Tofogliflozin hydrate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Tofogliflozin (CSG-452) 是一种有效的、高选择性的 SGLT2 抑制剂，对人、大鼠和小鼠 SGLT2 的 Ki 值分别为 2.9、14.9 和 6.4 nM。

Tofogliflozin (CSG-452) is a potent, highly selective SGLT2 inhibitor with Ki of 2.9, 14.9, and 6.4 nM against human, rat, and mouse SGLT2, respectively; displays high selectivity over human SGLT2 versus human SGLT1, SGLT6, and sodium/myo-inositol transporter 1; increases renal glucose clearance and lowered the blood glucose level in Zucker diabetic fatty rats, also improves postprandial glucose excursion; reduces glycated hemoglobin and improved glucose tolerance in the oral glucose tolerance test in vivo.Diabetes Approved(In Vitro):Tofofloxacin (3-30 nM; 24 hours; tubular epithelial cells) treatment inhibits the oxidative stress generation and monocyte chemoattractant protein-1 (MCP-1) gene expression in tubular cells induced by high glucose.Tofofloxacin (3-30 nM; 8 days; tubular epithelial cells) treatment inhibits the apoptotic cell death induced by high glucose.(In Vivo):Tofogliflozin (0.1-10 mg/kg; oral administration; once daily; for 4 weeks;?db/db?mice) treatment improves hyperglycemia and thereby ameliorated glucose intolerance of the obese diabetic mice.

Tofofloxacin (3-30 nM; 24 hours; tubular epithelial cells) treatment inhibits the oxidative stress generation and monocyte chemoattractant protein-1 (MCP-1) gene expression in tubular cells induced by high glucose.Tofofloxacin (3-30 nM; 8 days; tubular epithelial cells) treatment inhibits the apoptotic cell death induced by high glucose. RT-PCR Cell Line:Tubular epithelial cells Concentration:3 nM and 30 nM Incubation Time:24 hours Result:Inhibited MCP-1 gene expression in tubular cells induced by high glucose exposure.Apoptosis Analysis Cell Line:Tubular epithelial cells Concentration:3 nM and 30 nM Incubation Time:8 days Result:Inhibited the apoptotic cell death induced by high glucose.

Tofogliflozin (0.1-10 mg/kg; oral administration; once daily; for 4 weeks; db/db mice) treatment improves hyperglycemia and thereby ameliorated glucose intolerance of the obese diabetic mice. Animal Model:db/db miceDosage:0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, or 10 mg/kg Administration:Oral administration; once daily; for 4 weeks Result:Observed acute blood glucose reduction, dose-dependently reduced glycated hemoglobin, significantly prevented the decrease of IRI levels at doses of 3 and 10 mg/kg, and no difference in food intake or body weight.

CSG452 hydrate | CSG-452 hydrate

GPCR/G Protein

SGLT

SGLT

Metabolic Disease

Diabetes

1201913-82-7

404.5

C22H28O7

>98% (HPLC)

10 mM in DMSO

CCC1=CC=C(C=C1)CC2=CC3=C(COC34C(C(C(C(O4)CO)O)O)O)C=C2.O

Spiro[isobenzofuran-1(3H),2'-[2H]pyran]-3',4',5'-triol, 6-[(4-ethylphenyl)methyl]-3',4',5',6'-tetrahydro-6'-(hydroxymethyl)-, hydrate (1:1), (1S,3'R,4'S,5'S,6'R)-

(-20℃)

With Ice Pack

≥ 2 years