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Canagliflozin hemihydrate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Canagliflozin hemihydrate图片
CAS NO:928672-86-0
包装:100 mg
市场价:1243元

产品名称
JNJ-28431754
TA-7284
TA 7284
JNJ 28431754
JNJ28431754
TA7284
产品介绍
Canagliflozin hemihydrate (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。

产品描述

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.

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].

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].

Cas No.

928672-86-0

分子式

C48H52F2O11S2

分子量

907.05

别名

JNJ-28431754;TA-7284;TA 7284;JNJ 28431754;JNJ28431754;TA7284

储存和溶解度

DMSO:90mg/mL (198.4mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years