AMMONIUM SACCHARIN

US Previously Marketed

First marketed in 1921

Details

Stereochemistry	ACHIRAL
Molecular Formula	C7H4NO3S.H4N
Molecular Weight	200.215
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

[NH4+].O=C1[N-]S(=O)(=O)C2=CC=CC=C12

InChI

InChIKey=XTPLQANXHDDXIH-UHFFFAOYSA-N

InChI=1S/C7H5NO3S.H3N/c9-7-5-3-1-2-4-6(5)12(10,11)8-7;/h1-4H,(H,8,9);1H3

HIDE SMILES / InChI

Molecular Formula	C7H5NO3S
Molecular Weight	183.185
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	H3N
Molecular Weight	17.0305
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.cancer.gov/about-cancer/causes-prevention/risk/diet/artificial-sweeteners-fact-sheet
Curator's Comment: description was created based on several sources, including http://www.diabetes.co.uk/sweeteners/saccharin.html http://www.ukfoodguide.net/e954.htm

Saccharin is the most established of the artificial sweeteners on the market, this mixture of dextrose and saccharin has been in use for over a century and is found in diet versions of soft drinks. It is 300-500 times sweeter than sugar and contains zero calories. In 1977, the FDA tried to ban its use after evidence showed it caused cancer in rats. Extensive lobbying by the diet food industry allowed products to stay on the shelves as long as they carried warnings about the cancer risks in animals. This warning was removed in 2001 when the Calorie Control Council insisted the link between animal and human cancers could not automatically be made. Consumption of saccharin-sweetened products can benefit diabetics as the substance goes directly through the human digestive system without being digested. While saccharin has no food energy, it can trigger the release of insulin in humans due to its sweet taste. The T1R2/R3 sweet taste receptor exist on the surface of pancreatic beta cells. Saccharin is a unique in that it inhibits glucose-stimulated insulin secretion (GSIS) at submaximal and maximal glucose concentrations, with the other sweeteners having no effect. Investigation of saccharin’s dose-response characteristics showed that concentrations of 0.1 and 0.5 mM stimulated insulin secretion, while concentrations of 1 and 2.5 mM inhibited insulin secretion. Saccharin’s effect on insulin secretion was shown to be reversible in INS-1 832/13 clonal pancreatic beta cells after chronic exposure to 1 mM saccharin. Artificial sweeteners may affect insulin secretion via interaction with the sweet taste receptor, also saccharin may affect other cellular processes linked to insulin secretion, and that these effects are both time- and concentration-dependent

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Taste receptor type 1 member 2 7 Target ID: Q8TE23 Gene ID: 80834.0 Gene Symbol: TAS1R2 Target Organism: Homo sapiens (Human) Sources: http://www.fasebj.org/content/25/1_Supplement/530.1	Binding Agent 1076
Taste receptor type 1 member 3 14 Target ID: Q7RTX0 Gene ID: 83756.0 Gene Symbol: TAS1R3 Target Organism: Homo sapiens (Human) Sources: http://www.fasebj.org/content/25/1_Supplement/530.1	Binding Agent 1076

Conditions

Condition	Modality	Targets	Highest Phase	Product
Unknown 2596

C_max

Value	Dose	Co-administered	Analyte	Population
27 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7303723/	2 g single, oral dose: 2 g route of administration: Oral experiment type: SINGLE co-administered:		SACCHARIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
14 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7303723/	2 g single, oral dose: 2 g route of administration: Oral experiment type: SINGLE co-administered:		SACCHARIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED

AUC

Value	Dose	Co-administered	Analyte	Population
3700 μg × min/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7303723/	10 mg/kg single, intravenous dose: 10 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered:		SACCHARIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
5800 μg × min/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7303723/	10 mg/kg single, intravenous dose: 10 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: PROBENECID	PROBENECID	SACCHARIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
6800 μg × min/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7303723/	2 g single, oral dose: 2 g route of administration: Oral experiment type: SINGLE co-administered:		SACCHARIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
6500 μg × min/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7303723/	2 g single, oral dose: 2 g route of administration: Oral experiment type: SINGLE co-administered:		SACCHARIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED

