Canagliflozin

目录号:S2760 别名: TA 7284, JNJ 28431754

Canagliflozin Chemical Structure

Molecular Weight(MW): 444.52

Canagliflozin是一种高效的,选择性SGLT2抑制剂,作用于hSGLT2,无细胞试验中IC50为2.2 nM,比作用于hSGLT1选择性高413倍。

规格 价格 库存 购买数量  
In DMSO RMB 3948.03 现货
RMB 2211.13 现货
RMB 3016.78 现货
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客户使用Selleck该产品发表文献9篇:

客户使用该产品的5个实验数据:

  • Canagliflozin dose-dependently increases pAMPK and pACC in PC3 cells after 30 min

    Mol Metab, 2016, 5(10):1048-56. Canagliflozin purchased from Selleck.

    Serum lipid and fasting blood glucose levels in Cana- and control-groups after 5 weeks of canagliflozin/vehicle oral administration. Significant reduction in total cholesterol, triglyceride, LDL-cholesterol and fasting blood glucose levels was observed in Cana-group at the end of experimental procedure compared to baseline. Fasting glucose was the only significantly increased parameter observed in the control group at the end of intervention. Data are shown as mean ± SD (***P ≤ 0.001, **P ≤ 0.01)

    Cardiovasc Diabetol, 2018, 17(1):106. Canagliflozin purchased from Selleck.

  • Pretreatment of SGLT inhibitors significantly attenuates sodium nitroprusside (SNP)-induced vascular relaxation in pulmonary arteries. A: dose-response curves of SNP-induced relaxation in the presence or absence of phlorizin in pulmonary arteries (vehicle: 0.05% methanol, phlorizin: 100 µmol/l). Data are means ± SE; n = 4 mice/group. *P < 0.05 vs. vehicle. B: dose-response curves of SNP-induced relaxation in the presence or absence of canagliflozin in pulmonary arteries (vehicle: 0.1% DMSO, canagliflozin: 10 µmol/l). Data are means ± SE; n = 3 mice/group. *P < 0.05 vs. vehicle. C: dose-response curves of SNP-induced relaxation in the presence or absence of phlorizin in coronary arteries. Data are means ± SE; n = 5 mice/group. D: dose-response curves of SNP-induced relaxation in the presence or absence of canagliflozin in coronary arteries. Data are means ± SE; n = 3 mice/group.

    Am J Physiol Lung Cell Mol Physiol, 2015, 309(9):L1027-36. . Canagliflozin purchased from Selleck.

    Dixon plots for canagliflozin inhibition of the enzyme/substrate pairs: (A) UGT1A1/β-EST; (B) HLM/β-EST; (C) UGT1A9+BSA/4MU; (D) UGT1A9+BSA/PRO; and (E) HLM+BSA/PRO. Concentrations of canagliflozin and substrates are corrected for binding to the respective enzyme sources and BSA (0.5% w/v). Points are experimentally derived values (mean of duplicate estimates; < 5% variance), whereas lines are from fitting with eq. 1 (UGT1A9) or eq. 4 (UGT1A1).

    Drug Metab Dispos, 2015, 43(10):1468-76.. Canagliflozin purchased from Selleck.

  • Plasma concentration of anti-diabetic drugs (A) Canagliflozin in ZDF and SD rat after a single intravenous administration at 1 mg/kg. Data points represent mean ± S.D. (n = 4). *P < 0.05 and **P < 0.01 compared with concentration in SD rats.

    Drug Metab Dispos, 2016, 44(8):1184-92. Canagliflozin purchased from Selleck.

产品安全说明书

SGLT抑制剂选择性比较

生物活性

产品描述 Canagliflozin是一种高效的,选择性SGLT2抑制剂,作用于hSGLT2,无细胞试验中IC50为2.2 nM,比作用于hSGLT1选择性高413倍。
靶点
mSGLT2 [1]
(Cell-free assay)
rSGLT2 [1]
(Cell-free assay)
hSGLT2 [1]
(Cell-free assay)
2 nM 3.7 nM 4.4 nM
体外研究

Canagliflozin 是新型C-葡萄糖苷,具有噻吩环。Canagliflozin 抑制 Na+依赖性的14C-AMG 吸收,这种作用存在浓度依赖性。Canagliflozin作用于 CHO-hSGLT1 和mSGLT1 细胞,抑制 14C-AMG 吸收,IC50 分别为 0.7 μM 和 >1 μM。Canagliflozin作用于 L6成肌细胞,抑制 50%以下 (非-Na+-关联的) GLUT调节的2H-2-DG吸收。在50 µM DNJ存在时,Canagliflozin (10 µM) 或phlorizin (3 mM) 单独作用于注射空白对照的卵母细胞,不影响电流。DMSO 和 Canagliflozin 10 µM 作用于注射SGLT3-的卵母细胞,抑制DNJ诱导的电流,分别抑制 15.6% 和 23.4%。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO-K1 cells NX;PNo1lTnWwY4Tpc44h[XO|YYm= NXe1[5FsUW6qaXLpeIlwdiCxZjDoeY1idiCVR1zUNkBmgHC{ZYPz[YQhcW5iQ1jPMWsyKGOnbHzzJIJ6KFtzNFPdRW1IKHWydHHr[UBie3OjeTygTWM2OD14Lkegcm0> NWPjOFU4OjJ4NUKyOVU>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-β-catenin / β-catenin / Cyclin D1; 

