Details of the Drug Formulation (DFM)

General Information of DFM (ID: F23705)
Name
Desoximetasone 0.25% spray
Company
Taro Pharms
Active Pharmaceutical Ingredient (API) Desoximetasone 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
E00PSA DIG Info Glyceryl monooleate Bioadhesive material ...
E0N2PK DIG Info Isopropyl alcohol Antimicrobial preservative ...
E07RWU DIG Info Isopropyl myristate Emollient ...
E0NG2J DIG Info Levomenthol Flavoring agent
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      Transferase (TFase)
            DBT Name: Diacylglycerol kinase alpha (DGKA) 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 Glyceryl monooleate
                    Biological Activity Ki = 91000 nM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID DGKA_HUMAN
      Primary active transporter (PAT)
            DBT Name: Multidrug resistance protein 2 (ABCC2) 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 Glyceryl monooleate
                    Biological Activity Inhibition ratio = 62 % (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MRP2_HUMAN
            DBT Name: Multidrug resistance protein 1 (ABCB1) 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 Glyceryl monooleate
                    Biological Activity Protein expression downregulation = 39.1 % (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Glyceryl monooleate
                    Biological Activity Inhibition ratio = 39 % (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
               Experiment (3) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Glyceryl monooleate
                    Biological Activity Inhibition ratio = 63 % (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
      Transmembrane channel/porin (TC/P)
            DBT Name: Wasabi receptor (TRPA1) 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 Levomenthol
                    Biological Activity EC50 = 96000 nM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID TRPA1_HUMAN
            DBT Name: Transient receptor potential p8 (TRPM8) 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 Levomenthol
                    Biological Activity EC50 = 10100 nM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID TRPM8_HUMAN
            DBT Name: Calcium channel alpha-1C (CAC1C) 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 Levomenthol
                    Biological Activity IC50 = 74600 nM (tested by experiment) [5]
                    Tested Species Oryctolagus cuniculus (Rabbit)
                    UniProt ID CAC1C_RABIT
      Cell line (CELL)
            DBT Name: Lymphoma P388/ADR cells (P388/ADR) 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 Isopropyl alcohol
                    Biological Activity IC50 = 0.22 uM (estimated based on the structural similarity with CHEMBL545 ) [6]
                    Structural Similarity Tanimoto coefficient = 0.789473684
                    Tested Species Mus musculus (Mouse)
                    Cellosaurus ID CVCL_IZ75
References
1 Identification of a novel DGKalpha inhibitor for XLP-1 therapy by virtual screening. Eur J Med Chem. 2019; 164:378-390.
2 Effects of monoglycerides on rhodamine 123 accumulation, estradiol 17 beta-D-glucuronide bidirectional transport and MRP2 protein expression within Caco-2 cells. J Pharm Pharm Sci. 2008;11(3):45-62.
3 Effects of monoglycerides on P-glycoprotein: modulation of the activity and expression in Caco-2 cell monolayers. Mol Pharm. Sep-Oct 2008;5(5):863-75.
4 Identification of a Novel TRPM8 Agonist from Nutmeg: A Promising Cooling Compound. ACS Med Chem Lett. 2017 May 31; 8(7):715-719.
5 IC50 data for the L-type calcium channel extracted from a set of literature articles.
6 Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. J Med Chem. 2004 Mar 11; 47(6):1413-22.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhang and Dr. Mou.