
            DBT Name: Carbonic anhydrase VB (CA5B) 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 Benzosulfimide
                    Biological Activity Ki = 7210 nM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH5B_HUMAN
            DBT Name: Carbonic anhydrase I (CA1) 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 Benzosulfimide
                    Biological Activity Ki > 10000 nM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH1_HUMAN
            DBT Name: Carbonic anhydrase II (CA2) 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 Benzosulfimide
                    Biological Activity Ki = 5180 nM (tested by experiment) [5]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH2_HUMAN
            DBT Name: Carbonic anhydrase IV (CA4) 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 Benzosulfimide
                    Biological Activity Ki = 7920 nM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH4_HUMAN
            DBT Name: Carbonic anhydrase IX (CA9) 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 Benzosulfimide
                    Biological Activity Ki = 100 nM (tested by experiment) [6]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH9_HUMAN
            DBT Name: Carbonic anhydrase VI (CA6) 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 Benzosulfimide
                    Biological Activity Ki = 935 nM (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH6_HUMAN
            DBT Name: Carbonic anhydrase VII (CA7) 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 Benzosulfimide
                    Biological Activity Ki = 10 nM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH7_HUMAN
            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 Benzosulfimide
                    Biological Activity Ki = 633 nM (tested by experiment) [8]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH12_HUMAN
            DBT Name: Carbonic anhydrase XIV (CA14) 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 Benzosulfimide
                    Biological Activity Ki = 773 nM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH14_HUMAN
References
1 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
2 Sulfonamides as multifunctional agents for Alzheimer's disease. Bioorg Med Chem Lett. 2015 Feb 1; 25(3):626-30.
3 Cyclic secondary sulfonamides: unusually good inhibitors of cancer-related carbonic anhydrase enzymes. J Med Chem. 2014 Apr 24; 57(8):3522-31.
4 A Sweet Combination: Developing Saccharin and Acesulfame K Structures for Selectively Targeting the Tumor-Associated Carbonic Anhydrases IX and XII. J Med Chem. 2020 Jan 9; 63(1):321-333.
5 Mutation of active site residues Asn67 to Ile, Gln92 to Val and Leu204 to Ser in human carbonic anhydrase II: influences on the catalytic activity and affinity for inhibitors. Bioorg Med Chem. 2012 Apr 1; 20(7):2208-13.
6 Seriously Sweet: Acesulfame K Exhibits Selective Inhibition Using Alternative Binding Modes in Carbonic Anhydrase Isoforms. J Med Chem. 2018 Feb 8; 61(3):1176-1181.
7 Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata. Bioorg Med Chem Lett. 2011 Jan 15; 21(2):710-4.
8 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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