Overview

CYP3A4	CYP2C9	CYP2D6	hERG

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2B 16	CYP2B 10	CYP2B 32

Drug as perpetrator

Target	Modality	Activity	Metabolite	Clinical evidence
CYP2B 41	inducer 1966 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5266375/	no		no (co-administration study) Comment: coadministration with bupropion: had no effect on the CYP2B activity Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5266375/
CYP2B 41	inhibitor 4027 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5266375/	no		no (co-administration study) Comment: coadministration with bupropion: saccharin had no inhibitory effect on CYP2B activity in vivo Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5266375/

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
CYP2B 10	substrate 4014 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5266375/	no

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:32111	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:32111
ChemicalBook	CB1743735	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB1743735
ChemicalBook	CB32485657	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB32485657
eMolecules	478184	https://www.emolecules.com/cgi-bin/more?vid=478184
MolPort	MolPort-000-881-701	https://www.molport.com/shop/molecule-link/MolPort-000-881-701
ZINC	ZINC000002560357	http://zinc15.docking.org/substances/ZINC000002560357

PubMed

Title	Date	PubMed
Ceramide dissociates 3'-phosphoinositide production from pleckstrin homology domain translocation.	2001-03-01	11171115
GLUT4 vesicle trafficking in rat adipocytes after ethanol feeding: regulation by heterotrimeric G-proteins.	2001-03-01	11171110
Spatial compartmentalization of signal transduction in insulin action.	2001-03	11223878
Development of cataractous macrophthalmia in mice expressing an active MEK1 in the lens.	2001-03	11222509
Time-resolved study of the inner space of lactose permease.	2001-03	11222310
Effects of excitotoxic brain lesions on taste-mediated odor learning in the rat.	2001-03	11222055
Genetic multiplicity of the human UDP-glucuronosyltransferases and regulation in the gastrointestinal tract.	2001-03	11179432
Hormonal regulation of chicken intestinal NHE and SGLT-1 activities.	2001-03	11171642
Impaired PI 3-kinase activation in adipocytes from early growth-restricted male rats.	2001-03	11171610
Effects of cellular ATP depletion on glucose transport and insulin signaling in 3T3-L1 adipocytes.	2001-03	11171597
Glucose metabolism in perfused mouse hearts overexpressing human GLUT-4 glucose transporter.	2001-03	11171596
Identification of N- and O-linked oligosaccharides in human seminal vesicles.	2001-02-24	11191091
Effect of growth hormone on intestinal Na+/glucose cotransporter activity.	2001-02-24	11190985
Glucans exhibit weak antioxidant activity, but stimulate macrophage free radical activity.	2001-02-15	11182295
Adipose-selective targeting of the GLUT4 gene impairs insulin action in muscle and liver.	2001-02-08	11217863
Diabetes. Dialogue between muscle and fat.	2001-02-08	11217842
Negative-ion electrospray mass spectrometry of neutral underivatized oligosaccharides.	2001-02-01	11217777
Skeletal muscle and insulin sensitivity: pathophysiological alterations.	2001-02-01	11171554
Cysteine residues in the D-galactose-H+ symport protein of Escherichia coli: effects of mutagenesis on transport, reaction with N-ethylmaleimide and antibiotic binding.	2001-02-01	11171069
A new type of endo-xyloglucan transferase devoted to xyloglucan hydrolysis in the cell wall of azuki bean epicotyls.	2001-02	11230569
[Micelle-mediated extraction for concentrating conjugated bilirubin in urine].	2001-02	11218735
Serial changes in 14C-deoxyglucose and 201Tl uptake in autoimmune myocarditis in rats.	2001-02	11216528
Na+-to-sugar stoichiometry of SGLT3.	2001-02	11208603
Involvement of PI 3-kinase in IGF-I stimulation of jejunal Na+-K+-ATPase activity and nutrient absorption.	2001-02	11208544
Diurnal rhythmicity in intestinal SGLT-1 function, V(max), and mRNA expression topography.	2001-02	11208542
Automated noninvasive measurement of cyclophosphamide-induced changes in murine voiding frequency and volume.	2001-02	11176453
Characterization of EDTA-soluble polysaccharides from the scape of Musa paradisiaca (banana).	2001-02	11171036
Direct inhibition of the hexose transporter GLUT1 by tyrosine kinase inhibitors.	2001-01-23	11170395
Engineering conformational flexibility in the lactose permease of Escherichia coli: use of glycine-scanning mutagenesis to rescue mutant Glu325-->Asp.	2001-01-23	11170394
Functional asymmetry of the sodium-D-glucose cotransporter expressed in yeast secretory vesicles.	2001-01-15	11220364
Polysaccharides of green Arabica and Robusta coffee beans.	2001-01-15	11217967
The occurrence of internal (1 --> 5)-linked arabinofuranose and arabinopyranose residues in arabinogalactan side chains from soybean pectic substances.	2001-01-15	11217953
Compositional analysis of glycosaminoglycans by electrospray mass spectrometry.	2001-01-15	11199971
Further glucosides of lichens' acids from Central Asian lichens.	2001-01	11219812
A novel assay method for glycosphingolipid deacylase by enzyme-linked immunochemical detection of lysoglycosphingolipid.	2001-01	11214737
An overview of pathophysiology and treatment of insulin resistance.	2001-01	11211569
GLUT4--at the cross roads between membrane trafficking and signal transduction.	2001-01	11208163
Distinct long-term regulation of glycerol and non-esterified fatty acid release by insulin and TNF-alpha in 3T3-L1 adipocytes.	2001-01	11206412
Distinct differences in binding capacity to saccharide epitopes in supratentorial pilocytic astrocytomas, astrocytomas, anaplastic astrocytomas, and glioblastomas.	2001-01	11202177
Suppression of ethanol responding by centrally administered CTOP and naltrindole in AA and Wistar rats.	2001-01	11198711
What's the truth about the health risks of sugar substitutes such as saccharin and aspartame?	2001-01	11198407
Hypoxia-Induced increase in FDG uptake in MCF7 cells.	2001-01	11197971
The Schistosoma mansoni host-interactive tegument forms from vesicle eruptions of a cyton network.	2001-01	11197766
Changes of nasal function after temperature-controlled radiofrequency tissue volume reduction for the turbinate.	2001-01	11192885
The rate-limiting step for tumor [18F]fluoro-2-deoxy-D-glucose (FDG) incorporation.	2001-01	11182558
High-resolution genetic mapping of the saccharin preference locus (Sac) and the putative sweet taste receptor (T1R1) gene (Gpr70) to mouse distal Chromosome 4.	2001-01	11178737
Placental glucose transport in gestational diabetes mellitus.	2001-01	11174489
A saccharinate-iron(II) complex with a free saccharin molecule present, [Fe(phen)3]sac2.sacH.6H2O.	2001-01	11173377
Improved water solubility of neohesperidin dihydrochalcone in sweetener blends.	2001-01	11170576
Cytological and lectin histochemical characterization of secretion production and secretion composition in the tubular glands of the canine anal sacs.	2001	11173805

