ChemicalBook
Chinese Japanese Germany Korea

Canagliflozin

Abstract Oral diabetes drugs Clinical study How it works Invokana tables Taboo References
Canagliflozin
Canagliflozin structure
CAS No.
842133-18-0
Chemical Name:
Canagliflozin
Synonyms
CS-183;TA 7284;Invokana;Cagliflozin;Canaglifozin;Canagliflozi;JNJ 28431754;Canaglifozion;Canagliflozin;JNJ 24831754ZAE
CBNumber:
CB02510088
Molecular Formula:
C24H25FO5S
Formula Weight:
444.52
MOL File:
842133-18-0.mol

Canagliflozin Properties

Boiling point:
642.9±55.0 °C(Predicted)
Density 
1.364
pka
13.34±0.70(Predicted)
CAS DataBase Reference
842133-18-0
FDA UNII
0SAC974Z85
NCI Drug Dictionary
canagliflozin
ATC code
A10BK02

Canagliflozin price More Price(4)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 11575 Canagliflozin ≥98% 842133-18-0 5mg $45 2021-03-22 Buy
Cayman Chemical 11575 Canagliflozin ≥98% 842133-18-0 10mg $81 2021-03-22 Buy
Cayman Chemical 11575 Canagliflozin ≥98% 842133-18-0 25mg $158 2021-03-22 Buy
Cayman Chemical 11575 Canagliflozin ≥98% 842133-18-0 50mg $293 2021-03-22 Buy

Canagliflozin Chemical Properties,Uses,Production

Abstract

Canagliflozin(Invokana) is an oral diabetes medicine that helps control blood sugar levels. It works by helping the kidneys get rid of glucose from your bloodstream. Invokana is used together with diet and exercise to treat type 2 diabetes. To mention the advantage, this drug helps patients to reduce blood sugars without increasing the likelihood of gaining weight as long as a healthy, balanced diet is followed and regular exercise taken.

Oral diabetes drugs

Canagliflozin is an Inhibitor drug for SGLT2. It can lower blood glucose levels by expelling the glucose from the body through the kidneys after its decomposition. In addition, Canagliflozin has a broad prospect due to its significant antiobesity effects and few hypoglycemic events.
According to the results of 2 phase III clinical trials on June 9th, 2012, Canagliflozin, which is an Experimental type 2 diabetes drug of JNJ is better than Januvia of Merck or an older drug called glimepiride. Meanwhile, Canagliflozin has a more significant antiobesity effect. Compared with glimepiride, it causes less hypoglycemic events. On January 11th, 2013, Janssen Pharmaceutical of JNJ announced that its diabetes drug canagliflozin (trade name INVOKANA?)was recommended and approved by the committee of experts of FDA by the vote of 10 to 5 to treat adult patients with type 2 diabetes. On march 29th, 2013, canagliflozin (trade name INVOKANA, Janssen Pharmaceutical China of JNJ)was approved by the US Food and Drug Administration (FDA) to control blood glucose of adult patients with type 2 diabetes. On December 25th, 2013, Janssen Pharmaceutical of JNJ announced that new diabetes drug INVOKANA(canagliflozin)was approved by European Commission(EC)to treat adult patients with type 2 diabetes and improve glucose control. In September, 2014, Canagliflozin Won the positive Suggestions for recommend approval of Committee for Medicinal Products for Human Use (CHMP) of  European Medicines Agency (EMA). In addition, Canagliflozin has been approved by FDA in March this year, and approved by Australia rencently.
Canagliflozin is a once daily oral diabetes drug, which works by inhibiting sodium glucose co-transporter 2 (SGLT2)as a new drug. It can lower blood glucose levels by interdicting the blood glucose reabsorption of the kidneys and increasing the excretion of blood glucose in urine. Compared with non-diabetic population, the kidneys of adult patients with type 2 diabetes absorb a large number of glucose into the blood stream, which will push up the blood glucose levels. Canagliflozin is one of the most promising drug candidates of JNJ. The department of Janssen Pharmaceutical of JNJ has the rights to sell this drug in North America, South America, Europe, Middle East, Africa, Australia, New Zealand and some Asian countries.

