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Canagliflozin hemihydrate

Canagliflozin hemihydrate (TA 7284) (JNJ28431754 hemihydrate) 是一种选择性的 SGLT2 抑制剂，作用于表达 mSGLT2，rSGLT2 和 hSGLT2 的 CHO 细胞，IC50 分别为 2 nM，3.7 nM 和 4.4 nM。

CAS号

928672-86-0

分子式

C48H52F2O11S2

主要靶点

SGLT

仅限科研使用

Cat No : CM06427

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Synonyms

JNJ-28431754|TA-7284|JNJ 28431754|JNJ28431754|TA7284|TA 7284

验证数据展示

  • CAS No.: 928672-86-0

    Canagliflozin hemihydrate
    CAS#: 928672-86-0

产品信息

Canagliflozin hemihydrate is a drug of the gliflozin class or subtype 2 sodium-glucose transport inhibitors used for the treatment of type 2 diabetes. SGLT2 is responsible for at least 90% of renal glucose reabsorption (SGLT1 being responsible for the remaining 10%). Blocking this transporter causes up to 119 grams of blood glucose per day to be eliminated through the urine, corresponding to 476 kilocalories.

CAS号 928672-86-0
分子式 C48H52F2O11S2
主要靶点 SGLT
主要通路 G蛋白偶联受体
分子量 907.05
纯度 99.96%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 JNJ-28431754|TA-7284|JNJ 28431754|JNJ28431754|TA7284|TA 7284

靶点活性

mSGLT2/rSGLT2/hSGLT2, in CHOK cells:2/3.7/4.4 nM (IC50)

体内活性

Canagliflozin (30 mg/kg treatment for 4 weeks) reduced blood glucose (BG) levels, respiratory exchange ratio, and body weight gain in DIO mice[1]. Canagliflozin (3 mg/kg for 3 weeks) increases urinary glucose excretion (UGE) with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight In ZF rats[1].

体外活性

Canagliflozin inhibits Na+-dependent 14C-AMG uptake in CHO-hSGLT2 cells, with an IC50 of 4.4±1.2 nM. Similar IC50 values are obtained in CHO-rSGLT2 and CHO-mSGLT2 cells (IC50 = 3.7 and 2.0 nM for rat and mouse SGLT2, respectively). Canagliflozin inhibits 14C-AMG uptake in CHO-hSGLT1 and mSGLT1 cells with IC50 of 684±159 nM and >1,000 nM, respectively[1].

溶解度

DMSO:90mg/mL (198.4mM)

参考文献

1.Liang Y, 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.
2.Davidson JA, Sloan L. Fixed-Dose Combination of Canagliflozin and Metformin for the Treatment of Type 2 Diabetes: An Overview. Adv Ther. 2016 Nov 16.
3.Qiu R, et al. Canagliflozin: Efficacy and Safety in Combination with Metformin Alone or with Other Antihyperglycemic Agents in Type 2 Diabetes. Diabetes Ther. 2016 Oct 12.
4.Canagliflozin (Invokana) for Type 2 Diabetes Mellitus [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2015 Sep. Available from http://www.ncbi.nlm.nih.gov/books/NBK349575/ PubMed PMID: 26962611.
5.Kaur K, et al. Efficacy and safety of canagliflozin among patients with type 2 diabetes mellitus: A systematic review and meta-analysis. Indian J Endocrinol Metab. 2015 Nov-Dec;19(6):705-21.

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