Patents

Sample Use Guides

In Vivo Use Guide

no more than 80 to 3000 mg saccharin per kilogram or litre should be used

Route of Administration: Oral

In Vitro Use Guide

After assaying for prolactin (PRL) in saccharin-treated cultures, it was observed that this sweetener is also capable of stimulating PRL production two- to sixfold in a dose-dependent manner. Enhancement of PRL production can be observed at 0.5 mM saccharin, yet this is 10 times less than the saccharin concentration required to alter cell shape. These effects of saccharin on cell morphology and on PRL production are reversible in rat pituitary tumor cells (GH4C1). When added to cultures along with maximal concentrations of epidermal growth factor (EGF) or thyrotropin-releasing hormone (TRH), the effects of saccharin on PRL production are additive, suggesting that the actions of saccharin are mediated by a somewhat different pathway from that of the peptide hormones

Substance Class	Chemical Created by `admin` on `Mon Mar 31 17:57:53 GMT 2025` Edited by `admin` on `Mon Mar 31 17:57:53 GMT 2025`
Record UNII	63Q3BCF15A
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

AMMONIUM SACCHARIN

Common Name

English

DARAMIN

Preferred Name

English

SACCHARINATE AMMONIUM

Common Name

English

1,2-BENZISOTHIAZOLIN-3-ONE 1,1-DIOXIDE AMMONIUM SALT

Common Name

English

1,2-BENZISOTHIAZOL-3(2H)-ONE, 1,1-DIOXIDE, AMMONIUM SALT

Common Name

English

SACCHARIN AMMONIUM SALT [MI]

Common Name

English

1,2-BENZISOTHIAZOL-3(2H)-ONE, 1,1-DIOXIDE, AMMONIUM SALT (1:1)

Common Name

English

SUCLINE

Brand Name

English

AMMONIUM SACCHARIN [FCC]

Common Name

English

SACCHARIN AMMONIUM

Common Name

English

Code System Code Type Description

EPA CompTox

DTXSID7027621