Clinical study

Canagliflozin is the first FDA approved inhibitor for SGLT2 and used to treat adult patients with type 2 diabetes. As a kind of glucose transporter, SGLT has two subtypes of SGLT1and SGLT2, which are distributed in the intestinal mucosa and renal tubular respectively, and able to transport glucose into the blood. Canagliflozin can inhibit SLCT2 and, interdict the reabsorption of glucose in Renal tubular and increase the excretion of blood glucose in urine. Thus, the blood glucose levels can be lowered. Glucose was passed into the urine through the kidneys, accompanied by renal impairment, symptomatic hypotension, fungal infections and other side effects. 9 clinical trials involving 10285 patients have demonstrated the safety and efficacy of Invokana, either used alone or in combination with other hypoglycemic agents. In a double-blind controlled trial for 26 weeks, 584 adult patients with type 2 diabetes were divided into three groups, namely 100mg Canagliflozin group, 300mg Canagliflozin group and placebo group. Compared with placebo group, the HbA1c of the 100mg Canagliflozin group and 300mg Canagliflozin group was lowed extra 0.91% and 1.16% respectively.

How it works

Invokana is in a class of drugs called sodium-glucose transport protein 2 (or SGLT2) inhibitors, which drugs work by increasing the amount of glucose that gets passed out in the urine.
When blood passes through the kidneys, the kidneys filter glucose out of the blood and the SGLT proteins then help reabsorb glucose back into the blood.
SGLT2 proteins are responsible for 90% of the glucose that is reabsorbed, so by blocking the action these proteins, less glucose is reabsorbed and so more glucose is excreted via the urine.

Invokana tables

Invokana is supplied as film-coated tablets for oral administration, containing 102 and 306 mg of canagliflozin in each tablet strength, corresponding to 100 mg and 300 mg of canagliflozin (anhydrous), respectively.
Inactive ingredients of the core tablet are croscarmellose sodium, hydroxypropyl cellulose, lactose anhydrous, magnesium stearate, and microcrystalline cellulose. The magnesium stearate is vegetable-sourced. The tablets are finished with a commercially available film-coating consisting of the following excipients: polyvinyl alcohol (partially hydrolyzed), titanium dioxide, macrogol/PEG, talc, and iron oxide yellow, E172 (100 mg tablet only).

Taboo

You should not use Invokana if you have severe kidney disease (or if you are on dialysis).
Invokana is not for treating type 1 diabetes.

References

https://www.drugs.com/cdi/canagliflozin.html
http://www.diabetes.co.uk/diabetes-medication/invokana-canagliflozin.html

Description

In March 2013, the US FDA approved canagliflozin (JNJ-28431754; TA-7284) for the treatment of type 2 diabetes in adults. Canagliflozin is the first US-approved sodium-glucose co-transporter (SGLT) inhibitor for the treatment of type 2 diabetes. Inhibition of renal SGLT suppresses glucose reabsorption, which permits glucose excretion into urine and reduction of hyperglycemia. Canagliflozin was discovered through structural modifications of phlorizin, a known inhibitor of renal glucose reabsorption. Early modifications of OH groups on the glucose moiety were insufficient to adequately impair hydrolysis by intestinal β-glucosidase. Introduction of the C-glucoside moiety, as in the clinical candidate dapagliflozin, afforded sufficient resistance to hydrolysis. Finally, incorporation of the thiophene moiety in canagliflozin provided improved potency for hSGLT2 (exclusive to kidney), IC50=2.2 nM, while offering significant selectivity over hSGLT1 (in kidney and heart), IC50=910 nM. Hyperglycemic, high-fat (HF) diet fedmice (KKstrain) that received a single 3 mg/kg oral dose of canagliflozin had a 48% reduction in blood glucose levels after 6 h versus vehicle-treatedmice. Noteworthy in themultistep synthesis of canagliflozin is the stereoselective formation of the β-C-glucoside which is accomplished by coupling of the aryllithiumaglycone with 2,3,4,6-tetra-O-trimethylsilyl-β-Dgluconolactone followed by desilylation and stereoselective reduction with triethylsilane and boron trifluoride etherate.