PubMed: 31142735     


CANA treatment upregulated the expression of p-β-catenin and inhibited β-catenin/cyclin D1 signaling in a dose-dependent manner. The relative signal intensity was listed below each band, and the average changes of p-β-catenin in triplicated tests were shown on right.

pACC / ACC / p-AMPKα / AMPKα / p-S6K / S6K / p-S6 / S6 ; 

PubMed: 27689018     


Representative western blot of Canagliflozin treated PC3 cells. Canagliflozin (30 μM) increases pAMPK and pACC and reduces pS6k and pS6. 

31142735 27689018
体内研究 Canagliflozin 处理高脂肪饲料饲喂的KK(HF-KK)小鼠,具有显著的抗高血糖效果。Canagliflozin 按30 mg/kg剂量口服处理给药雄性SD大鼠,诱导葡萄糖外排,处理24小时,每 200 g 体重外排3,696 mg 糖。药代动力学研究显示Canagliflozin 口服处理药效更高。Canagliflozin 按3和 10 mg/kg剂量分别静脉注射和口服处理给药雄性SD 大鼠, 测定AUC0−inf, po, t1/2 和生物有效性分别为 35,980 ng·h/mL, 5.2 小时,和 85%。Canagliflozin口服处理,抑制肾小管中的SGLT2,很可能是因为持续抑制葡萄糖的重吸收。广泛的UGE可反映 Canagliflozin 在体内优秀的药代动力学特性,及对SGLT2的高效抑制。由于大部分过滤的葡糖糖在肾小管中被SGLT2 重吸收,所以新型化合物将是很有效的抗糖尿病试剂。Canagliflozin 按3 mg/kg 剂量单独口服处理高糖高脂肪饲料喂养的KK(HF-KK)小鼠,显著降低血糖水平,不影响食物吸收。处理6个小时,与对照组相比,血糖水平降低48%。相反, Canagliflozin作用于正常血糖小鼠,只轻微影响血糖水平。因此, Canagliflozin 在治疗T2DM时可控制高血糖,也降低低血糖风险。[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:[1]
- 合并
  • Cell lines: L6 细胞系
  • Concentrations: 0-10 μM
  • Incubation Time: 24 小时
  • Method: 使用从大鼠骨骼肌提取的细胞系L6,检测 Canagliflozin 作用于葡糖糖载体 1 (GLUT1)活性的效果。细胞培养在含5.6 mM葡萄糖,补充10% 胎牛血清的DMEM培养基中,按每孔3.0×105个细胞的密度接种到14孔板中,在含5% CO2的环境中37oC下培养24小时。使用Kreb's ringer 磷酸HEPES buffer (pH 7.4,150 mM NaCl,5 mM KCl,1.25 mM MgSO4,1.25 mM CaCl2, 2.9 mM Na2HPO4, 10 mM HEPES)漂洗2次细胞,然后与Canagliflozin 溶液(250 µL, 10 uM) 在室温下预温育5分钟。加入50 µL 4.5 mM 2-DG (作为GLUTs的底物)/3H-2-DG(0.625 µCi)开始反应,随便在室温下温育15分钟。 通过吸取温育混合物而使2-DG 吸收停止。使用冰冻PBS立刻冲洗细胞3次。使用0.3 N NaOH萃取样本,通过液体闪烁法测定放射性。
    (Only for Reference)
动物实验:[2]
- 合并
  • Animal Models: KK (HF-KK) 小鼠
  • Formulation: 0.2% CMC/0.2% Tween-80
  • Dosages: 10 mg/kg
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 88 mg/mL (197.96 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
0.5% CMC+0.25% Tween 80
18 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 444.52
化学式

C24H25FO5S

CAS号 842133-18-0
储存条件 粉状
溶于溶剂
别名 TA 7284, JNJ 28431754

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02912455 Terminated Drug: canagliflozin|Drug: Placebo (for canagliflozin) Diabetes Mellitus Type 2|Obesity The Cleveland Clinic|Janssen Scientific Affairs LLC January 5 2017 Phase 4
NCT02891954 Enrolling by invitation Drug: Canagliflozin Diabetes Mellitus Type 2 University of Maryland Baltimore|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) September 2016 Phase 1
NCT02737657 Completed -- Diabetes Mellitus Type 2 Janssen-Cilag International NV April 2016 --
NCT02857764 Completed -- Diabetes Mellitus Type 2 Janssen Research & Development LLC February 15 2016 --
NCT02688075 Completed Other: No Intervention Diabetes Mellitus Type 2 Janssen Inc. November 13 2015 --

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID