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Sodium/glucose cotransporter 1

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Target not currently curated in GtoImmuPdb

Target id: 915

Nomenclature: Sodium/glucose cotransporter 1

Abbreviated Name: SGLT1

Systematic Nomenclature: SLC5A1

Family: Hexose transporter family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 13 664 22q12.3 SLC5A1 solute carrier family 5 member 1
Mouse 13 665 5 B1 Slc5a1 solute carrier family 5 (sodium/glucose cotransporter), member 1
Rat 13 665 14q21 Slc5a1 solute carrier family 5 member 1
Previous and Unofficial Names Click here for help
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 | solute carrier family 5 (sodium/glucose cotransporter)
Database Links Click here for help
Specialist databases
Bioparadigms SLC Tables SLC5A1 (Hs)
RESOLUTE SLC5A1 (Hs)
Other databases
Alphafold P13866 (Hs), Q8C3K6 (Mm), P53790 (Rn)
ChEMBL Target CHEMBL4979 (Hs), CHEMBL5374 (Rn)
Ensembl Gene ENSG00000100170 (Hs), ENSMUSG00000011034 (Mm), ENSRNOG00000017775 (Rn)
Entrez Gene 6523 (Hs), 20537 (Mm), 25552 (Rn)
Human Protein Atlas ENSG00000100170 (Hs)
KEGG Gene hsa:6523 (Hs), mmu:20537 (Mm), rno:25552 (Rn)
OMIM 182380 (Hs)
Pharos P13866 (Hs)
UniProtKB P13866 (Hs), Q8C3K6 (Mm), P53790 (Rn)
Wikipedia SLC5A1 (Hs)
Stoichiometry Click here for help
2 Na+ : 1 glucose [6]

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
mizagliflozin Small molecule or natural product Hs Inhibition 7.6 pKi 5
⤷ pKi 7.6 (Ki 2.7x10-8 M) [5]
Description: Monitoring the uptake of 14C-labeled AMG
remogliflozin Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.3 pKi 3
⤷ pKi 5.3 (Ki 4.52x10-6 M) [3]
sergliflozin Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.1 pKi 7
⤷ pKi 5.1 (Ki 7.943x10-6 M) [7]
licogliflozin Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.7 pIC50 1
⤷ pIC50 7.7 (IC50 2.2x10-8 M) [1]
Description: Measuring inhibition of sodium-dependent [14]C- alpha-methyl-glucopyranoside (AMG) transport into the interior of cells transfected with hSGLT1.
sotagliflozin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.4 pIC50 14
⤷ pIC50 7.4 (IC50 3.6x10-8 M) [14]
dapagliflozin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.4 pIC50 8
⤷ pIC50 6.4 (IC50 3.7x10-7 M) [8]
enavogliflozin Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.3 pIC50 2
⤷ pIC50 6.3 (IC50 5.49x10-7 M) [2]
Description: Determined by measuring the uptake of the substrate methyl a-D-glucopyranoside (AMG) in CHO cells expressing hSGLT1.
canagliflozin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.2 pIC50 9
⤷ pIC50 6.2 (IC50 6.84x10-7 M) [9]
ipragliflozin Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inhibition 5.9 pIC50 12
⤷ pIC50 5.9 (IC50 1.166x10-6 M) [12]
Description: Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing rSGLT1.
ipragliflozin Small molecule or natural product Approved drug Click here for species-specific activity table Mm Inhibition 5.9 pIC50 12
⤷ pIC50 5.9 (IC50 1.38x10-6 M) [12]
Description: Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing mSGLT1.
ipragliflozin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 5.7 pIC50 12
⤷ pIC50 5.7 (IC50 1.876x10-6 M) [12]
Description: Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing hSGLT1.
ertugliflozin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 5.7 pIC50 10
⤷ pIC50 5.7 (IC50 1.96x10-6 M) [10]
bexagliflozin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 5.3 pIC50 13
⤷ pIC50 5.3 (IC50 5.6x10-6 M) [13]
empagliflozin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.1 pIC50 4
⤷ pIC50 5.1 (IC50 7.943x10-6 M) [4]
tofogliflozin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 5.1 pIC50 11
⤷ pIC50 5.1 (IC50 8.444x10-6 M) [11]
Description: Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing hSGLT1.
View species-specific inhibitor tables
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Glucose/galactose malabsorption; GGM
Synonyms: Glucose-galactose malabsorption [Orphanet: ORPHA35710]
OMIM: 606824
Orphanet: ORPHA35710

References

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1. Bebernitz GR, Bock MG, Reddy DS, Hajare AK, Vyavahare V, Bhosale B, Kurhade SE, Salunkhe V, Shaikh NS, Bhuniya D et al.. (2011) Glycoside derivatives and uses thereof. Patent number: WO2011048112A1. Assignee: Novartis Ag. Priority date: 20/10/2009. Publication date: 28/04/2011.

2. Choi MK, Nam SJ, Ji HY, Park MJ, Choi JS, Song IS. (2020) Comparative Pharmacokinetics and Pharmacodynamics of a Novel Sodium-Glucose Cotransporter 2 Inhibitor, DWP16001, with Dapagliflozin and Ipragliflozin. Pharmaceutics, 12 (3): 268. [PMID:32183468]

3. 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]

4. 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 Metab, 14 (1): 83-90. [PMID:21985634]

5. 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, 806: 25-31. [PMID:28410751]

6. 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]

7. 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]

8. 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]

9. 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 ONE, 7 (2): e30555. [PMID:22355316]

10. 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]

11. 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]

12. 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]

13. Xu B, Feng Y, Cheng H, Song Y, Lv B, Wu Y, Wang C, Li S, Xu M, Du J et al.. (2011) C-aryl glucosides substituted at the 4'-position as potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes. Bioorg Med Chem Lett, 21 (15): 4465-70. [PMID:21737266]

14. 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 25/01/2023. Accessed on 09/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=915.