Chemical Properties

Pale Yellow Solid

Originator

Mitsubishi Tanabe Pharma (Japan)

Uses

Canagliflozin is a sodium/glucose cotransporter 2 (SGLT2) inhibitor. Canagliflozin has been shown to dose dependently reduce calculated renal threshold for glucose excretion and increase urinary glucose excretion. Canagliflozin is a candidate for the treatment of type 2 diabetes and obesity.

Definition

ChEBI: A C-glycosyl compound that is used (in its hemihydrate form) for treatment of type II diabetes via inhibition of sodium-glucose transport protein subtype 2.

brand name

Invokana

Canagliflozin Preparation Products And Raw materials

Raw materials

Preparation Products


Canagliflozin Suppliers

Global( 332)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Echemi Group
18905328650 86-18905328650
pharma@echemi.com CHINA 215 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22607 55
Hangzhou FandaChem Co.,Ltd.
008615858145714
+86-571-56059825 fandachem@gmail.com CHINA 8909 55
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 E-mail:sales03@shyrchem.com
+86-21-34979012 sales03@shyrchem.com CHINA 739 60
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 26762 60
Anqing Chico Pharmaceutical Co., Ltd.
15380796838
chloewu@chicopharm.cn CHINA 341 58
Lianyungang happen teng technology co., LTD
15950718863
wang666xt@163.com CHINA 296 58
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 29954 58
Biochempartner
0086-13720134139
candy@biochempartner.com CHINA 968 58
Hubei Jusheng Technology Co.,Ltd.
86-18871470254
027-59599243 linda@hubeijusheng.com CHINA 28229 58

View Lastest Price from Canagliflozin manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2021-11-15 Canagliflozin
US $0.00 / KG 1KG 99% 200000pcs Hebei Yirun Sega Biological Technology Co. Ltd
2021-11-09 Canagliflozin
842133-18-0
US $0.00 / Kg/Bag 2Kg/Bag 99% up, High Density 20 tons Sinoway Industrial co., ltd.
2021-10-29 Canagliflozin
842133-18-0
US $0.00 / ASSAYS 100ASSAYS 99.99 10000 Jiangsu Monade Biological Technology Co., Ltd.

842133-18-0(Canagliflozin)Related Search:


  • Canaglifozion
  • D-Glucitol, 1,5-anhydro-1-C-[3-[[5-(4-fluorophenyl)-2-thienyl]Methyl]-4-Methylphenyl]-, (1S)-
  • Cango coluMn net
  • TA 7284
  • Cagliflozin
  • CS-183
  • Invokana
  • Canagliflozin(TA-7284)
  • (2S,3R,4R,5S,6R)-2-(3-((5-(4-fluorophenyl)thiophen-2-yl)methyl)-4-methylphenyl)-6-(hydroxymethyl)-tetrahydro-2H-pyran-3,4,5-triol
  • Canaglifozin
  • Canagliflozin, >=98%
  • Canagliflozin-D6
  • D-Glucitol, 1,5-anhydro-1-C-[3-[[5-(4-fluorophenyl)-2-thienyl]Methyl]-4-Methylphenyl
  • (1S)-1,5-anhydro-1-[3-[[5-(4-fluorophenyl)-2-thienyl]methyl]-4 -methylphenyl]-D-glucitol
  • Canagliflozin WS
  • Canagliflozi
  • (1S)-1,5-Anhydro-1-C-[3-[[5-(4-fluorophenyl)-2-thienyl]methyl]-4-methylphenyl]-D-glucitol
  • JNJ 24831754ZAE
  • JNJ 28431754
  • JNJ 28431754AAA
  • Canagliflozin
  • Canagliflozin fandachem
  • Canagliflozin USP/EP/BP
  • (2S,3R,4R,5S,6R)-2-[3-[[5-(4-fluorophenyl)thiophen-2-yl]methyl]-4-methylphenyl]-6-(hydroxymethyl)oxane-3,4,5-triol
  • 842133-18-0
  • 842133--86-0
  • C24H25FO5S
  • Aromatics
  • Heterocycles
  • Inhibitors
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Sulfur & Selenium Compounds
  • Other APIs
  • Stable Isotopes
Copyright 2017 © ChemicalBook. All rights reserved