Sodium/glucose cotransporter 2

Target id: 916

Nomenclature: Sodium/glucose cotransporter 2

Abbreviated Name: SGLT2

Systematic Nomenclature: SLC5A2

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 2 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 11 672 16p11.2 SLC5A2 solute carrier family 5 member 2
Mouse 11 672 7 70.08 cM Slc5a2 solute carrier family 5 (sodium/glucose cotransporter), member 2
Rat 11 670 1q36 Slc5a2 solute carrier family 5 member 2
Previous and Unofficial Names
low affinity sodium-glucose cotransporter | low affinity Na-dependent glucose transporter (SGLT2) | Na(+)/glucose cotransporter 2 | solute carrier family 5 member 2 | solute carrier family 5 (sodium/glucose cotransporter), member 2
Database Links
Specialist databases
Bioparadigms SLC Tables SLC5A2 (Hs)
Other databases
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Gene
OMIM
UniProtKB
Wikipedia
Substrates and Reaction Kinetics
Substrate Sp. Property Value Units Standard property Standard value Assay description Assay conditions Comments Reference
D-glucose Hs -
α-MDG Hs -
Stoichiometry
1 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
remogliflozin Hs Inhibition 7.9 pKi 2
pKi 7.9 (Ki 1.24x10-8 M) [2]
sergliflozin Hs Inhibition 6.8 pKi 6
pKi 6.8 (Ki 1.58x10-7 M) [6]
dapagliflozin Hs Inhibition 9.3 pIC50 5
pIC50 9.3 (IC50 4.9x10-10 M) [5]
ertugliflozin Hs Inhibition 9.1 pIC50 8
pIC50 9.1 (IC50 8.77x10-10 M) [8]
sotagliflozin Hs Inhibition 8.7 pIC50 11
pIC50 8.7 (IC50 1.8x10-9 M) [11]
tofogliflozin Hs Inhibition 8.5 pIC50 9
pIC50 8.5 (IC50 2.9x10-9 M) [9]
Description: Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing hSGLT2.
empagliflozin Hs Inhibition 8.5 pIC50 3
pIC50 8.5 (IC50 3.2x10-9 M) [3]
canagliflozin Hs Inhibition 8.4 pIC50 7
pIC50 8.4 (IC50 4.4x10-9 M) [7]
ipragliflozin Mm Inhibition 8.3 pIC50 10
pIC50 8.3 (IC50 5.64x10-9 M) [10]
Description: Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing mSGLT2.
ipragliflozin Rn Inhibition 8.2 pIC50 10
pIC50 8.2 (IC50 6.37x10-9 M) [10]
Description: Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing rSGLT2.
ipragliflozin Hs Inhibition 8.1 pIC50 10
pIC50 8.1 (IC50 7.38x10-9 M) [10]
Description: Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing hSGLT2.
View species-specific inhibitor tables
Clinically-Relevant Mutations and Pathophysiology
Disease:  Renal glucosuria
Synonyms: Renal glycosuria [Disease Ontology: DOID:9432]
Disease Ontology: DOID:9432
OMIM: 233100
Orphanet: ORPHA69076
References:  1

References

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1. Calado J, Soto K, Clemente C, Correia P, Rueff J. (2004) Novel compound heterozygous mutations in SLC5A2 are responsible for autosomal recessive renal glucosuria. Hum. Genet.114 (3): 314-6. [PMID:14614622]

2. 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]

3. 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]

4. Hummel CS, Lu C, Loo DD, Hirayama BA, Voss AA, Wright EM. (2011) Glucose transport by human renal Na+/D-glucose cotransporters SGLT1 and SGLT2. Am. J. Physiol., Cell Physiol.300 (1): C14-21. [PMID:20980548]

5. Kang SY, Song KS, Lee J, Lee SH, Lee J. (2010) Synthesis of pyridazine and thiazole analogs as SGLT2 inhibitors. Bioorg. Med. Chem.18 (16): 6069-79. [PMID:20637636]

6. 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]

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 2. Last modified on 22/11/2016. Accessed on 21/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=916.