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Catalog No.S2760 Synonyms: TA 7284, JNJ 28431754

17 publications

Canagliflozin Chemical Structure

CAS No. 842133-18-0

Canagliflozin (TA 7284, JNJ 28431754) is a highly potent and selective SGLT2 inhibitor for hSGLT2 with IC50 of 2.2 nM in a cell-free assay, exhibits 413-fold selectivity over hSGLT1.

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10mM (1mL in DMSO) GBP 393 In stock
GBP 221 In stock
GBP 303 In stock
GBP 876 In stock
GBP 2022 In stock
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Selleck's Canagliflozin has been cited by 17 publications

5 Customer Reviews

  • Canagliflozin dose-dependently increases pAMPK and pACC in PC3 cells after 30 min

    Mol Metab, 2016, 5(10):1048-56. Canagliflozin purchased from Selleck.

  • Serum lipid and fasting blood glucose levels in Cana- and control-groups after 5 weeks of canagliflozin/vehicle oral administration. Significant reduction in total cholesterol, triglyceride, LDL-cholesterol and fasting blood glucose levels was observed in Cana-group at the end of experimental procedure compared to baseline. Fasting glucose was the only significantly increased parameter observed in the control group at the end of intervention. Data are shown as mean ± SD (***P ≤ 0.001, **P ≤ 0.01)

    Cardiovasc Diabetol, 2018, 17(1):106. Canagliflozin purchased from Selleck.

  • Pretreatment of SGLT inhibitors significantly attenuates sodium nitroprusside (SNP)-induced vascular relaxation in pulmonary arteries. A: dose-response curves of SNP-induced relaxation in the presence or absence of phlorizin in pulmonary arteries (vehicle: 0.05% methanol, phlorizin: 100 µmol/l). Data are means ± SE; n = 4 mice/group. *P < 0.05 vs. vehicle. B: dose-response curves of SNP-induced relaxation in the presence or absence of canagliflozin in pulmonary arteries (vehicle: 0.1% DMSO, canagliflozin: 10 µmol/l). Data are means ± SE; n = 3 mice/group. *P < 0.05 vs. vehicle. C: dose-response curves of SNP-induced relaxation in the presence or absence of phlorizin in coronary arteries. Data are means ± SE; n = 5 mice/group. D: dose-response curves of SNP-induced relaxation in the presence or absence of canagliflozin in coronary arteries. Data are means ± SE; n = 3 mice/group.

    Am J Physiol Lung Cell Mol Physiol, 2015, 309(9):L1027-36. . Canagliflozin purchased from Selleck.

  • Dixon plots for canagliflozin inhibition of the enzyme/substrate pairs: (A) UGT1A1/β-EST; (B) HLM/β-EST; (C) UGT1A9+BSA/4MU; (D) UGT1A9+BSA/PRO; and (E) HLM+BSA/PRO. Concentrations of canagliflozin and substrates are corrected for binding to the respective enzyme sources and BSA (0.5% w/v). Points are experimentally derived values (mean of duplicate estimates; < 5% variance), whereas lines are from fitting with eq. 1 (UGT1A9) or eq. 4 (UGT1A1).

    Drug Metab Dispos, 2015, 43(10):1468-76.. Canagliflozin purchased from Selleck.

  • Plasma concentration of anti-diabetic drugs (A) Canagliflozin in ZDF and SD rat after a single intravenous administration at 1 mg/kg. Data points represent mean ± S.D. (n = 4). *P < 0.05 and **P < 0.01 compared with concentration in SD rats.

    Drug Metab Dispos, 2016, 44(8):1184-92. Canagliflozin purchased from Selleck.

