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Canagliflozin

Catalog No.
A8333
SGLT2 inhibitor,potent and selective
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$66.00
In stock
10mg
$58.00
In stock
50mg
$75.00
In stock
100mg
$96.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Canagliflozin is a novel, potent, and highly selective sodium glucose co-transporter (SGLT) 2 inhibitor [1]. It has been proved that Canagliflozin can increase urine glucose excretion by reducing the renal glucose threshold and by decreasing the filtered glucose re-absorption [2].

Canagliflozin has been shown to inhibit the Na+-mediated 14C-AMG intakes in CHO-hSGLT2, CHO-rat SGLT2 and CHO-mouse SGLT2?with IC50 values of 4.4, 3.7 and 2.0 nM, respectively [1].

Canagliflozin has been reported to reduce the blood glucose (BG) levels dose-dependently in both db/db Mice and Zucker diabetic fatty (ZDF) Rats. Additionally, canagliflozin has proved to decrease the respiratory exchange ratio, and body weight in DIO mice and ZDF rats [1].

Canagliflozin can be taken orally [1].

References:
[1] Liang Y1,?Arakawa K,?Ueta K,?Matsushita Y,?Kuriyama C?Martin T,?Du F,?Liu Y,?Xu J,?Conway B,?Conway J,?Polidori D,?Ways K,?Demarest K. Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models. PLoS One.?2012;7(2):e30555
[2] Sarnoski-Brocavich S,?Hilas O. Canagliflozin (Invokana), a Novel Oral Agent For Type-2 Diabetes. P T.?2013 Nov;38(11):656-66

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt444.52
Cas No.842133-18-0
FormulaC24H25FO5S
SynonymsJNJ 24831754ZAE; JNJ 28431754; JNJ 28431754AAA; TA 7284
Solubility≥22.25 mg/mL in DMSO; insoluble in H2O; ≥49.5 mg/mL in EtOH
Chemical Name(2S,3R,4R,5S,6R)-2-[3-[[5-(4-fluorophenyl)thiophen-2-yl]methyl]-4-methylphenyl]-6-(hydroxymethyl)oxane-3,4,5-triol
SDFDownload SDF
Canonical SMILESCC1=C(C=C(C=C1)C2C(C(C(C(O2)CO)O)O)O)CC3=CC=C(S3)C4=CC=C(C=C4)F
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment:[1]

Cell lines

Rat skeletal muscle cell line L6

Reaction Conditions

10 μM canagliflozin for 15 min incubation

Applications

At 10 μM, canagliflozin inhibited the facilitative (non-Na+-linked) glucose transporter-mediated 2-deoxy-glucose uptake in L6 myoblasts by less than 50%.
Animal experiment:[1]

Animal models

Male C57BL/ksj-db/db hyperglycemic mice

Dosage form

0.1, 1 and 10 mg/kg

Administrated via oral gavage

Applications

In db/db mice, single doses of canagliflozin dose-dependently reduced non-fasting blood glucose (BG) concentrations. The onset of the BG-lowering effect after a single dose was rapid, and BG levels in canagliflozin-treated mice (at 1 and 10 mg/kg doses) were significantly different from those of vehicle-treated mice at 1 hour after treatment. This antihyperglycemic effect reached its peak at 6 hours.

Note

The technical data provided above is for reference only.

References:

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

Biological Activity

Targets hSGLT2 rSGLT2 mSGLT2      
IC50 4.4 nM 3.7 nM 2 nM      

Quality Control