Canagliflozin
Based on 47 publication(s) in Google Scholar
Canagliflozin (JNJ 28431754) is a selective SGLT2 inhibitor with IC50s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively.
For research use only. We do not sell to patients.
- Purity: 99.99%
- CAS No.: 842133-18-0
- Formula: C24H25FO5S
- Molecular Weight:444.52
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
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Publications Citing Use of MedChemExpress (MCE) Canagliflozin
More- Nature. 2018 Aug;560(7719):499-503. [Abstract]
- Nat Cancer. 2024 Mar;5(3):433-447. [Abstract]
- Nat Cell Biol. 2022 Jun;24(6):954-967. [Abstract]
- Mol Cell. 2020 Oct 1;80(1):87-101.e5. [Abstract]
- Nat Commun. 2025 Dec 19. [Abstract]
- Cardiovasc Res. 2023 Oct 24;119(13):2368-2381. [Abstract]
- Cardiovasc Res. 2021 Dec 17;117(14):2794-2806. [Abstract]
- Cell Commun Signal. 2024 Nov 7;22(1):534. [Abstract]
- Acta Pharmacol Sin. 2024 Dec;45(12):2579-2597. [Abstract]
- Diabetes. 2025 Feb 11:db240955. [Abstract]
- Biomed Pharmacother. 2024 Jun 27:177:117044. [Abstract]
- Biomed Pharmacother. 2023 Aug:164:114907. [Abstract]
- Biomed Pharmacother. 2023 Mar:159:114228. [Abstract]
- Biomed Pharmacother. 2020 Dec;132:110821. [Abstract]
- Arch Toxicol. 2025 Feb;99(2):729-744. [Abstract]
- Neurotherapeutics. 2023 Dec 19, e00305.
- Antioxidants (Basel). 2024 Jul 11;13(7):831. [Abstract]
- Antioxidants (Basel). 2023 Mar 30;12(4):838. [Abstract]
- Biochem Pharmacol. 2020 May;175:113856. [Abstract]
- Biochem Pharmacol. 2018 Jun:152:45-59. [Abstract]
- Can J Cardiol. 2026 Apr 24:S0828-282X(26)00372-7. [Abstract]
- J Am Heart Assoc. 2022 Aug 2;11(15):e025328. [Abstract]
- Commun Biol. 2023 Sep 8;6(1):919. [Abstract]
- Int J Mol Sci. 2025 Oct 16;26(20):10098. [Abstract]
- Int J Mol Sci. 2025 Jan 24;26(3):978. [Abstract]
- Int J Mol Sci. 2024 Jul 10;25(14):7567. [Abstract]
- Int J Oncol. 2020 Nov;57(5):1223-1233. [Abstract]
- Front Pharmacol. 2025 Apr 30:16:1573032. [Abstract]
- Int Immunopharmacol. 2020 Nov;88:106969. [Abstract]
- Mol Oncol. 2023 Nov;17(11):2235-2256. [Abstract]
- FASEB J. 2025 Jul 31;39(14):e70880. [Abstract]
- FASEB J. 2025 May 31;39(10):e70630. [Abstract]
- Sci Rep. 2021 Jul 1;11(1):13700. [Abstract]
- Biochim Biophys Acta Mol Cell Res. 2025 Oct 12;1873(1):120069. [Abstract]
- Mol Cell Endocrinol. 2024 Mar 1:582:112139. [Abstract]
- Mol Med Rep. 2021 Oct;24(4):703. [Abstract]
- Vascul Pharmacol. 2018 Oct:109:56-71. [Abstract]
- Calcif Tissue Int. 2026 Jan 31;117(1):20. [Abstract]
- Int J Med Sci. 2018 Jun 13;15(9):937-943. [Abstract]
- J Diabetes Investig. 2025 Aug;16(8):1430-1444. [Abstract]
- Biochem Biophys Res Commun. 2023 Apr 23:653:53-61. [Abstract]
- Biomed Chromatogr. 2019 Nov;33(11):e4663. [Abstract]
- Biomed Chromatogr. 2016 Oct;30(10):1549-55. [Abstract]
- University of Porto. 2025.
- University of Porto. 2025.
- Patent. US20210236501A1.
- Research Square Preprint. 2023 Dec 28.
