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Canagliflozin hemihydrate

Cat. No. M8956
Canagliflozin hemihydrate Structure
Synonym:

JNJ-28431754; TA 7284

Size Price Availability Quantity
100mg USD 50  USD50 In stock
500mg USD 150  USD150 In stock
1g USD 220  USD220 In stock
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Quality Control & Documentation
Biological Activity

Canagliflozin hemihydrate is an inhibitor of subtype 2 sodium-glucose transport protein (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney. Canagliflozin hemihydrate inhibits hSGLT2 with IC50 of 2.2 nM, exhibits 413-fold selectivity over hSGLT1. Blocking SGLT2 causes up to 119 grams of blood glucose per day to be eliminated through the urine, corresponding to 476 kilocalories.

Chemical Information
Molecular Weight 453.52
Formula C24H25FO5S.1/2H2O
CAS Number 928672-86-0
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Nicolle LE, et al. Curr Med Res Opin. Effect of canagliflozin, a sodium glucose co-transporter 2 (SGLT2) inhibitor, on bacteriuria and urinary tract infection in subjects with type 2 diabetes enrolled in a 12-week, phase 2 study.

[2] Rosenstock J, et al. Diabetes Care. Dose-ranging effects of canagliflozin, a sodium-glucose cotransporter 2 inhibitor, as add-on to metformin in subjects with type 2 diabetes.

[3] Liang Y, et al. PLoS One. Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models.

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Tofogliflozin

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Mizagliflozin

Mizagliflozin (DSP-3235 free base) is a potent, orally active and selective SGLT1 inhibitor, with a Ki of 27 nM for human SGLT1. Mizagliflozin displays 303-fold selectivity over SGLT2. Mizagliflozin is used as an antidiabetic agent that can modify postprandial blood glucose excursion. Mizagliflozin also exhibits potential in the amelioration of chronic constipation.

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Keywords: Canagliflozin hemihydrate, JNJ-28431754; TA 7284 supplier, SGLT, inhibitors, activators


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