Canagliflozin hemihydrate
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MedKoo CAT#: 329456

CAS#: 928672-86-0 (hemihydrate)

Description: Canagliflozin, also known as JNJ-28431754 and TA 7284, is a drug of the gliflozin class or subtype 2 sodium-glucose transport (SGLT-2) 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. Additional water is eliminated by osmotic diuresis, resulting in a lowering of blood pressure.


Price and Availability

Size
Price

500mg
USD 150
5g
USD 750
50g
USD 2450
Size
Price

1g
USD 250
10g
USD 1250
100g
USD 3650
Size
Price

2g
USD 450
20g
USD 1650
200g
USD 4750

Canagliflozin hemihydrate, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 329456
Name: Canagliflozin hemihydrate
CAS#: 928672-86-0 (hemihydrate)
Chemical Formula: C48H52F2O11S2
Exact Mass:
Molecular Weight: 907.0498
Elemental Analysis: C, 63.56; H, 5.78; F, 4.19; O, 19.40; S, 7.07


Related CAS #: 928672-86-0 (hemihydrate)   842133-18-0 (free)    

Synonym: JNJ 28431754; JNJ-28431754; JNJ28431754; TA 7284; TA-7284; TA7284; JNJ-24831754-ZAE; JNJ-28431754-AAA; Canagliflozin hemihydrate; brand name: Invokana. Sulisent.

IUPAC/Chemical Name: (3R,4R,5S,6R)-2-(3-((5-(4-fluorophenyl)thiophen-2-yl)methyl)-4-methylphenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol hemihydrate

InChi Key: VHOFTEAWFCUTOS-HTDYLQHCSA-N

InChi Code: InChI=1S/2C24H25FO5S.H2O/c2*1-13-2-3-15(24-23(29)22(28)21(27)19(12-26)30-24)10-16(13)11-18-8-9-20(31-18)14-4-6-17(25)7-5-14;/h2*2-10,19,21-24,26-29H,11-12H2,1H3;1H2/t2*19-,21-,22+,23-,24?;/m11./s1

SMILES Code: O[C@H]1C(O[C@@H]([C@H]([C@@H]1O)O)CO)C2=CC=C(C(CC3=CC=C(S3)C4=CC=C(C=C4)F)=C2)C.[H]O[H].O[C@H]5C(O[C@@H]([C@H]([C@@H]5O)O)CO)C6=CC=C(C(CC7=CC=C(S7)C8=CC=C(C=C8)F)=C6)C


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

Related CAS#
842133-18-0 (Canagliflozin)
928672-86-0 (Canagliflozin hemihydrate)


References

1: 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. [Epub ahead of print] Review. PubMed PMID: 27854055.

2: Qiu R, Balis D, Capuano G, Xie J, Meininger G. Canagliflozin: Efficacy and Safety in Combination with Metformin Alone or with Other Antihyperglycemic Agents in Type 2 Diabetes. Diabetes Ther. 2016 Oct 12. [Epub ahead of print] Review. PubMed PMID: 27734320.

3: 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.

4: Kaur K, Likar N, Dang A, Kaur G. 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. doi: 10.4103/2230-8210.167562. Review. PubMed PMID: 26693420; PubMed Central PMCID: PMC4673798.

5: Parveen R, Agarwal NB, Kaushal N, Mali G, Raisuddin S. Efficacy and safety of canagliflozin in type 2 diabetes mellitus: systematic review of randomized controlled trials. Expert Opin Pharmacother. 2016;17(1):105-15. doi: 10.1517/14656566.2016.1109629. Review. PubMed PMID: 26650511.

6: Seufert J. SGLT2 inhibitors - an insulin-independent therapeutic approach for treatment of type 2 diabetes: focus on canagliflozin. Diabetes Metab Syndr Obes. 2015 Nov 9;8:543-54. doi: 10.2147/DMSO.S90662. Review. PubMed PMID: 26609242; PubMed Central PMCID: PMC4644173.

7: Syed SH, Gosavi S, Shami W, Bustamante M, Farah Z, Teleb M, Abbas A, Said S, Mukherjee D. A Review of Sodium Glucose Co-transporter 2 Inhibitors Canagliflozin, Dapagliflozin and Empagliflozin. Cardiovasc Hematol Agents Med Chem. 2015;13(2):105-12. Review. PubMed PMID: 26549321.

