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Canagliflozin hemihydrate

Canagliflozin hemihydrate
Canagliflozin hemihydrate (TA 7284) is a drug of the gliflozin class or subtype 2 sodium-glucose transport 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.
Catalog No. T1782LCas No. 928672-86-0
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Purity:99.96%
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Canagliflozin hemihydrate

Catalog No. T1782LAlias TA-7284, TA7284, TA 7284, JNJ-28431754, JNJ28431754, JNJ 28431754Cas No. 928672-86-0

Canagliflozin hemihydrate (TA 7284) is a drug of the gliflozin class or subtype 2 sodium-glucose transport 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.
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Pack SizePriceAvailabilityQuantity
25 mg$497-10 days
1 mL x 10 mM (in DMSO)$43In Stock
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Product Introduction

Bioactivity
Description
Canagliflozin hemihydrate (TA 7284) is a drug of the gliflozin class or subtype 2 sodium-glucose transport 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.
Targets&IC50
mSGLT2/rSGLT2/hSGLT2 (CHOK cells):2/3.7/4.4 nM (IC50)
In vitro
Canagliflozin inhibits Na+-dependent 14C-AMG uptake in CHO-hSGLT2 cells, with an IC50 of 4.4±1.2 nM. Similar IC50 values are obtained in CHO-rSGLT2 and CHO-mSGLT2 cells (IC50 = 3.7 and 2.0 nM for rat and mouse SGLT2, respectively). Canagliflozin inhibits 14C-AMG uptake in CHO-hSGLT1 and mSGLT1 cells with IC50 of 684±159 nM and >1,000 nM, respectively[1].
In vivo
Canagliflozin (30 mg/kg treatment for 4 weeks) reduced blood glucose (BG) levels, respiratory exchange ratio, and body weight gain in DIO mice, while Canagliflozin (3 mg/kg for 3 weeks) increased urinary glucose excretion (UGE) without significant change in total food intake, resulting in decreased body weight in ZF rats[1].
AliasTA-7284, TA7284, TA 7284, JNJ-28431754, JNJ28431754, JNJ 28431754
Chemical Properties
Molecular Weight907.05
FormulaC48H52F2O11S2
Cas No.928672-86-0
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 90 mg/mL (198.4 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.1025 mL5.5124 mL11.0248 mL55.1238 mL
5 mM0.2205 mL1.1025 mL2.2050 mL11.0248 mL
10 mM0.1102 mL0.5512 mL1.1025 mL5.5124 mL
20 mM0.0551 mL0.2756 mL0.5512 mL2.7562 mL
50 mM0.0220 mL0.1102 mL0.2205 mL1.1025 mL
100 mM0.0110 mL0.0551 mL0.1102 mL0.5512 mL

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