General Information of DFM (ID: F23304)
Name	Tenapanor 50 mg tablet
Company	Ardelyx
Active Pharmaceutical Ingredient (API)	Tenapanor		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
	E0V2QO	DIG Info	Cellulose microcrystalline	Adsorbent ...
	E0P9YZ	DIG Info	Hydrophobic colloidal silica	Anticaking agent ...
	E0J4OX	DIG Info	Hydroxypropyl cellulose	Binding agent ...
	E0T4YW	DIG Info	Hypromellose	Coating agent
	E0U9NK	DIG Info	Propyl gallate	Antimicrobial preservative ...
	E06VNY	DIG Info	Stearic acid	Emulsifying agent ...
	E06RNC	DIG Info	Tartaric acid	Acidulant ...
	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	Stearic acid
Biological Activity	IC50 = 10 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	AA3R_HUMAN
Oxidoreductase (ORase)
DBT Name: N1-methyl adenine demethylase (FTO)				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	Propyl gallate
Biological Activity	Ki = 3 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	FTO_HUMAN
DBT Name: Arachidonate 5-lipoxygenase (ALOX5)				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	Propyl gallate
Biological Activity	Ki = 0.43 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	LOX5_HUMAN
DBT Name: Prostaglandin G/H synthase 1 (COX-1)				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	Stearic acid
Biological Activity	IC50 > 500000 nM (tested by experiment)					[2]
Tested Species	Bos taurus (Bovine)
UniProt ID	PGH1_BOVIN
DBT Name: Prostaglandin G/H synthase 2 (COX-2)				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	Stearic acid
Biological Activity	IC50 > 500000 nM (tested by experiment)					[2]
Tested Species	Ovis aries (Sheep)
UniProt ID	PGH2_SHEEP
Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Propyl gallate
Biological Activity	IC50 = 7.2 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	PGH2_HUMAN
DBT Name: Lysine-specific demethylase 4C (KDM4C)				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	Propyl gallate
Biological Activity	Ki = 39 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	KDM4C_HUMAN
DBT Name: Tyrosine 3-monooxygenase (TH)				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	Propyl gallate
Biological Activity	Ki = 1.9 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	TY3H_HUMAN
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	Hypromellose
Biological Activity	Protein expression upregulation (tested by experiment)					[3]
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	Hypromellose
Biological Activity	Protein expression downregulation (tested by experiment)					[3]
Tested Species	Homo sapiens (Human)
UniProt ID	CP3A4_HUMAN
DBT Name: Cytochrome P450 2E1 (CYP2E1)				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	Hypromellose
Biological Activity	IC50 = 253.5 uM (tested by experiment)					[4]
Tested Species	Homo sapiens (Human)
UniProt ID	CP2E1_HUMAN
DBT Name: Mephenytoin 4-hydroxylase (CYP2C19)				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	Hydroxypropyl cellulose
Biological Activity	EC50 = 89.5 uM (tested by experiment)					[4]
Tested Species	Homo sapiens (Human)
UniProt ID	CP2CJ_HUMAN
Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Hypromellose
Biological Activity	EC50 = 211.8 uM (tested by experiment)					[4]
Tested Species	Homo sapiens (Human)
UniProt ID	CP2CJ_HUMAN
DBT Name: Debrisoquine 4-hydroxylase (CYP2D6)				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	Hydroxypropyl cellulose
Biological Activity	EC50 = 148.3 uM (tested by experiment)					[4]
Tested Species	Homo sapiens (Human)
UniProt ID	CP2D6_HUMAN
Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Hypromellose
Biological Activity	EC50 = 159.3 uM (tested by experiment)					[4]
Tested Species	Homo sapiens (Human)
UniProt ID	CP2D6_HUMAN
DBT Name: Cytochrome P450 3A5 (CYP3A5)				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	Hypromellose
Biological Activity	IC50 = 19.4 uM (tested by experiment)					[4]
Tested Species	Homo sapiens (Human)
UniProt ID	CP3A5_HUMAN
Cation-dependent O-methyltransferase
DBT Name: Catechol O-methyltransferase (COMT)				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	Propyl gallate
Biological Activity	Ki = 0.015 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	COMT_HUMAN
Hydrolase (HDase)
