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Canagliflozin hemihydrate

Cat. No. M8956
Canagliflozin hemihydrate Structure
Synonym:

JNJ-28431754; TA 7284

Size Price Availability Quantity
10mg USD 81  USD90 In stock
50mg USD 180  USD200 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 453.52
Formula C24H25FO5S.1/2H2O
CAS Number 928672-86-0
Purity >99%
Solubility DMSO
Storage at -20°C
References

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.
Nicolle LE, et al. Curr Med Res Opin. 2012 Jul;28(7):1167-71. PMID: 22548646.

Dose-ranging effects of canagliflozin, a sodium-glucose cotransporter 2 inhibitor, as add-on to metformin in subjects with type 2 diabetes.
Rosenstock J, et al. Diabetes Care. 2012 Jun;35(6):1232-8. PMID: 22492586.

Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models.
Liang Y, et al. PLoS One. 2012;7(2):e30555. PMID: 22355316.

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Luseogliflozin

Luseogliflozin is a SGLT2 inhibitor, it reduced reabsorption of renal filtered glucose and decreased renal glucose threshold (RTG) in urine to increase urinary glucose excretion.

LX2761

LX2761 is a locally acting SGLT1 and SGLT2 inhibitor in vitro with IC50 values of 2.2 nM and 2.7 nM for hSGLT1 and hSGLT2, respectively.

Dapagliflozin ((2S)-1,2-propanediol, hydrate)

Dapagliflozin(BMS512148) is a selective, orally active inhibitor of the renal sodium-glucose co-transporter type 2 (SGLT2) is in development for the treatment of type 2 diabetes mellitus (T2DM).

LX-4211

LX-4211 is an oral dual SGLT1/SGLT2 inhibitor with IC50 of 36 nM and 1.8 nM, respectively.

  Catalog
Abmole Inhibitor Catalog 2017




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

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