Customer Validation & Images
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Biological Activity
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SGLT2 |
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Cell Line
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Type | Value | Description | References |
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| CHO-K1 | IC50 |
1900 nM
Compound: 4
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Inhibition of human SGLT1 expressed in CHO-K1 cells by [14C]AMG uptake assay
Inhibition of human SGLT1 expressed in CHO-K1 cells by [14C]AMG uptake assay
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[PMID: 22652255] |
| CHO-K1 | IC50 |
6.7 nM
Compound: 4
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Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay
Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay
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[PMID: 22652255] |
Canagliflozin inhibits Na+-dependent 14C-AMG uptake in CHO-hSGLT2 cells, with an IC50 of 4.4±1.2 nM. Similar IC50 values are obtained in CHO-rSGLT2 and CHO-mSGLT2 cells (IC50 = 3.7 and 2.0 nM for rat and mouse SGLT2, respectively). Canagliflozin inhibits 14C-AMG uptake in CHO-hSGLT1 and mSGLT1 cells with IC50 of 684±159 nM and >1,000 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Canagliflozin (3 mg/kg for 3 weeks) increases urinary glucose excretion (UGE) with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight In ZF rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Diet-induced obese, insulin resistantmice (DIO) Mice[1]
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Dosage:30 mg/kg
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Administration:Oral gavage; daily; 4 weeks
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Result:Reduced BG levels, respiratory exchange ratio, and body weight gain.
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Animal Model:Male Zucker fatty (ZF) obese, insulin resistant rats[1]
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Dosage:3 mg/kg
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Administration:Oral gavage; daily; 3 weeks
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Result:UGE was increased with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight.
Chemical Information
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CAS No. 842133-18-0
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Appearance Solid
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Molecular Weight 444.52
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Formula C24H25FO5S
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Color White to light yellow
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SMILES
FC1=CC=C(C2=CC=C(CC3=C(C=CC([C@@H]4O[C@@H]([C@H]([C@@H]([C@H]4O)O)O)CO)=C3)C)S2)C=C1
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Synonyms
JNJ 28431754
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (47)
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Journal Impact Factor
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Most Recent
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Nature
2018 Aug;560(7719):499-503. PMID: 30051890 -
Nat Cancer
Loss of Pip4k2c confers liver-metastatic organotropism through insulin-dependent PI3K-AKT pathway activation. [Abstract]2024 Mar;5(3):433-447. PMID: 38286827 -
Nat Cell Biol
Cancer-cell-secreted extracellular vesicles suppress insulin secretion through miR-122 to impair systemic glucose homeostasis and contribute to tumour growth. [Abstract]2022 Jun;24(6):954-967. PMID: 35637408 -
Mol Cell
Cell-Autonomous versus Systemic Akt Isoform Deletions Uncovered New Roles for Akt1 and Akt2 in Breast Cancer. [Abstract]2020 Oct 1;80(1):87-101.e5. PMID: 32931746 -
Nat Commun
IDH2 lactylation promotes angiogenesis in murine diabetic myocardial infarction via blocking Cav1-eNOS interaction. [Abstract]2025 Dec 19. PMID: 41419771 -
Cardiovasc Res
SGLT2 inhibitor canagliflozin alleviates vascular calcification through suppression of NLRP3 inflammasome. [Abstract]2023 Oct 24;119(13):2368-2381. PMID: 37523743 -
Cardiovasc Res
Off-target effects of sodium-glucose co-transporter 2 blockers: empagliflozin does not inhibit Na+/H+ exchanger-1 or lower [Na+]i in the heart. [Abstract]2021 Dec 17;117(14):2794-2806. PMID: 33135077 -
Cell Commun Signal
Inhibition of SGLT2 protects podocytes in diabetic kidney disease by rebalancing mitochondria-associated endoplasmic reticulum membranes. [Abstract]2024 Nov 7;22(1):534. PMID: 39511548 -
Acta Pharmacol Sin
SGLT2 inhibitors ameliorate NAFLD in mice via downregulating PFKFB3, suppressing glycolysis and modulating macrophage polarization. [Abstract]2024 Dec;45(12):2579-2597. PMID: 39294445 -
Diabetes
2025 Feb 11:db240955. PMID: 39932694 -
Biomed Pharmacother
Xelaglifam, a novel GPR40/FFAR1 agonist, exhibits enhanced β-arrestin recruitment and sustained glycemic control for type 2 diabetes. [Abstract]2024 Jun 27:177:117044. PMID: 38941892 -
Biomed Pharmacother
Canagliflozin mitigates carfilzomib-induced endothelial apoptosis via an AMPK-dependent pathway. [Abstract]2023 Aug:164:114907. PMID: 37247463 -
Biomed Pharmacother
Canagliflozin inhibits inflammasome activation in diabetic endothelial cells - Revealing a novel calcium-dependent anti-inflammatory effect of canagliflozin on human diabetic endothelial cells. [Abstract]2023 Mar:159:114228. PMID: 36623448 -
Biomed Pharmacother
Sodium-glucose co-transporter-2 (SGLT-2) inhibition reduces glucose uptake to induce breast cancer cell growth arrest through AMPK/mTOR pathway. [Abstract]2020 Dec;132:110821. PMID: 33068934
Canagliflozin purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Dec;132:110821. [Abstract]
MCF-7 and ZR-75-1 cells are exposed to Canagliflozin 0, 11, 33, and 100 μM for 24 h and protein levels of p-AMPK, total AMPK, p-p70S6K1 and total p70S6K1 are detected using immunoblot assay.
