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Canagliflozin



Chemical Properties of 'Canagliflozin'

CAT No. :

CS-O-10825
CAS Registry No. : 842133-18-0
Category : API Standards
Molecular Weight: 444.52
Molecular Formula : C₂₄H₂₅FO₅S



OTHER INFORMATION of 'Canagliflozin'
Purity : Not less than 95%
Therapeutic : Anti-Diabetic
Purity : Not less than 95%
Therapeutic : Anti-Diabetic
IUPAC Name :(2S,3R,4R,5S,6R)-2-[3-[[5-(4-fluorophenyl)thiophen-2-yl]methyl]-4-methylphenyl]-6-(hydroxymethyl)oxane-3,4,5-triol
Applicationnotes :Canagliflozin belongs to a new class of anti-diabetic drugs that works by inhibiting the sodium-glucose transport protein (SGLT2). This transport protein is found in the kidney and is responsible for reabsorbing glucose that has been filtered.
Synonym :Not available
References :"Chao; E, et al,: Drug Fut,; 36; 351 (2011); Sha; S, et al,: Diab, Obes, Metab,; 13; 669 (2011); Kipnes; M,S,: Clin, Invest,; 1; 145 (2011);"
Smileys :CC1=C(C=C(C=C1)C2C(C(C(C(O2)CO)O)O)O)CC3=CC=C(S3)C4=CC=C(C=C4)F
Appearance :White to off white powder
Melting Point :68-72
Boiling Point :‎642.9±55.0
Solubility :almost insoluble
Use Classification :Human drugs -> Invokana -> EMA Drug Category
Hazard Class :Acute Tox. 4 (33.33%)
EC Number :695-192-1
UNII :6S49DGR869
NCI Thesaurus Code :C91019
RXCUI :1546031
MeSH Entry Terms :1-(Glucopyranosyl)-4-methyl-3-(5-(4-fluorophenyl)-2-thienylmethyl)benzene - T777973
Other Synonyms :Canagliflozin
Removed Synonyms :Canagliflozin/
Vapor Pressure : 1.07X10-18 mm Hg at 25 °C (est)
Other Experimental Properties :log Kow: 1.59; Koc: 5.9 /Canagliflozin hemihydrate (928672-86-0)/
Label Ingredient : CANAGLIFLOZIN
NDC Code :50090-4364-0, 50090-5029-0, 50090-5033-0, 50090-5033-1, 50090-5034-0, 50090-5034-1, 50458-140-01, 50458-140-10, 50458-140-30, 50458-140-50 ... total 37.
Disposal Methods :SRP: Expired or waste pharmaceuticals shall carefully take into consideration applicable DEA, EPA, and FDA regulations. It is not appropriate to dispose by flushing the pharmaceutical down the toilet or discarding to trash. If possible return the pharmaceutical to the manufacturer for proper disposal being careful to properly label and securely package the material. Alternatively, the waste pharmaceutical shall be labeled, securely packaged and transported by a state licensed medical waste contractor to dispose by burial in a licensed hazardous or toxic waste landfill or incinerator.
Toxicity Summary :**Overdose information** If an overdose occurs, contact the Poison Control Center. Normal supportive measures should be taken, including the removal unabsorbed drug from the gastrointestinal tract, initiating clinical monitoring of the patient, and providing supportive treatment as deemed necessary. Canagliflozin has been removed in very small quantities after a 4-hour hemodialysis session. This drug is likely not dialyzable by peritoneal dialysis. **Pregnancy and lactation** Animal data has demonstrated that canagliflozin may cause adverse renal effects in a growing fetus. Data are insufficient at this time in determining a potential canagliflozin related risk for major birth defects or possible miscarriage in humans. There are known risks, however, of uncontrolled diabetes in pregnancy. Inform female patients taking canagliflozin of the potential risk, which is increased during the second and third trimesters. This drug is not recommended during nursing. **Mutagenesis and carcinogenicity** Canagliflozin was not found to be mutagenic in both metabolically activated and inactivated states in the Ames assay. Canagliflozin showed mutagenicity in laboratory mouse lymphoma assay, but only in the activated state. Canagliflozin was not found to be mutagenic in several _in vivo_ assays performed on rats. The carcinogenic risk of canagliflozin was assessed in 2-year studies completed in both CD1 mice and Sprague-Dawley rats. Canagliflozin was not shown to increase tumor incidence in mouse models given doses less than or equal to 14 times the exposure from a typical 300 mg dose in humans. Despite these negative findings in mice, the incidence of several tumors increased in mice, including Leydig cell tumors, renal tubular adenomas, and adrenal pheochromocytomas.
Interactions :Inhibitors of sodium-glucose cotransporters type 2 (SGLT2) reduce hyperglycaemia by decreasing renal glucose threshold and thereby increasing urinary glucose excretion. They are proposed as a novel approach for the management of type 2 diabetes mellitus. They have proven their efficacy in reducing glycated haemoglobin, without inducing hypoglycaemia, as monotherapy or in combination with various other glucose-lowering agents, with the add-on value of promoting some weight loss and lowering arterial blood pressure. As they may be used concomitantly with many other drugs, we review the potential drug-drug interactions (DDIs) regarding the three leaders in the class (dapagliglozin, canagliflozin and empagliflozin). Most of the available studies were performed in healthy volunteers and have assessed the