| CAS NO: | 842133-18-0 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 100mg | 电议 |
| 500mg | 电议 |
| 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 |
| 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
Canagliflozin是一种新型的、有效的和高选择性的钠葡萄糖共转运蛋白（SGLT2）抑制剂[1]。研究表明，Canagliflozin可以通过减少肾糖阈值和减小过滤葡萄糖重吸收，增加尿葡萄糖排泄[2]。
在CHO-SGLT2、CHO-rat SGLT2和CHO-mouse SGLT2中，Canagliflozin抑制Na+介导的14C-AMG的摄入，IC50分别为4.4、3.7和2.0 nM[1]。
有研究表明，在db/db小鼠和Zucker糖尿病肥胖（ZDF）大鼠中，Canagliflozin剂量依赖性降低血糖（BG）水平。此外，在DIO小鼠和ZDF大鼠中，canagliflozin减少呼吸交换率和体重[1]。
Canagliflozin可以口服使用
参考文献：
[1] Liang Y1,Arakawa K,Ueta K,Matsushita Y,Kuriyama CMartin 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
| 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. | |
| Targets | hSGLT2 | rSGLT2 | mSGLT2 | |||
| IC50 | 4.4 nM | 3.7 nM | 2 nM |
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