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Arch Toxicol
Canagliflozin differentially modulates carfilzomib-induced endoplasmic reticulum stress in multiple myeloma and endothelial cells. [Abstract]2025 Feb;99(2):729-744. PMID: 39645617 -
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Antioxidants (Basel)
Canagliflozin Inhibits Palmitic Acid-Induced Vascular Cell Aging In Vitro through ROS/ERK and Ferroptosis Pathways. [Abstract]2024 Jul 11;13(7):831. PMID: 39061899 -
Antioxidants (Basel)
Canagliflozin Delays Aging of HUVECs Induced by Palmitic Acid via the ROS/p38/JNK Pathway. [Abstract]2023 Mar 30;12(4):838. PMID: 37107212 -
Biochem Pharmacol
Canagliflozin inhibits p-gp function and early autophagy and improves the sensitivity to the antitumor effect of doxorubicin. [Abstract]2020 May;175:113856. PMID: 32061772 -
Biochem Pharmacol
Canagliflozin exerts anti-inflammatory effects by inhibiting intracellular glucose metabolism and promoting autophagy in immune cells. [Abstract]2018 Jun:152:45-59. PMID: 29551587
Canagliflozin purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Jun:152:45-59. [Abstract]
Effects of NF-κB inhibitor (10 μM MLN120B) is measured on p62 protein in LPS-induced RAW264.7 cells.
Canagliflozin purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Jun:152:45-59. [Abstract]
PFK2 expression is significantly increased by LPS but is attenuated by Canagliflozin (CAN).
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Can J Cardiol
Canagliflozin Alleviates Pressure Overload-Induced Cardiac Dysfunction via PINK1 Regulation by Inhibiting Mitophagy-Driven Ferroptosis. [Abstract]2026 Apr 24:S0828-282X(26)00372-7. PMID: 42035950 -
J Am Heart Assoc
Sodium-Glucose Cotransporter 2 Inhibitor Canagliflozin Antagonizes Salt-Sensitive Hypertension Through Modifying Transient Receptor Potential Channels 3 Mediated Vascular Calcium Handling. [Abstract]2022 Aug 2;11(15):e025328. PMID: 35904193 -
Commun Biol
The SGLT2 inhibitor canagliflozin suppresses growth and enhances prostate cancer response to radiotherapy. [Abstract]2023 Sep 8;6(1):919. PMID: 37684337 -
Int J Mol Sci
Comparison of the Effects of Sodium-Glucose Cotransporter 2 Inhibitors on Cardiac Fibroblast Properties. [Abstract]2025 Oct 16;26(20):10098. PMID: 41155391 -
Int J Mol Sci
Dual Roles of Canagliflozin on Cholangiocarcinoma Cell Growth and Enhanced Growth Suppression in Combination with FK866. [Abstract]2025 Jan 24;26(3):978. PMID: 39940750 -
Int J Mol Sci
SGLT2 Inhibitors Empagliflozin and Canagliflozin Ameliorate Allergic Asthma Responses in Mice. [Abstract]2024 Jul 10;25(14):7567. PMID: 39062810 -
Int J Oncol
Inhibitory effects of canagliflozin on pancreatic cancer are mediated via the downregulation of glucose transporter‑1 and lactate dehydrogenase A. [Abstract]2020 Nov;57(5):1223-1233. PMID: 32901837 -
Front Pharmacol
Canagliflozin alleviates progestin resistance by suppressing RARβ/CRABP2 signaling in THRB knockout endometrial cancer cells. [Abstract]2025 Apr 30:16:1573032. PMID: 40371351 -
Int Immunopharmacol
Canagliflozin alleviates LPS-induced acute lung injury by modulating alveolar macrophage polarization. [Abstract]2020 Nov;88:106969. PMID: 33182027 -
Mol Oncol
Canagliflozin mediates tumor suppression alone and in combination with radiotherapy in non-small cell lung cancer (NSCLC) through inhibition of HIF-1α. [Abstract]2023 Nov;17(11):2235-2256. PMID: 37584455 -
FASEB J
Deubiquitinase OTUD4 Stabilizes SLC5A2 to Promote Pancreatic Cancer Proliferation and Migration Through Enchaining Glycolysis-Mediated Autophagy. [Abstract]2025 Jul 31;39(14):e70880. PMID: 40719816 -
FASEB J
Canagliflozin Delays Aortic Valve Calcification by Enhancing the AMPK/Nrf2/HO-1 Antioxidant Signaling Pathway in Valvular Interstitial Cells. [Abstract]2025 May 31;39(10):e70630. PMID: 40357866 -
Sci Rep