pharmacokinetic interferences with a single administration of the SGLT2 inhibitor. The exposure [assessed by peak plasma concentrations (Cmax) and area under the concentration-time curve (AUC)] to each SGLT2 inhibitor tested was not significantly influenced by the concomitant administration of other glucose-lowering agents or cardiovascular agents commonly used in patients with type 2 diabetes. Reciprocally, these medications did not influence the pharmacokinetic parameters of dapagliflozin, canagliflozin or empagliflozin. Some modest changes were not considered as clinically relevant. However, drugs that could specifically interfere with the metabolic pathways of SGLT2 inhibitors [rifampicin, inhibitors or inducers of uridine diphosphate-glucuronosyltransferase (UGT)] may result in significant changes in the exposure of SGLT2 inhibitors, as shown for dapagliflozin and canagliflozin. Potential DDIs in patients with type 2 diabetes receiving chronic treatment with an SGLT2 inhibitor deserve further attention, especially in individuals treated with several medications or in more fragile patients with hepatic and/or renal impairment.
Antidoteand Emergency Treatment :/SRP:/ Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR if necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on the left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Poisons A and B/
Human Toxicity Excerpts :/OTHER TOXICITY INFORMATION/ Renal hyperfiltration has been used as a surrogate marker for increased intraglomerular pressure in patients with diabetes mellitus. Previous human investigation examining the pathogenesis of hyperfiltration has focused on the role of neurohormones such as the renin-angiotensin-aldosterone system (RAAS). Unfortunately, RAAS blockade does not completely attenuate hyperfiltration or diabetic kidney injury. More recent work has therefore investigated the contribution of renal tubular factors, including the sodium-glucose cotransporter, to the hyperfiltration state, which is the topic of this review. Novel sodium-glucose cotransporter-2 (SGLT2) inhibitors reduce proximal tubular sodium reabsorption, thereby increasing distal sodium delivery to the macula densa, causing tubuloglomerular feedback, afferent vasoconstriction and decreased hyperfiltration in animals. In humans, SGLT2 inhibition was recently shown to reduce hyperfiltration in normotensive, normoalbuminuric patients with type 1 diabetes. In clinical trials of type 2 diabetes, SGLT2 is associated with significant renal effects, including modest, acute declines in estimated glomerular filtration rate followed by the maintenance of stable renal function, and reduced albuminuria.
Non Human Toxicity Excerpts :/LABORATORY ANIMALS: Chronic Exposure or Carcinogenicity/ Canagliflozin is an SGLT2 inhibitor used for the treatment of type 2 diabetes mellitus. Studies were conducted to investigate the mechanism responsible for renal tubular tumors and pheochromocytomas observed at the high dose in a 2-year carcinogenicity study in rats. At the high dose (100 mg/kg) in rats, canagliflozin caused carbohydrate malabsorption evidenced by inhibition of intestinal glucose uptake, decreased intestinal pH and increased urinary calcium excretion. In a 6-month mechanistic study utilization of a glucose-free diet prevented carbohydrate malabsorption and its sequelae, including increased calcium absorption and urinary calcium excretion, and hyperostosis. Cell proliferation in the kidney and adrenal medulla was increased in rats maintained on standard diet and administered canagliflozin (100 mg/kg), and in addition an increase in the renal injury biomarker KIM-1 was observed. Increased cell proliferation is considered as a proximal event in carcinogenesis. Effects on cell proliferation, KIM-1 and calcium excretion were inhibited in rats maintained on the glucose-free diet, indicating they are secondary to carbohydrate malabsorption and are not direct effects of canagliflozin.
Protein Binding :Canagliflozin is mainly bound to albumin. The plasma protein binding of this drug is 99%.
Exact Mass :444.14067323
InChI :InChI=1S/C24H25FO5S/c1-13-2-3-15(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/h2-10,19,21-24,26-29H,11-12H2,1H3/t19-,21-,22+,23-,24+/m1/s1
InchIKey :XTNGUQKDFGDXSJ-ZXGKGEBGSA-N
Canonical SMILES :CC1=C(C=C(C=C1)C2C(C(C(C(O2)CO)O)O)O)CC3=CC=C(S3)C4=CC=C(C=C4)F
Isomeric SMILES :CC1=C(C=C(C=C1)[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CO)O)O)O)CC3=CC=C(S3)C4=CC=C(C=C4)F
Product Description :Canagliflozin is 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. It has a role as a hypoglycemic agent and a sodium-glucose transport protein subtype 2 inhibitor. It is a C-glycosyl compound, a member of thiophenes and an organofluorine compound.
Custom Duty : Applicable
Port of Loading : Canada
Expected Dispatch : 15-Aug-2022
Taxes : Not Applicable
Refund Policy : 30-days money back
Custom Duty : Applicable
Port of Loading : Canada
Expected Dispatch : 15-Aug-2022
Taxes : Not Applicable
Refund Policy : 30-days money back


