Sodium/glucose cotransporter 1

Target id: 915

Nomenclature: Sodium/glucose cotransporter 1

Abbreviated Name: SGLT1

Systematic Nomenclature: SLC5A1

Family: Hexose transporter family

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for Sodium/glucose cotransporter 1 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 13 664 22q12.3 SLC5A1 solute carrier family 5 member 1
Mouse 14 665 5 17.46 cM Slc5a1 solute carrier family 5 (sodium/glucose cotransporter)
Rat 13 665 14a21 Slc5a1 solute carrier family 5 member 1
Previous and Unofficial Names
high affinity sodium-glucose cotransporter | NAGT | Na(+)/glucose cotransporter 1 | solute carrier family 5, member 1 | solute carrier family 5 (sodium/glucose cotransporter), member 1
Database Links
Specialist databases
Bioparadigms SLC Tables SLC5A1 (Hs)
Other databases
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Gene
OMIM
UniProtKB
Wikipedia
Stoichiometry
2 Na+ : 1 glucose [4]

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
mizagliflozin Hs Inhibition 7.6 pKi 3
pKi 7.6 (Ki 2.7x10-8 M) [3]
Description: Monitoring the uptake of 14C-labeled AMG
remogliflozin Hs Inhibition 5.3 pKi 1
pKi 5.3 (Ki 4.52x10-6 M) [1]
sergliflozin Hs Inhibition 5.1 pKi 5
pKi 5.1 (Ki 7.943x10-6 M) [5]
sotagliflozin Hs Inhibition 7.4 pIC50 11
pIC50 7.4 (IC50 3.6x10-8 M) [11]
dapagliflozin Hs Inhibition 6.4 pIC50 6
pIC50 6.4 (IC50 3.7x10-7 M) [6]
canagliflozin Hs Inhibition 6.2 pIC50 7
pIC50 6.2 (IC50 6.84x10-7 M) [7]
ipragliflozin Rn Inhibition 5.9 pIC50 10
pIC50 5.9 (IC50 1.166x10-6 M) [10]
Description: Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing rSGLT1.
ipragliflozin Mm Inhibition 5.9 pIC50 10
pIC50 5.9 (IC50 1.38x10-6 M) [10]
Description: Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing mSGLT1.
ipragliflozin Hs Inhibition 5.7 pIC50 10
pIC50 5.7 (IC50 1.876x10-6 M) [10]
Description: Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing hSGLT1.
ertugliflozin Hs Inhibition 5.7 pIC50 8
pIC50 5.7 (IC50 1.96x10-6 M) [8]
empagliflozin Hs Inhibition 5.1 pIC50 2
pIC50 5.1 (IC50 7.943x10-6 M) [2]
tofogliflozin Hs Inhibition 5.1 pIC50 9
pIC50 5.1 (IC50 8.444x10-6 M) [9]
Description: Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing hSGLT1.
View species-specific inhibitor tables
Clinically-Relevant Mutations and Pathophysiology
Disease:  Glucose/galactose malabsorption; GGM
Synonyms: Glucose-galactose malabsorption [Orphanet: ORPHA35710]
OMIM: 606824
Orphanet: ORPHA35710

References

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1. Fujimori Y, Katsuno K, Nakashima I, Ishikawa-Takemura Y, Fujikura H, Isaji M. (2008) Remogliflozin etabonate, in a novel category of selective low-affinity sodium glucose cotransporter (SGLT2) inhibitors, exhibits antidiabetic efficacy in rodent models. J. Pharmacol. Exp. Ther.327 (1): 268-76. [PMID:18583547]

2. Grempler R, Thomas L, Eckhardt M, Himmelsbach F, Sauer A, Sharp DE, Bakker RA, Mark M, Klein T, Eickelmann P. (2012) Empagliflozin, a novel selective sodium glucose cotransporter-2 (SGLT-2) inhibitor: characterisation and comparison with other SGLT-2 inhibitors. Diabetes Obes Metab14 (1): 83-90. [PMID:21985634]

3. Inoue T, Takemura M, Fushimi N, Fujimori Y, Onozato T, Kurooka T, Asari T, Takeda H, Kobayashi M, Nishibe H et al.. (2017) Mizagliflozin, a novel selective SGLT1 inhibitor, exhibits potential in the amelioration of chronic constipation. Eur. J. Pharmacol.,  [Epub ahead of print]. [PMID:28410751]

4. Kanai Y, Lee WS, You G, Brown D, Hediger MA. (1994) The human kidney low affinity Na+/glucose cotransporter SGLT2. Delineation of the major renal reabsorptive mechanism for D-glucose. J. Clin. Invest.93 (1): 397-404. [PMID:8282810]

5. Katsuno K, Fujimori Y, Takemura Y, Hiratochi M, Itoh F, Komatsu Y, Fujikura H, Isaji M. (2007) Sergliflozin, a novel selective inhibitor of low-affinity sodium glucose cotransporter (SGLT2), validates the critical role of SGLT2 in renal glucose reabsorption and modulates plasma glucose level. J. Pharmacol. Exp. Ther.320 (1): 323-30. [PMID:17050778]

6. Li AR, Zhang J, Greenberg J, Lee T, Liu J. (2011) Discovery of non-glucoside SGLT2 inhibitors. Bioorg. Med. Chem. Lett.21 (8): 2472-5. [PMID:21398124]

7. Liang Y, Arakawa K, Ueta K, Matsushita Y, Kuriyama C, Martin T, Du F, Liu Y, Xu J, Conway B et al.. (2012) Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models. PLoS ONE7 (2): e30555. [PMID:22355316]

8. Mascitti V, Maurer TS, Robinson RP, Bian J, Boustany-Kari CM, Brandt T, Collman BM, Kalgutkar AS, Klenotic MK, Leininger MT et al.. (2011) Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors. J. Med. Chem.54 (8): 2952-60. [PMID:21449606]

9. Ohtake Y, Sato T, Kobayashi T, Nishimoto M, Taka N, Takano K, Yamamoto K, Ohmori M, Yamaguchi M, Takami K et al.. (2012) Discovery of tofogliflozin, a novel C-arylglucoside with an O-spiroketal ring system, as a highly selective sodium glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes. J. Med. Chem.55 (17): 7828-40. [PMID:22889351]

10. Tahara A, Kurosaki E, Yokono M, Yamajuku D, Kihara R, Hayashizaki Y, Takasu T, Imamura M, Qun L, Tomiyama H et al.. (2012) Pharmacological profile of ipragliflozin (ASP1941), a novel selective SGLT2 inhibitor, in vitro and in vivo. Naunyn Schmiedebergs Arch. Pharmacol.385 (4): 423-36. [PMID:22139434]

11. Zambrowicz B, Freiman J, Brown PM, Frazier KS, Turnage A, Bronner J, Ruff D, Shadoan M, Banks P, Mseeh F et al.. (2012) LX4211, a dual SGLT1/SGLT2 inhibitor, improved glycemic control in patients with type 2 diabetes in a randomized, placebo-controlled trial. Clin. Pharmacol. Ther.92 (2): 158-69. [PMID:22739142]

How to cite this page

Hexose transporter family: Sodium/glucose cotransporter 1. Last modified on 20/04/2017. Accessed on 13/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=915.