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卡格列净 /Canagliflozin {[allProObj[0].p_purity_real_show]}

货号：A335983 同义名： JNJ 28431754;TA-7284

Canagliflozin (JNJ 28431754)是一种选择性SGLT2抑制剂，其在CHOK细胞中对mSGLT2、rSGLT2和hSGLT2的IC50值分别为2 nM、3.7 nM和4.4 nM。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Canagliflozin 化学结构 CAS号：842133-18-0
Canagliflozin 化学结构
CAS号：842133-18-0
Canagliflozin 3D分子结构
CAS号：842133-18-0
Canagliflozin 化学结构 CAS号：842133-18-0
Canagliflozin 3D分子结构 CAS号：842133-18-0
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Canagliflozin 纯度/质量文件 产品仅供科研

货号：A335983 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 SGLT1 ↓ SGLT2 ↓ 其他靶点 纯度
Phloretin ✔ 98%
Canagliflozin +++

hSGLT2, IC50: 3.7 nM

mSGLT2, IC50: 2 nM

 		95%
Empagliflozin ++

SGLT2, IC50: 3.1 nM

 		98%
Dapagliflozin ++++

hSGLT2, EC50: 1.1 nM

 		97%
Tofogliflozin (hydrate) +++

hSGLT2, IC50: 2.9 nM

 		99%+
Sotagliflozin +

SGLT1, IC50: 36 nM

 		++++

SGLT2, IC50: 1.8 nM

 		98%
Ipragliflozin ++

hSGLT2, IC50: 7.4 nM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Canagliflozin 生物活性

靶点

  • SGLT2

    hSGLT2, IC50:3.7 nM

    mSGLT2, IC50:2 nM
描述 Sodium glucose co-transporter 2 (SGLT2) is a high-capacity glucose transporter mediating the majority of the glucose resorption in kidney. Canagliflozin is a selective, potent SGLT2 inhibitor with IC50 values of 4.4, 3.7, and 2.0 nM for human SGLT2, rat SGLT2, and mouse SGLT2, respectively. In contrast, canagliflozin inhibited human, rat and mouse SGLT1 with IC50 values of 684, 571, and >1000 nM, respectively. In L6 myoblasts, canagliflozin at 10 μM blocked the non-Na+-linked GLUT-mediated 3H-2-DG uptake by < 50%. Canagliflozin at 10 μM inhibited DNJ-induced currents by 23.4% in SGLT3-injected oocytes, whereas the same treatment of canagliflozin had no effect on currents in water-injected oocytes. In Zucker diabetic fatty (ZDF) rats treated by 1 mg/kg canagliflozin hemihydrate, renal threshold for glucose excretion was reduced from 415 mg/dl to 94 mg/dl at 90 min post treatment. In db/db mice, single dose of canagliflozin (1 and 10 mg/kg) rapidly downregulated non-fasting blood glucose concentration in a dose-dependent manner at 1h post treatment. When ZDF rats were treated with canagliflozin at different doses (3, 10, or 30 mg/kg) for 4 weeks, the non-fasting blood glucose and the level of HbA1c were decreased in all canagliflozin hemihydrate-treated rats compared to control group. Decreased blood glucose level following an oral glucose tolerance test was also observed in canagliflozin hemihydrate-treated rats. Treatment of 30 mg/kg canagliflozin in DIO mice for 4 weeks decreased their blood glucose level, respiratory exchange ratio, and body weight gain compared to vehicle-treated mice[2].

Canagliflozin 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
CHO-K1 cells Function assay Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay, IC50=6.7 nM 22652255

Canagliflozin 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02053116 Type 2 Diabetes Mellitus Phase 2 Terminated(On 25April2014, stu... 展开 >>dy was terminated before any dosing due to an AE of safety concern that occurred in protocol B1731003 with the same drug.) 收起 << - United States, Florida ... 展开 >> Pfizer Investigational Site DeLand, Florida, United States, 32720 收起 <<
NCT00650806 - Completed - -
NCT01273558 Diabetes Mellitus, Type 2 Phase 1 Completed - Germany ... 展开 >> Neuss, Germany 收起 <<

Canagliflozin 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.25mL

0.45mL

0.22mL

11.25mL

2.25mL

1.12mL

22.50mL

4.50mL

2.25mL

Canagliflozin 技术信息

CAS号842133-18-0
分子式C24H25FO5S
分子量 444.52
别名 JNJ 28431754;TA-7284;JNJ-24831754
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C
溶解度

DMSO: 50 mg/mL(112.48 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

0.5% CMC+0.25% Tween 80+water 18 mg/mL suspension

Tags: Canagliflozin | JNJ 28431754;TA-7284;JNJ-24831754 | SGLT | AmBeed-信号通路专用抑制剂 | Canagliflozin 纯度/质量文件 | Canagliflozin 亚型比较 | Canagliflozin 生物活性 | Canagliflozin 细胞研究 | Canagliflozin 临床数据 | Canagliflozin 实验方案 | Canagliflozin 技术信息

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