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Canagliflozin

Catalog No. T1782 CAS 842133-18-0

Synonyms: JNJ 24831754ZAE, JNJ 28431754AAA, TA 7284, JNJ 28431754

Canagliflozin (JNJ 28431754AAA), a sodium-glucose transporter 2( SGLT2) and P-Glycoprotein inhibitor, is used in type 2 diabetes.

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Canagliflozin, CAS 842133-18-0

Pack Size	Availability	Price/USD
5 mg	In stock	$ 43.00
10 mg	In stock	$ 61.00
50 mg	In stock	$ 97.00
100 mg	In stock	$ 125.00
200 mg	In stock	$ 185.00
500 mg	In stock	$ 313.00
1 mL * 10 mM (in DMSO)	In stock	$ 48.00

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Purity: 100%

Purity: 99.76%

Purity: 99.72%

Purity: 98.01%

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Storage & Solubility Information

Description	Canagliflozin (JNJ 28431754AAA), a sodium-glucose transporter 2( SGLT2) and P-Glycoprotein inhibitor, is used in type 2 diabetes.
Targets&IC50	SGLT2 (rat):3.7 nM, SGLT2 (mouse):2 nM, SGLT2 (human):4.4 nM
In vitro	In oocytes injected with SGLT3, Canagliflozin (10 μM) inhibits the DNJ-induced current. It also suppresses the uptake of 14C-AMG in CHO-hSGLT1 cells (IC50=0.7 μM) and mSGLT1 cells (IC50=>1 μM). Additionally, in L6 myoblasts, Canagliflozin inhibits the absorption of 2H-2-DG regulated by GLUT that is not associated with Na+ (non-Na+-linked).
In vivo	In KK mice fed a high-fat and high-sugar diet, oral administration of Canagliflozin (3 mg/kg) demonstrated a significant anti-hyperglycemic effect. Similarly, in male SD rats, oral ingestion of Canagliflozin (30 mg/kg) induced glucose excretion and effectively reduced blood sugar levels.
Cell Research	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)

Synonyms	JNJ 24831754ZAE, JNJ 28431754AAA, TA 7284, JNJ 28431754
Molecular Weight	444.52
Formula	C24H25FO5S
CAS No.	842133-18-0

Storage

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 82 mg/mL (184.5 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Liang Y, et al. PLoS One. 2012, 7(2), e30555. 2. Nomura S, et al. J Med Chem. 2010, 53(17), 6355-6360.

Citations

1. Ding L, Chen X, Zhang W, et al.Canagliflozin primes antitumor immunity by triggering PD-L1 degradation in endocytic recycling.The Journal of Clinical Investigation.2023, 133(1). 2. Huang H, Kung F L, Huang Y W, et al.Sensitization of cancer cells to paclitaxel-induced apoptosis by canagliflozin.Biochemical Pharmacology.2024: 116140.

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library EMA Approved Drug Library Inhibitor Library Anti-Cancer Drug Library Membrane Protein-targeted Compound Library GPCR Compound Library Target-Focused Phenotypic Screening Library

Related Products

Related compounds with same targets

Empagliflozin Picraline Dapagliflozin ((2S)-1,2-propanediol, hydrate) Canagliflozin hemihydrate Phloretin Mizagliflozin Ertugliflozin L-pyroglutamic acid LY2794193

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Keywords

Canagliflozin 842133-18-0 GPCR/G Protein SGLT Sodium-dependent glucose cotransporters TA-7284 JNJ 24831754ZAE JNJ 28431754AAA TA 7284 JNJ-28431754 Inhibitor JNJ 28431754 inhibit JNJ28431754 TA7284 inhibitor

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