Details of the Drug Formulation (DFM)

General Information of DFM (ID: F24306)
Name
Lixisenatide 100 mcg/ml Injection
Company
Sanofi-Aventis U.S.
Active Pharmaceutical Ingredient (API) Lixisenatide API Info click to show the detail info of this API
Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E06WYP DIG Info Glycerin Antimicrobial preservative ...
E0H0KW DIG Info Hydrochloric acid Acidulant
E08HTI DIG Info Metacresol Antimicrobial preservative
E0D0QF DIG Info Methionine Buffering agent ...
E0VN9W DIG Info Sodium acetate Antimicrobial preservative ...
E0L2PN DIG Info Sodium hydroxide Alkalizing agent
E0H2SC DIG Info Water Solvent
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      Lyase/isomerase/ligase (L/I/G)
            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 Sodium acetate
                    Biological Activity Ki = 10800 nM (tested by experiment) [1]
                    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 Sodium acetate
                    Biological Activity Ki = 130000 nM (tested by experiment) [2]
                    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 Hydrochloric acid
                    Biological Activity Ki = 90000 nM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH4_HUMAN
            DBT Name: Carbonic anhydrase V (CA5) 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 Hydrochloric acid
                    Biological Activity Ki = 156 nM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH5A_HUMAN ; CAH5B_HUMAN
      Potential-driven transporter (PDT)
            DBT Name: Integral membrane E16 (SLC7A5) 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 Methionine
                    Biological Activity IC50 = 120000 nM (estimated based on the structural similarity with CHEMBL1234268 ) [5]
                    Structural Similarity Tanimoto coefficient = 1
                    Tested Species Homo sapiens (Human)
                    UniProt ID LAT1_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 Metacresol
                    Biological Activity IC50 = 37000 nM (estimated based on the structural similarity with CHEMBL4470418 ) [6]
                    Structural Similarity Tanimoto coefficient = 0.941860465
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0023
            DBT Name: Carcinoma MDA-MB-231 cells (MDA-MB-231) 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 Metacresol
                    Biological Activity IC50 = 27000 nM (estimated based on the structural similarity with CHEMBL4470418 ) [6]
                    Structural Similarity Tanimoto coefficient = 0.941860465
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0062
References
1 Carbonic anhydrase inhibitors. Inhibition of the -class enzymes from the fungal pathogens Candida albicans and Cryptococcus neoformans with branched aliphatic/aromatic carboxylates and their derivatives. Bioorg Med Chem Lett. 2011 Apr 15; 21(8):2521-6.
2 Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with carboxylates. Bioorg Med Chem Lett. 2005 Feb 1; 15(3):573-8.
3 Carbonic anhydrase inhibitors: inhibition of the membrane-bound human isozyme IV with anions. Bioorg Med Chem Lett. 2004 Dec 6; 14(23):5769-73.
4 Carbonic anhydrase inhibitors. Inhibition of the newly isolated murine isozyme XIII with anions. Bioorg Med Chem Lett. 2004 Nov 1; 14(21):5435-9.
5 Reevaluating the Substrate Specificity of the L-Type Amino Acid Transporter (LAT1). J Med Chem. 2018 Aug 23; 61(16):7358-7373.
6 Isolation and Characterization of Anaephenes A-C, Alkylphenols from a Filamentous Cyanobacterium ( Hormoscilla sp., Oscillatoriales). J Nat Prod. 2018 Dec 28; 81(12):2716-2721.

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