8: Triplitt C, Cornell S. Canagliflozin Treatment in Patients with Type 2 Diabetes Mellitus. Clin Med Insights Endocrinol Diabetes. 2015 Oct 18;8:73-81. doi: 10.4137/CMED.S31526. Review. PubMed PMID: 26523120; PubMed Central PMCID: PMC4610726.

9: Perkovic V, Jardine M, Vijapurkar U, Meininger G. Renal effects of canagliflozin in type 2 diabetes mellitus. Curr Med Res Opin. 2015 Dec;31(12):2219-31. doi: 10.1185/03007995.2015.1092128. Review. PubMed PMID: 26494163.

10: Rosenthal N, Meininger G, Ways K, Polidori D, Desai M, Qiu R, Alba M, Vercruysse F, Balis D, Shaw W, Edwards R, Bull S, Di Prospero N, Sha S, Rothenberg P, Canovatchel W, Demarest K. Canagliflozin: a sodium glucose co-transporter 2 inhibitor for the treatment of type 2 diabetes mellitus. Ann N Y Acad Sci. 2015 Nov;1358:28-43. doi: 10.1111/nyas.12852. Review. PubMed PMID: 26305874.

11: Fleming JW, Fleming LW, Davis CS. Fixed-dose combinations in type 2 diabetes - role of the canagliflozin metformin combination. Diabetes Metab Syndr Obes. 2015 Jun 25;8:287-94. doi: 10.2147/DMSO.S69282. Review. PubMed PMID: 26150733; PubMed Central PMCID: PMC4485795.

12: Patel S, Gohel K, Patel BG. A Systematic Review on Effect of Canagliflozin in Special Population. Curr Diabetes Rev. 2016;12(3):211-22. Review. PubMed PMID: 26084476.

13: Devineni D, Polidori D. Clinical Pharmacokinetic, Pharmacodynamic, and Drug-Drug Interaction Profile of Canagliflozin, a Sodium-Glucose Co-transporter 2 Inhibitor. Clin Pharmacokinet. 2015 Oct;54(10):1027-41. doi: 10.1007/s40262-015-0285-z. Review. PubMed PMID: 26041408.

14: Scheen AJ. [Canagliflozin (Invokana): kidney SGLT2 cotransporter inhibitor for treating type 2 diabetes]. Rev Med Liege. 2014 Dec;69(12):692-9. Review. French. PubMed PMID: 25796788.

15: Khurana M, Vaidyanathan J, Marathe A, Mehrotra N, Sahajwalla CG, Zineh I, Jain L. Canagliflozin use in patients with renal impairment-Utility of quantitative clinical pharmacology analyses in dose optimization. J Clin Pharmacol. 2015 Jun;55(6):647-56. doi: 10.1002/jcph.466. Review. PubMed PMID: 25612234.

16: Amblee A. Patient profiling in diabetes and role of canagliflozin. Pharmgenomics Pers Med. 2014 Nov 18;7:367-77. doi: 10.2147/52761.S0. Review. PubMed PMID: 25540592; PubMed Central PMCID: PMC4270036.

17: Sehgal V, Bajwa SJ, Sehgal R, Consalvo JA. Management of diabetes in the elderly with canagliflozin: A newer hypoglycemic drug on the horizon. J Pharmacol Pharmacother. 2014 Oct;5(4):227-31. doi: 10.4103/0976-500X.142428. Review. Erratum in: J Pharmacol Pharmacother. 2015 Jan-Mar;6(1):58. PubMed PMID: 25422561; PubMed Central PMCID: PMC4231550.

18: Boyle LD, Wilding JP. A safety evaluation of canagliflozin : a first-in-class treatment for type 2 diabetes. Expert Opin Drug Saf. 2014 Nov;13(11):1535-44. doi: 10.1517/14740338.2014.959488. Review. PubMed PMID: 25340618.

19: Brunton S, Reid TS. Canagliflozin, a sodium glucose co-transporter 2 inhibitor, for the management of type 2 diabetes. Hosp Pract (1995). 2014 Aug;42(3):96-108. doi: 10.3810/hp.2014.08.1122. Review. PubMed PMID: 25255411.

20: Rosiak M, Grzeszczak S, Kosior DA, Postuła M. Emerging treatments in type 2 diabetes: focus on canagliflozin. Ther Clin Risk Manag. 2014 Aug 21;10:683-9. doi: 10.2147/TCRM.S39145. Review. PubMed PMID: 25187722; PubMed Central PMCID: PMC4149387.