Purity & Quality Control

Choose Selective SGLT Inhibitors

Biological Activity

Description Canagliflozin (TA 7284, JNJ 28431754) is a highly potent and selective SGLT2 inhibitor for hSGLT2 with IC50 of 2.2 nM in a cell-free assay, exhibits 413-fold selectivity over hSGLT1.
mSGLT2 [1]
(Cell-free assay)
rSGLT2 [1]
(Cell-free assay)
hSGLT2 [1]
(Cell-free assay)
2 nM 3.7 nM 4.4 nM
In vitro

Canagliflozin is a novel C-glucoside with thiophene ring. Canagliflozin inhibits Na+-dependent 14C-AMG uptake in a concentration-dependent fashion. Canagliflozin inhibits 14C-AMG uptake in CHO-hSGLT1 and mSGLT1 cells with IC50 of 0.7 μM and >1 μM, respectively. Canagliflozin inhibits the facilitative (non-Na+-linked) GLUT-mediated 2H-2-DG uptake in L6 myoblasts by less than 50%. In sham-injected oocytes, Canagliflozin (10 μM) or phlorizin (3 mM) alone in the presence of 50 μM DNJ does not affect currents. In SGLT3-injected oocytes, DMSO and Canagliflozin 10 μM inhibits DNJ-induced currents by 15.6% and 23.4%, respectively.[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO MXHGeY5kfGmxbjDhd5NigQ>? M3KyTlEzOCCvaX7z M2XVe2lvcGmkaYTpc44hd2ZiaIXtZY4hW0eOVEKg[ZhxemW|c3XkJIlvKEOKTzDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckB2eHSja3Wgc4YhYzF2Q23BUWch[W[2ZYKgNVIxKG2rboOgZpkhXG:yQ3;1cpQhdWW2aH;kMEBKSzVyIE2gNE4xODJ{IN88UU4> MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR2N{e5NUc,Ojh2NEe3PVE9N2F-
CHO MoS1SpVv[3Srb36gZZN{[Xl? MXyxNlAhdWmwcx?= M1;FUmlvcGmkaYTpc44hd2ZiaIXtZY4hW0eOVEGg[ZhxemW|c3XkJIlvKEOKTzDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckB2eHSja3Wgc4YhYzF2Q23BUWch[W[2ZYKgNVIxKG2rboOgZpkhXG:yQ3;1cpQhdWW2aH;kMEBKSzVyIE2gNE4zPjVizszNMi=> NG\iWmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OES0O|c6OSd-Mki0OFc4QTF:L3G+
CHO-K1 M1TpOWZ2dmO2aX;uJIF{e2G7 M{LUN2lvcGmkaYTpc44hd2ZiaIXtZY4hW0eOVEKg[ZhxemW|c3XkJIlvKEOKTz3LNUBk\WyuczDifUBcOTSFXVHNS{B2eHSja3WgZZN{[XluIFnDOVAhRSByLkCwOlch|ryPLh?= NWf6[WJJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVIzPTVpPkKyOlUzOjV3PD;hQi=>
CHO-K1 NVfWS4h5TnWwY4Tpc44h[XO|YYm= NWrQ[3VFUW6qaXLpeIlwdiCxZjDoeY1idiCVR1zUNUBmgHC{ZYPz[YQhcW5iQ1jPMWsyKGOnbHzzJIJ6KFtzNFPdRW1IKHWydHHr[UBie3OjeTygTWM2OCB;IEGuPUDPxE1w NXXndnRQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVIzPTVpPkKyOlUzOjV3PD;hQi=>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
p-β-catenin / β-catenin / Cyclin D1; 

PubMed: 31142735     

CANA treatment upregulated the expression of p-β-catenin and inhibited β-catenin/cyclin D1 signaling in a dose-dependent manner. The relative signal intensity was listed below each band, and the average changes of p-β-catenin in triplicated tests were shown on right.

pACC / ACC / p-AMPKα / AMPKα / p-S6K / S6K / p-S6 / S6 ; 

PubMed: 27689018     

Representative western blot of Canagliflozin treated PC3 cells. Canagliflozin (30 μM) increases pAMPK and pACC and reduces pS6k and pS6. 

