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Home>>Signaling Pathways>> Metabolism>> SGLT>>Canagliflozin

Canagliflozin Sale

(Synonyms: 卡格列净; JNJ 28431754) 目录号 : GC13771

Canagliflozin是一种用于治疗2型糖尿病的钠葡萄糖共转运体（SGLT2）抑制剂。

Canagliflozin Chemical Structure

Cas No.:842133-18-0

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥385.00
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5mg
¥350.00
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10mg
¥525.00
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50mg
¥686.00
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100mg
¥875.00
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Description

Canagliflozin is a sodium glucose co-transporter (SGLT) 2 inhibitor in clinical development for the treatment of type 2 diabetes mellitus[1].

Canagliflozin demonstrates selective inhibition of SGLT2 in CHOK cells, with IC50 values of 2nM, 3.7nM, and 4.4nM for mSGLT2, rSGLT2, and hSGLT2, respectively[2]. Canagliflozin is a novel inhibitor of vascular smooth muscle cell proliferation and migration[3].

Canagliflozin (50μM; 24h) inhibits cell cycle progression and DNA synthesis in rat vascular smooth muscle cell[3]. Canagliflozin (5μg/ml; 24h) attenuates lipotoxicity in cardiomyocytes by inhibiting inflammation and ferroptosis through activating AMPK pathway in HL-1 cells[4]. Canagliflozin (50μM; 48h) significantly reduced SKBR3 cell proliferation in the presence of glucose (11mM; 48h)[5].

Canagliflozin (14.4mg/kg; oral adminstration; 23 months) significantly improved central Insulin (3U/kg; i.p. ; 15min) sensitivity in the hypothalamus and the hippocampus of 30-month-old male mice[6]. Canagliflozin (20mg/kg; i.p. ; 6 weeks) mitigates ferroptosis and improves myocardial oxidative stress in mice with diabetic cardiomyopathy[7].

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 [J]. PLoS One, 2012, 7(2): e30555.
[2] GUO Y Y, ZHANG J Y, SUN J F, et al. A comprehensive review of small-molecule drugs for the treatment of type 2 diabetes mellitus: Synthetic approaches and clinical applications [J]. Eur J Med Chem, 2024, 267(116185.
[3] BEHNAMMANESH G, DURANTE G L, KHANNA Y P, et al. Canagliflozin inhibits vascular smooth muscle cell proliferation and migration: Role of heme oxygenase-1 [J]. Redox Biol, 2020, 32(101527.3
[4] ZHANG W, LU J, WANG Y, et al. Canagliflozin Attenuates Lipotoxicity in Cardiomyocytes by Inhibiting Inflammation and Ferroptosis through Activating AMPK Pathway [J]. Int J Mol Sci, 2023, 24(1):
[5] PAPADOPOLI D, UCHENUNU O, PALIA R, et al. Perturbations of cancer cell metabolism by the antidiabetic drug canagliflozin [J]. Neoplasia, 2021, 23(4): 391-9.
[6] JAYARATHNE H S M, DEBARBA L K, JABORO J J, et al. Neuroprotective effects of Canagliflozin: Lessons from aged genetically diverse UM-HET3 mice [J]. Aging Cell, 2022, 21(7): e13653.
[7] DU S, SHI H, XIONG L, et al. Canagliflozin mitigates ferroptosis and improves myocardial oxidative stress in mice with diabetic cardiomyopathy [J]. Front Endocrinol (Lausanne), 2022, 13(1011669.

Canagliflozin是一种用于治疗2型糖尿病的钠葡萄糖共转运体（SGLT2）抑制剂[1]。Canagliflozin在CHOK细胞中表现出对SGLT2的选择性抑制，对mSGLT2、rSGLT2和hSGLT2的IC50值分别为2nM、3.7nM和4.4nM[2]。Canagliflozin是一种新型的血管平滑肌细胞增殖和迁移抑制剂[3]。

Canagliflozin（50μM; 24h）抑制大鼠血管平滑肌细胞的细胞周期进程和DNA合成[3]。Canagliflozin（5μg/ml; 24h）通过激活HL-1细胞中的AMPK通路，抑制炎症和铁死亡，从而减轻心肌细胞的脂肪毒性[4]。Canagliflozin（50μM; 48h）显著抑制葡萄糖（11mM; 48h）存在下SKBR3细胞的增殖[5]。

