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Canagliflozin

坎格列净,卡格列净,TA-7284,TA 7284,JNJ 28431754,JNJ 24831754ZAE,TA7284,JNJ-28431754,

Canagliflozin是高活性hSGLT2选择性抑制剂，IC50为2.2 nM，比对hSGLT1的抑制性强413倍。

目录号
EY1779
EY1779
EY1779
EY1779
纯度
99.47%
99.47%
99.47%
99.47%
规格
5 mg
10 mg
50 mg
100 mg
原价
480
720
950
1190
售价
480
720
950
1190
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
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  • 生物活性

    Canagliflozin is a highly potent and selective SGLT2 inhibitor for hSGLT2 with IC50 of 2.2 nM in a cell-free assay, exhibits 413-fold selectivity over hSGLT1.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    0-10 μM

  • 动物实验

    10 mg/kg 口服处理

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Liang Y, et al. PLoS One. 2012, 7(2), e30555.
    [2] Alan J. Sinclair,et al. Efficacy and Safety of Canagliflozin in Individuals Aged 75 and Older with Type 2 Diabetes Mellitus: A Pooled Analysis. J Am Geriatr Soc. 2016 Mar; 64(3): 543–552. Published online 2016 Mar 21. doi: 10.1111/jgs.14028.
    [3] Nelson B. Watts,et al. Effects of Canagliflozin on Fracture Risk in Patients With Type 2 Diabetes Mellitus. J Clin Endocrinol Metab. 2016 Jan; 101(1): 157–166. Published online 2015 Nov 18. doi: 10.1210/jc.2015-3167.

    分子式
    C24H25FO5S    		 分子量
    444.52    		 CAS号
    842133-18-0    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    85 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT01157000 Healthy Drug: Canagliflozin Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Phase 1 2010-05-01 2014-04-07
    NCT02912455 Diabetes Mellitus, Type 2|Obesity Drug: canagliflozin|Drug: Placebo (for canagliflozin) The Cleveland Clinic|Janssen Scientific Affairs, LLC Phase 4 2017-01-05 2017-02-03
    NCT02673138 Type 1 Diabetes Drug: canagliflozin|Other: basal interruption without canagliflozin Yale University|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) 2016-01-01 2016-08-23
    NCT01186588 Healthy|Hepatic Insufficiency Drug: Canagliflozin Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Phase 1 2010-08-01 2013-05-27
    NCT01877889 Healthy Drug: Canagliflozin|Drug: Dapagliflozin Janssen-Cilag International NV Phase 1 2013-07-01 2014-03-25
    NCT01718652 Healthy Drug: Canagliflozin (JNJ-28431754)|Drug: Cyclosporine Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Phase 1 2011-02-01 2012-11-22
    NCT02891954 Diabetes Mellitus, Type 2 Drug: Canagliflozin University of Maryland|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) Phase 1 2016-09-01 2016-09-01
    NCT02000700 Diabetes Mellitus, Type 2 Drug: Canagliflozin 100 mg|Drug: Canagliflozin 50 mg|Drug: Canagliflozin 300 mg|Drug: Placebo Janssen Research & Development, LLC Phase 1 2014-03-01 2017-03-01
    NCT01428284 Healthy Drug: Canagliflozin/Probenecid Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Phase 1 2011-08-01 2012-02-16
    NCT02624908 Diabetes Mellitus, Type 2 Drug: canagliflozin|Drug: placebo Atlanta Research and Education Foundation|Janssen Scientific Affairs, LLC Phase 4 2016-04-01 2016-07-11
    NCT01343290 Healthy Drug: Canagliflozin Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Phase 1 2011-04-01 2012-09-29
    NCT02324842 Type 2 Diabetes Mellitus Drug: Canagliflozin|Drug: Liraglutide Ralph DeFronzo|Janssen Scientific Affairs, LLC|The University of Texas Health Science Center at San Antonio 2014-11-01 2017-03-13
    NCT01340677 Healthy Drug: Canagliflozin, 50 mg|Drug: Canagliflozin, 300 mg|Drug: Canagliflozin, 100 mg Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Phase 1 2011-05-01 2012-08-16
    NCT01273571 Healthy Drug: Canagliflozin/Metformin Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Phase 1 2010-12-01 2013-07-26
    NCT01395927 Healthy Drug: Rifampin|Drug: Canagliflozin Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Phase 1 2011-07-01 2013-05-03
    NCT02354235 Type 2 Diabetes Mellitus Drug: Teneligliptin|Drug: Canagliflozin|Drug: Placebo Mitsubishi Tanabe Pharma Corporation Phase 3 2015-01-01 2016-08-05
    NCT01707316 Healthy Drug: Treatment A: Canagliflozin 100 mg|Drug: Treatment B: Canagliflozin 300 mg|Other: Treatment C: Placebo Janssen Research & Development, LLC Phase 1 2012-06-01 2013-02-18
    NCT02597309 Diabetes, Obesity Drug: Canagliflozin Joslin Diabetes Center Phase 4 2015-11-01 2017-02-28
    NCT02243202 Obesity Drug: Canagliflozin|Drug: Phentermine|Drug: Matching Placebo to Canagliflozin|Drug: Matching Placebo to Phentermine Janssen Research & Development, LLC Phase 2 2014-09-01 2016-08-10
    NCT02139943 Diabetes Mellitus, Type 1 Drug: Canagliflozin 100 mg|Drug: Canagliflozin 300 mg|Drug: Placebo Janssen Research & Development, LLC Phase 2 2014-05-01 2016-06-07

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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