More information about Canagliflozin


Canagliflozin, sold under the brand name Invokana among others, is a medication used to treat type 2 diabetes. It is a third-line medication to be tried after metformin, a first-line medication for type 2 diabetes. It is used together with exercise and diet. It is not recommended in type 1 diabetes. It is taken by mouth.

Common side effects include vaginal yeast infections, nausea, constipation, and urinary tract infections. Serious side effects may include low blood sugar, Fournier's gangrene, leg amputation, kidney problems, high blood potassium, and low blood pressure. Diabetic ketoacidosis may occur despite nearly normal blood sugar levels. Use in pregnancy and breastfeeding is not recommended. Canagliflozin is a sodium-glucose cotransporter-2 (SGLT2) inhibitor. It works by increasing the amount of glucose lost in the urine.

Canagliflozin was approved for medical use in the United States, in the European Union, and in Australia in 2013. It is on the World Health Organization's List of Essential Medicines. In 2018, it was the 191st most commonly prescribed medication in the United States, with more than 3\u00a0million prescriptions.





This page contains information about Canagliflozin , Canagliflozin cas, Canagliflozin synthesis, Canagliflozin suppliers

What is Canagliflozin ?
Canagliflozin falls under API Standards of Canagliflozin.Canagliflozin belongs to a new class of anti-diabetic drugs that works by inhibiting the sodium-glucose transport protein (SGLT2). This transport protein is found in the kidney and is responsible for reabsorbing glucose that has been filtered.
What is the CAS Number of Canagliflozin?
The CAS Number of Canagliflozin is 842133-18-0
Who are the suppliers of Canagliflozin?
CLEARSYNTH is a worldwide supplier of Canagliflozin

Related compounds of Canagliflozin

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