Canagliflozin
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
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 444.52 |
| Cas No. | 842133-18-0 |
| Formula | C24H25FO5S |
| Synonyms | JNJ 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 |
| SDF | Download SDF |
| 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 |
| Shipping Condition | Small 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. |
| Cell experiment:[1] | |
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Cell lines |
Rat skeletal muscle cell line L6 |
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Reaction Conditions |
10 μM canagliflozin for 15 min incubation |
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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] | |
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Animal models |
Male C57BL/ksj-db/db hyperglycemic mice |
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Dosage form |
0.1, 1 and 10 mg/kg Administrated via oral gavage |
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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. |
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Note |
The technical data provided above is for reference only. |
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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. |
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| Targets | hSGLT2 | rSGLT2 | mSGLT2 | |||
| IC50 | 4.4 nM | 3.7 nM | 2 nM |
Quality Control & MSDS
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Chemical structure
Related Biological Data
Related Biological Data