使用Canagliflozin（14.4mg/kg; oral adminstration; 23 months）处理腹腔给予胰岛素（3U/kg; i.p. ; 15min）的30月龄雄性小鼠，Canagliflozin显著改善小鼠下丘脑和海马的敏感性[6]。使用 Canagliflozin（20mg/kg; i.p. ; 6 weeks）处理糖尿病性心肌病小鼠，Canagliflozin减轻糖尿病性心肌病小鼠的铁死亡，改善心肌氧化应激[7]。

实验参考方法

Cell experiment [1]:

Cell lines

HL-1 cells

Preparation Method

Cells were cultured in high-glucose DMEM, supplemented with 10% fetal bovine serum and 1% penicillin-streptomycin antibiotic in an incubator of 5% CO2 at 37℃. For inducing a lipotoxic cardiomyocyte model, cells were seeded into cell culture dishes or plates at an appropriate density and stimulated with 0.1mM palmitic acid for 24h in the presence or absence of Canagliflozin (5μg/mL). Bovine serum albumin used to liquefy palmitic acid, was also added to blank control cells. COX-2 inhibitor celecoxib (5μg/mL), iNOS inhibitor SMT (10μM), and the ferroptosis inhibitor Fer-1 (5μM) were added simultaneously with palmitic acid. AMPK inhibitor Compound C (5μg/mL) was added with palmitic acid and Canagliflozin.

Reaction Conditions

5μg/ml; 24h

Applications

Canagliflozin attenuates lipotoxicity in cardiomyocytes by inhibiting inflammation and ferroptosis through activating AMPK pathway in HL-1 cells.
Animal experiment [2]:

Animal models

Male C57BL/6J mice

Preparation Method

Male C57BL/6J mice aged 6-8 weeks were kept under specific-pathogen-free (SPF) environment (room temperature 22±2°C, humidity 55±5%, 12h light/12h dark cycle), with unrestricted access to food and water.
Mice were allowed to acclimatize in the laboratory environment for 1 week before the beginning of the experiment.
Diabetic cardiomyopathy (DCM) model establishment: The mice were given a single intraperitoneal injection of 150mg/kg 1% streptozotocin (STZ, dissolved in 0.1 mol/L sodium citrate buffer, pH = 4.4-4.6). Mouse blood from the tail vein was collected in each group of the model mice and tested by glucose meter on day 3, 5 and 7 after injection. The mice with random blood glucose levels≥16.7mmol/L were considered as diabetic models, and then kept for 4 weeks to induce DCM.
DCM group: DCM model mice were treated with saline for 6 weeks; DCM + Cana group: DCM model mice were treated with 20mg/kg/d Canagliflozin for 6 weeks. On the last day, electrocardiogram examination was performed after the drug intervention, then all animals were weighted and sacrificed, heart tissues were removed freshly and aseptically for measurement.

Dosage form

20mg/kg; i.p. ; 6 weeks

Applications

Canagliflozin mitigates ferroptosis and improves myocardial oxidative stress in mice with diabetic cardiomyopathy.

References:
[1] ZHANG W, LU J, WANG Y, et al. Canagliflozin Attenuates Lipotoxicity in Cardiomyocytes by Inhibiting Inflammation and Ferroptosis through Activating AMPK Pathway [J]. Int J Mol Sci, 2023, 24(1):
[2] DU S, SHI H, XIONG L, et al. Canagliflozin mitigates ferroptosis and improves myocardial oxidative stress in mice with diabetic cardiomyopathy [J]. Front Endocrinol (Lausanne), 2022, 13(1011669.

化学性质

Cas No. 842133-18-0 SDF
别名 卡格列净; JNJ 28431754
化学名 (2S,3R,4R,5S,6R)-2-[3-[[5-(4-fluorophenyl)thiophen-2-yl]methyl]-4-methylphenyl]-6-(hydroxymethyl)oxane-3,4,5-triol
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
分子式 C24H25FO5S 分子量 444.52
溶解度 ≥ 22.25mg/mL in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.2496 mL 11.2481 mL 22.4962 mL
5 mM 0.4499 mL 2.2496 mL 4.4992 mL
10 mM 0.225 mL 1.1248 mL 2.2496 mL

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