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编 号：F628472
分子式：C24H26FNO5
分子量：427.47
分子式：C24H26FNO5
分子量：427.47
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CAS No: 1003005-29-5
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生物活性：
TA-1887 (JNJ-39933673) is a highly potent, selective and orally active SGLT2 inhibitor (IC50: 1.4 nM) with antihyperglycemic effects. TA-1887 can be used in the research of diabetes.
体内研究：
TA-1887 (30 mg/kg, oral administration, rats) induces glucose excretion over a 24 h period of 2502 mg per 200 g body weight.TA-1887 (3 mg/kg, oral administration) reduces blood glucose levels without influencing food intake in hyperglycemic high-fat diet-fed KK (HF-KK) mice.TA-1887 (30?mg/kg/day, oral gavage for 2 weeks) significantly reduces GFR (glomerular filtration rate) in BSA-overloaded diabetic mice.TA-1887 (0.01% w/w in chow, HF diets fed mice) antagonizes diabetic cachexia and decreases mortality in diabetic mice.Animal Model:Sprague-Dawley rats
Dosage:30 mg/kg
Administration:Oral administration
Result:Induced extensive UGE (urinary glucose excretion) through continuous suppression of renal glucose reuptake.
Animal Model:BSA-overloaded diabetic mice
Dosage:30 mg/kg
Administration:Oral gavage for 2 weeks
Result:Suppressed the induction of TGF‐β2 level in vehicle‐treated BSA‐overloaded diabetic mice.Suppressed COL3 gene levels.
Animal Model:Male Sprague-Dawley rats (pharmacokinetic assay)
Dosage:3 mg/kg (i.v.), 10 mg/kg (p.o.)
Administration:Oral administration (p.o.), intravenous injection (i.v.)
Result:Pharmacokinetic (PK) parameters of TA-1887. Parametersdose (mg/kg) Cmax (ng/mL) t1/2 (h)F (%)
TA-18873(i.v.)3.9
TA-18873 10 (p.o.)27233.978
TA-1887 (JNJ-39933673) is a highly potent, selective and orally active SGLT2 inhibitor (IC50: 1.4 nM) with antihyperglycemic effects. TA-1887 can be used in the research of diabetes.
体内研究：
TA-1887 (30 mg/kg, oral administration, rats) induces glucose excretion over a 24 h period of 2502 mg per 200 g body weight.TA-1887 (3 mg/kg, oral administration) reduces blood glucose levels without influencing food intake in hyperglycemic high-fat diet-fed KK (HF-KK) mice.TA-1887 (30?mg/kg/day, oral gavage for 2 weeks) significantly reduces GFR (glomerular filtration rate) in BSA-overloaded diabetic mice.TA-1887 (0.01% w/w in chow, HF diets fed mice) antagonizes diabetic cachexia and decreases mortality in diabetic mice.Animal Model:Sprague-Dawley rats
Dosage:30 mg/kg
Administration:Oral administration
Result:Induced extensive UGE (urinary glucose excretion) through continuous suppression of renal glucose reuptake.
Animal Model:BSA-overloaded diabetic mice
Dosage:30 mg/kg
Administration:Oral gavage for 2 weeks
Result:Suppressed the induction of TGF‐β2 level in vehicle‐treated BSA‐overloaded diabetic mice.Suppressed COL3 gene levels.
Animal Model:Male Sprague-Dawley rats (pharmacokinetic assay)
Dosage:3 mg/kg (i.v.), 10 mg/kg (p.o.)
Administration:Oral administration (p.o.), intravenous injection (i.v.)
Result:Pharmacokinetic (PK) parameters of TA-1887. Parametersdose (mg/kg) Cmax (ng/mL) t1/2 (h)F (%)
TA-18873(i.v.)3.9
TA-18873 10 (p.o.)27233.978
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