DBT Name: Phosphodiesterase 3A (PDE3A)				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	Stearic acid
Biological Activity	IC50 = 3.1 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	PDE3A_HUMAN
DBT Name: Phosphodiesterase 4D (PDE4D)				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	Propyl gallate
Biological Activity	IC50 = 26 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	PDE4D_HUMAN
Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Stearic acid
Biological Activity	IC50 = 6.7 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 (1) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Hydroxypropyl cellulose
Biological Activity	EC50 = 139 uM (tested by experiment)					[4]
Tested Species	Homo sapiens (Human)
UniProt ID	CP1A2_HUMAN
Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Hypromellose
Biological Activity	EC50 = 106.7 uM (tested by experiment)					[4]
Tested Species	Homo sapiens (Human)
UniProt ID	CP1A2_HUMAN
Potential-driven transporter (PDT)
DBT Name: Solute carrier SLCO2B1 (OATPB)				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	Propyl gallate
Biological Activity	Inhibition ratio = 29.6 % (tested by experiment)					[5]
Tested Species	Homo sapiens (Human)
UniProt ID	SO2B1_HUMAN
Nuclear receptor (NR)
DBT Name: Estrogen receptor alpha (ESR1)				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	Stearic acid
Biological Activity	IC50 = 16 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	ESR1_HUMAN
DBT Name: PPAR-alpha (PPARA)				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	Stearic acid
Biological Activity	IC50 = 1100 nM (tested by experiment)					[6]
Tested Species	Homo sapiens (Human)
UniProt ID	PPARA_HUMAN
DBT Name: PPAR-delta (PPARD)				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	Stearic acid
Biological Activity	IC50 = 6000 nM (tested by experiment)					[6]
Tested Species	Homo sapiens (Human)
UniProt ID	PPARD_HUMAN
DBT Name: PPAR-gamma (PPARG)				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	Stearic acid
Biological Activity	IC50 = 30000 nM (tested by experiment)					[6]
Tested Species	Homo sapiens (Human)
UniProt ID	PPARG_HUMAN
Other protein families (OPF)
DBT Name: Anthrax toxin receptor 2 (CMG-2)				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	Propyl gallate
Biological Activity	IC50 > 300000 nM (tested by experiment)					[7]
Tested Species	Homo sapiens (Human)
UniProt ID	ANTR2_HUMAN
Cell line (CELL)
DBT Name: Colon cancer Caco-2 cells (Caco-2)				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	Hypromellose
Biological Activity	Promotion ratio > 18 % (tested by experiment)					[8]
Tested Species	Homo sapiens (Human)
Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Hypromellose
Biological Activity	Promotion ratio > 27 % (tested by experiment)					[8]
Tested Species	Homo sapiens (Human)
DBT Name: Colon cancer COLO 205 cells (COLO 205)				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	Stearic acid
Biological Activity	IC50 > 200000 nM (tested by experiment)					[9]
Tested Species	Homo sapiens (Human)
Cellosaurus ID	CVCL_0218
DBT Name: Colon cancer HT-29 cells (HT-29)				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	Stearic acid
Biological Activity	IC50 > 200000 nM (tested by experiment)					[9]
Tested Species	Homo sapiens (Human)
Cellosaurus ID	CVCL_0320

References
1	The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
2	Cox-2 inhibitory effects of naturally occurring and modified fatty acids. J Nat Prod. 2001 Jun; 64(6):745-9.
3	Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
4	Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
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	Molecular properties of fatty acids related to PPAR binding and metabolic diseases. Med Chem Res (2013) 22:3126-3133.
7	1,2,3,4,6-Penta-O-galloyl--D-glucopyranose inhibits angiogenesis via inhibition of capillary morphogenesis gene 2. J Med Chem. 2013 Mar 14; 56(5):1940-5.
8	Interactions between human multidrug resistance related protein (MRP2; ABCC2) and excipients commonly used in self-emulsifying drug delivery systems (SEDDS). Int J Pharm. 2013 Apr 15;447(1-2):192-8.
9	Liposomal formulation of retinoids designed for enzyme triggered release. J Med Chem. 2010 May 13; 53(9):3782-92.

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