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首页 / 抑制剂/激动剂 / 膜转运蛋白 / SGLT / Canagliflozin/卡格列净

Canagliflozin/卡格列净 {[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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Type HazMat fee for 500 gram (Estimated)
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Canagliflozin/卡格列净 化学结构 CAS号：842133-18-0
Canagliflozin/卡格列净 化学结构
CAS号：842133-18-0
Canagliflozin/卡格列净 3D分子结构
CAS号：842133-18-0
Canagliflozin/卡格列净 化学结构 CAS号：842133-18-0
Canagliflozin/卡格列净 3D分子结构 CAS号：842133-18-0
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Canagliflozin/卡格列净 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:

全球学术期刊中引用的产品

• Adv. Funct. Mater., 2025, 2500696. Ambeed. [ A245395 ]
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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/卡格列净 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/卡格列净 细胞研究

细胞系 浓度 检测类型 检测时间 活性说明 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/卡格列净 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/卡格列净 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/卡格列净 技术信息

CAS号842133-18-0
分子式C24H25FO5S
分子量 444.52
SMILES Code FC1=CC=C(C2=CC=C(CC3=C(C=CC([C@@H]4O[C@@H]([C@H]([C@@H]([C@H]4O)O)O)CO)=C3)C)S2)C=C1
MDL No. MFCD18251436
别名 JNJ 28431754; TA-7284; JNJ-24831754
运输蓝冰
InChI Key XTNGUQKDFGDXSJ-ZXGKGEBGSA-N
Pubchem ID 24812758
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案一
方案二
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/卡格列净 纯度/质量文件 | Canagliflozin/卡格列净 亚型比较 | Canagliflozin/卡格列净 生物活性 | Canagliflozin/卡格列净 细胞研究 | Canagliflozin/卡格列净 临床数据 | Canagliflozin/卡格列净 实验方案 | Canagliflozin/卡格列净 技术信息

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