Canagliflozin (JNJ 28431754)
For research use only.
Catalog No.S2760 Synonyms: TA 7284
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.
Selleck's Canagliflozin (JNJ 28431754) has been cited by 17 publications
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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 (JNJ 28431754) 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 (JNJ 28431754) 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 (JNJ 28431754) 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 (JNJ 28431754) purchased from Selleck.
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Choose Selective SGLT Inhibitors
|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.|
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.
|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. |
|In vitro||DMSO||88 mg/mL (197.96 mM)|
|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.
* 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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04720859||Recruiting||Drug: Canagliflozin 300 MG Oral Tablet||Postprandial Hypoglycemia||Hospital Universitari Vall d''Hebron Research Institute||January 5 2018||Not Applicable|
|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|
|NCT01877889||Completed||Drug: Canagliflozin|Drug: Dapagliflozin||Healthy||Janssen-Cilag International NV||July 2013||Phase 1|
|NCT01718652||Completed||Drug: Canagliflozin (JNJ-28431754)|Drug: Cyclosporine||Healthy||Johnson & Johnson Pharmaceutical Research & Development L.L.C.||February 2011||Phase 1|
|NCT01186588||Completed||Drug: Canagliflozin||Healthy|Hepatic Insufficiency||Johnson & Johnson Pharmaceutical Research & Development L.L.C.||August 2010||Phase 1|
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