Canagliflozin hemihydrate

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CAS NO:

928672-86-0

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	电议
10mg	电议
50mg	电议
100mg	电议
500mg	电议

产品介绍

Canagliflozin hemihydrate (JNJ28431754 hemihydrate; TA-7284 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 No.	928672-86-0
别名	卡格列净半水合物,JNJ 28431754 hemihydrate
Canonical SMILES	CC1=CC=C([C@H]2[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O2)C=C1CC3=CC=C(C4=CC=C(F)C=C4)S3.[0.5H2O]
分子式	C₂₄H₂₆FO₅.₅S
分子量	453.52
溶解度	DMSO: ≥ 100 mg/mL (220.50 mM)
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	Canagliflozin hemihydrate (JNJ28431754 hemihydrate; TA-7284 hemihydrate) is a selective SGLT2 inhibitor with IC50s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively[1]. IC50: 2/3.7/4.4 nM (mSGLT2/rSGLT2/hSGLT2, in CHOK cells)[1] 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]. 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]. Animal Model: Diet-induced obese, insulin resistantmice (DIO) Mice[1] [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.