Canagliflozin protects against sepsis capillary leak syndrome by activating endothelial α1AMPK. [Abstract]2021 Jul 1;11(1):13700. PMID: 34211080 -
Biochim Biophys Acta Mol Cell Res
Canagliflozin inhibits p38MAPK signaling to protect tubular epithelial cell against pyroptosis in sepsis-induced acute kidney injury. [Abstract]2025 Oct 12;1873(1):120069. PMID: 41086994 -
Mol Cell Endocrinol
Canagliflozin improves fatty acid oxidation and ferroptosis of renal tubular epithelial cells via FOXA1-CPT1A axis in diabetic kidney disease. [Abstract]2024 Mar 1:582:112139. PMID: 38128823 -
Mol Med Rep
Canagliflozin is a potential cardioprotective drug but exerts no significant effects on pirarubicin‑induced cardiotoxicity in rats. [Abstract]2021 Oct;24(4):703. PMID: 34368866 -
Vascul Pharmacol
Hyperglycaemic impairment of PAR2-mediated vasodilation: Prevention by inhibition of aortic endothelial sodium-glucose-co-Transporter-2 and minimizing oxidative stress. [Abstract]2018 Oct:109:56-71. PMID: 29908295 -
Calcif Tissue Int
Effect of Canagliflozin Pretreatment on the Efficacy of Insulin Therapy to Rescue Type 1 Diabetes-Related Bone Fragility in Male Mice. [Abstract]2026 Jan 31;117(1):20. PMID: 41618015 -
Int J Med Sci
Susceptibility to serious skin and subcutaneous tissue disorders and skin tissue distribution of sodium-dependent glucose co-transporter type 2 (SGLT2) inhibitors. [Abstract]2018 Jun 13;15(9):937-943. PMID: 30008607 -
J Diabetes Investig
Canagliflozin protects cardiovascular function in type 2 diabetic coronary artery disease by regulating natriuretic peptide B. [Abstract]2025 Aug;16(8):1430-1444. PMID: 40390212 -
Biochem Biophys Res Commun
Canagliflozin ameliorates epithelial-mesenchymal transition in high-salt diet-induced hypertensive renal injury through restoration of sirtuin 3 expression and the reduction of oxidative stress. [Abstract]2023 Apr 23:653:53-61. PMID: 36857900 -
Biomed Chromatogr
A new HPLC-MS/MS method for the simultaneous quantification of SGLT2 inhibitors and metformin in plasma and its application to a pharmacokinetic study in healthy volunteers. [Abstract]2019 Nov;33(11):e4663. PMID: 31339572 -
Biomed Chromatogr
A validated LC-MS/MS method for the determination of canagliflozin, a sodium-glucose co-transporter 2 (SGLT-2) inhibitor, in a lower volume of rat plasma: application to pharmacokinetic studies in rats. [Abstract]2016 Oct;30(10):1549-55. PMID: 26989857 -
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Solvent & Solubility
DMSO : ≥ 50 mg/mL (112.48 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.68 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.68 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 1% DMSO 99% Saline
Solubility: ≥ 0.5 mg/mL (1.12 mM); Clear solution
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (22.50 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (580 KB)
- English - EN (580 KB)
- Français - FR (580 KB)
- Deutsch - DE (580 KB)
- Norwegian - NO (580 KB)
- Español - ES (580 KB)
- Swedish - SV (580 KB)
- Italian - IT (580 KB)
- Korean - KR (580 KB)
- Portuguese - PT (580 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2496 mL | 11.2481 mL | 22.4962 mL | 56.2404 mL |
| 5 mM | 0.4499 mL | 2.2496 mL | 4.4992 mL | 11.2481 mL | |
| 10 mM | 0.2250 mL | 1.1248 mL | 2.2496 mL | 5.6240 mL | |
| 15 mM | 0.1500 mL | 0.7499 mL | 1.4997 mL | 3.7494 mL | |
| 20 mM | 0.1125 mL | 0.5624 mL | 1.1248 mL | 2.8120 mL | |
| 25 mM | 0.0900 mL | 0.4499 mL | 0.8998 mL | 2.2496 mL | |
| 30 mM | 0.0750 mL | 0.3749 mL | 0.7499 mL | 1.8747 mL | |
| 40 mM | 0.0562 mL | 0.2812 mL | 0.5624 mL | 1.4060 mL | |
| 50 mM | 0.0450 mL | 0.2250 mL | 0.4499 mL | 1.1248 mL | |
| 60 mM | 0.0375 mL | 0.1875 mL | 0.3749 mL | 0.9373 mL | |
| 80 mM | 0.0281 mL | 0.1406 mL | 0.2812 mL | 0.7030 mL | |
| 100 mM | 0.0225 mL | 0.1125 mL | 0.2250 mL | 0.5624 mL |
Canagliflozin Related Classifications
HY-10451 Related Classifications
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