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Canagliflozin hemihydrate

Catalog No. T1782L CAS 928672-86-0

Synonyms: JNJ28431754, TA 7284, TA7284, TA-7284, JNJ 28431754, JNJ-28431754

Canagliflozin hemihydrate (TA 7284) is a drug of the gliflozin class or subtype 2 sodium-glucose transport inhibitors used for the treatment of type 2 diabetes. SGLT2 is responsible for at least 90% of renal glucose reabsorption (SGLT1 being responsible for the remaining 10%). Blocking this transporter causes up to 119 grams of blood glucose per day to be eliminated through the urine, corresponding to 476 kilocalories.

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Canagliflozin hemihydrate Chemical Structure

Canagliflozin hemihydrate, CAS 928672-86-0

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25 mg	In stock	$ 49.00
1 mL * 10 mM (in DMSO)	In stock	$ 43.00

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Purity: 99.96%

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Description	Canagliflozin hemihydrate (TA 7284) is a drug of the gliflozin class or subtype 2 sodium-glucose transport inhibitors used for the treatment of type 2 diabetes. SGLT2 is responsible for at least 90% of renal glucose reabsorption (SGLT1 being responsible for the remaining 10%). Blocking this transporter causes up to 119 grams of blood glucose per day to be eliminated through the urine, corresponding to 476 kilocalories.
Targets&IC50	mSGLT2/rSGLT2/hSGLT2 (CHOK cells):2/3.7/4.4 nM (IC50)
In vitro	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].
In vivo	Canagliflozin (30 mg/kg treatment for 4 weeks) reduced blood glucose (BG) levels, respiratory exchange ratio, and body weight gain in DIO mice[1]. 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].

Synonyms	JNJ28431754, TA 7284, TA7284, TA-7284, JNJ 28431754, JNJ-28431754
Molecular Weight	907.05
Formula	C48H52F2O11S2
CAS No.	928672-86-0

Storage

store at low temperature

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

Solubility Information

DMSO: 90mg/mL (198.4mM)

References and Literature

1. Liang Y, et al. Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models. PLoS One. 2012;7(2):e30555. 2. Davidson JA, Sloan L. Fixed-Dose Combination of Canagliflozin and Metformin for the Treatment of Type 2 Diabetes: An Overview. Adv Ther. 2016 Nov 16. 3. Qiu R, et al. Canagliflozin: Efficacy and Safety in Combination with Metformin Alone or with Other Antihyperglycemic Agents in Type 2 Diabetes. Diabetes Ther. 2016 Oct 12. 4. Canagliflozin (Invokana) for Type 2 Diabetes Mellitus [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2015 Sep. Available from http://www.ncbi.nlm.nih.gov/books/NBK349575/ PubMed PMID: 26962611. 5. Kaur K, et al. Efficacy and safety of canagliflozin among patients with type 2 diabetes mellitus: A systematic review and meta-analysis. Indian J Endocrinol Metab. 2015 Nov-Dec;19(6):705-21.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library EMA Approved Drug Library Highly Selective Inhibitor Library Anti-Cancer Clinical Compound Library Inhibitor Library Anti-Cancer Approved Drug Library GPCR Compound Library Membrane Protein-targeted Compound Library Drug Repurposing Compound Library Bioactive Compounds Library Max

Related Products

Related compounds with same targets

SGLT inhibitor-1 Sotagliflozin Empagliflozin Tofogliflozin (hydrate) Phlorizin Velagliflozin Dapagliflozin Dapagliflozin ((2S)-1,2-propanediol, hydrate)

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Keywords

Canagliflozin hemihydrate 928672-86-0 GPCR/G Protein SGLT Canagliflozin JNJ28431754 TA 7284 TA7284 TA-7284 JNJ 28431754 JNJ-28431754 Canagliflozin Hemihydrate inhibitor inhibit

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