31142735 27689018
In vivo Canagliflozin shows pronounced anti-hyperglycemic effects in high-fat diet fed KK (HF-KK) mice. Oral administration at 30 mg/kg of Canagliflozin to male SD rats induces glucose excretion over 24 hours by 3,696 mg per 200 g body weight. Pharmacokinetic studies reveals a much higher exposure of Canagliflozin following oral administration. Following intravenous and oral doses of 3 and 10 mg/kg, respectively, to male SD rats, AUC0−inf, po, t1/2 and oral bioavailability are determined to be 35,980 ng·h/mL, 5.2 hours, and 85%, respectively. Thus, inhibition of SGLT2 in renal tubules after oral dosing of Canagliflozin is likely to continuously suppress reabsorption of glucose. The extensive UGE would reflect excellent pharmacokinetic properties of Canagliflozin in vivo as well as high potency of SGLT2 inhibition. Since most of the filtered glucose is reabsorbed by SGLT2 in the renal tubules, the novel compound would be useful for an anti-diabetic agent. Single oral administration of Canagliflozin at 3 mg/kg remarkably reduced blood glucose levels without influencing food intake in hyperglycemic high-fat diet fed KK (HF-KK) mice. There is a 48% reduction in blood glucose level versus vehicle at 6 hours. In contrast, Canagliflozin only slightly affects blood glucose levels in normoglycemic mice. Therefore, Canagliflozin would control hyperglycemia in the therapy of T2DM with low risk of hypoglycemia. [2]


Cell Research:[1]
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  • Cell lines: L6 cell lines
  • Concentrations: 0-10 μM
  • Incubation Time: 24 hours
  • Method: Cells from the rat skeletal muscle cell line, L6, is used to test the effect of Canagliflozin on glucose transporter 1 (GLUT1) activity. Cells are maintained in Dulbecco's modified Eagle's medium containing 5.6 mM glucose supplemented with 10% fetal bovine serum, are seeded in 24-well plates at a density of 3 × 105 cells/well and cultured for 24 hours in an atmosphere of 5% CO2 at 37 °C. Cells are rinsed twice with Kreb's ringer phosphate HEPES buffer (pH 7.4, 150 mM NaCl, 5 mM KCl, 1.25 mM MgSO4, 1.25 mM CaCl2, 2.9 mM Na2HPO4, 10 mM HEPES) and are pre-incubated with the solutions of Canagliflozin (250 μL, 10 μM) for 5 minutes at room temperature. The transport reaction is initiated by adding 50 μL of 4.5 mM 2-DG (a substrate for GLUTs)/3H-2-DG (0.625 μCi) followed by incubation for 15 minutes at room temperature. The 2-DG uptake is halted by aspiration of the incubation mixture. Cells are immediately washed 3 times with ice-cold PBS. Samples are extracted with 0.3 N NaOH, and radioactivity is determined by liquid scintillation.
    (Only for Reference)
Animal Research:[2]
- Collapse
  • Animal Models: KK (HF-KK) mice
  • Dosages: 10 mg/kg
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 88 mg/mL (197.96 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% CMC+0.25% Tween 80
For best results, use promptly after mixing.
18 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 444.52


CAS No. 842133-18-0
Storage powder
in solvent
Synonyms TA 7284, JNJ 28431754
Smiles CC1=C(C=C(C=C1)C2C(C(C(C(O2)CO)O)O)O)CC3=CC=C(S3)C4=CC=C(C=C4)F

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02891954 Enrolling by invitation Drug: Canagliflozin Diabetes Mellitus Type 2 University of Maryland Baltimore|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) September 2016 Phase 1
NCT02737657 Completed -- Diabetes Mellitus Type 2 Janssen-Cilag International NV April 2016 --
NCT02857764 Completed -- Diabetes Mellitus Type 2 Janssen Research & Development LLC February 15 2016 --
NCT02688075 Completed Other: No Intervention Diabetes Mellitus Type 2 Janssen Inc. November 13 2015 --

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID