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CAS No.: 928672-86-0

坎格列净半水合物 Catalog No. CSN16237

Synonyms: JNJ 28431754 hemihydrate;TA 7284 Hemihydrate;JNJ-28431754

Canagliflozin selectively inhibits SGLT2 with IC50 of 2.2 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 SGLT2

IC50:2.2nM
描述Sodium glucose co-transporter 2 (SGLT2) is a high-capacity glucose transporter mediating the majority of the glucose resorption in kidney. Canagliflozin hemihydrate is a selective, potent SGLT2 inhibitor with IC₅₀ values of 4.4, 3.7, and 2.0 nM for human SGLT2, rat SGLT2, and mouse SGLT2, respectively. In contrast, canagliflozin hemihydrate inhibited human, rat and mouse SGLT1 with IC₅₀ values of 684, 571, and >1000 nM, respectively. In L6 myoblasts, canagliflozin hemihydrate at 10 μM blocked the non-Na⁺-linked GLUT-mediated 3H-2-DG uptake by < 50%. Canagliflozin hemihydrate at 10 μM inhibited DNJ-induced currents by 23.4% in SGLT3-injected oocytes, whereas the same treatment of canagliflozin hemihydrate had no effect on currents in water-injected oocytes. In Zucker diabetic fatty (ZDF) rats treated by 1 mg/kg canagliflozin hemihydrate, renal threshold for glucose excretion was reduced from 415 mg/dl to 94 mg/dl at 90 min post treatment. In db/db mice, single dose of canagliflozin hemihydrate (1 and 10 mg/kg) rapidly downregulated non-fasting blood glucose concentration in a dose-dependent manner at 1h post treatment. When ZDF rats were treated with canagliflozin hemihydrate at different doses (3, 10, or 30 mg/kg) for 4 weeks, the non-fasting blood glucose and the level of HbA1c were decreased in all canagliflozin hemihydrate-treated rats compared to control group. Decreased blood glucose level following an oral glucose tolerance test was also observed in canagliflozin hemihydrate-treated rats. Treatment of 30 mg/kg canagliflozin hemihydrate in DIO mice for 4 weeks decreased their blood glucose level, respiratory exchange ratio, and body weight gain compared to vehicle-treated mice^[1].
作用机制Canagliflozin hemihydrate is a potent, selective inhibitor of SGLT2 that downregulates the renal glucose resorptive capacity, induces urinary glucose excretion, improves glycemic control and beta-cell function in vivo^[1].

动物研究

剂量

Rat: 10 mg/kg - 30 mg/kg^[2] (p.o.); 3 mg/kg^[2] (i.v.)

给药途径

p..o., i.v.

动物药代数据

Animal	Rats^[2]
Dose	3 mg/kg (i.v.) 10 mg/kg (p.o.)
Administration	i.v. p.o.
F	85% (p.o.)
CL_tot	236 ml/h/kg (i.v.)
T_1/2	5.0 h (i.v.) 5.2 h (p.o.)
T_max	5.0 h (p.o.)
AUC_0-inf	12703 ng·h/ml (i.v.) 35980 ng·h/ml (p.o.)
C_max	2513 ng/ml (p.o.)
Vd_ss	1357 ml/kg (i.v.)

参考文献

[1] Liang Y, Arakawa K, 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] Nomura S, Sakamaki S, et al. Discovery of canagliflozin, a novel C-glucoside with thiophene ring, as sodium-dependent glucose cotransporter 2 inhibitor for the treatment of type 2 diabetes mellitus. J Med Chem. 2010 Sep 9;53(17):6355-60.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.1025 mL
- 5.5124 mL
- 11.0248 mL
- 5 mM
- 0.2205 mL
- 1.1025 mL
- 2.2050 mL
- 10 mM
- 0.1102 mL
- 0.5512 mL
- 1.1025 mL

技术信息

CAS号

928672-86-0

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C48H52F2O11S2

运输

蓝冰

分子量

907.05

别名

JNJ 28431754 hemihydrate;TA 7284 Hemihydrate;JNJ-28431754;TA-7284;JNJ-24831754-ZAE;JNJ-28431754-AAA;brand name: Invokana. Sulisent

溶解度

DMSO	99.0 mg/mL (109.1 mM)
Water	Insoluble
Ethanol	100.0 mg/mL (110.2 mM)

动物实验配方

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坎格列净半水合物 Catalog No. CSN16237

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