产品
编 号：F488821
分子式：C17H24F2N6O
分子量：366.41
分子式：C17H24F2N6O
分子量：366.41
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是否有货
1mg
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询价
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CAS No: 869490-23-3
产品详情
生物活性：
Gosogliptin is a potent and selective inhibitor of dipeptidyl peptidase-IV (DPP-IV).
体内研究：
The objectives of the present study are to characterize the metabolism, pharmacokinetics, and excretion of [14C] Gosogliptin in Sprague-Dawley (SD) rats, beagle dogs, and humans. A single dose of [14C] Gosogliptin is administered orally to intact SD rats (5 mg/kg), beagle dogs (5 mg/kg), and humans (20 mg). After a single oral dose of [14C] Gosogliptin to SD rats, an overall mean of 97.1% of the administered radioactivity is recovered in the urine, feces, and cage wash over a period of 168 h postdose. The mean cumulative dose recovered in feces is 66.0%. The mean cumulative excretion in the urine is 30.8%. Approximately 95% of the excreted radioactivity recovery occurred in the first 48 h. Mean total recoveries of dosed radioactivity from bile duct-cannulated rats are 29.5% in urine and 62.0% in bile. No gender-related differences are observed in the excretion pattern of radioactivity.
体外研究：
Gosogliptin (PF-00734200) is a potent, orally active, selective, and competitive inhibitor of DPP-IV, the enzyme mainly responsible for the degradation of the incretin peptides GLP-1 and glucose-dependent insulinotropic polypeptide. Gosogliptin demonstrates greater than 200-fold selectivity over other members of the DPP family (DPP-2, DPP-3, DPP-8, and DPP-9) and the related serine proteases, fibroblast activation protein, aminopeptidase P, and propyl oligopeptidase, enzymes that possess similar catalytic activities. Gosogliptin demonstrates rapid and reversible inhibition of plasma DPP-4 activity when administered orally to rats, dogs, and monkeys. In various nonclinical models, Gosogliptin stimulates insulin secretion and improves glucose tolerance.
Gosogliptin is a potent and selective inhibitor of dipeptidyl peptidase-IV (DPP-IV).
体内研究：
The objectives of the present study are to characterize the metabolism, pharmacokinetics, and excretion of [14C] Gosogliptin in Sprague-Dawley (SD) rats, beagle dogs, and humans. A single dose of [14C] Gosogliptin is administered orally to intact SD rats (5 mg/kg), beagle dogs (5 mg/kg), and humans (20 mg). After a single oral dose of [14C] Gosogliptin to SD rats, an overall mean of 97.1% of the administered radioactivity is recovered in the urine, feces, and cage wash over a period of 168 h postdose. The mean cumulative dose recovered in feces is 66.0%. The mean cumulative excretion in the urine is 30.8%. Approximately 95% of the excreted radioactivity recovery occurred in the first 48 h. Mean total recoveries of dosed radioactivity from bile duct-cannulated rats are 29.5% in urine and 62.0% in bile. No gender-related differences are observed in the excretion pattern of radioactivity.
体外研究：
Gosogliptin (PF-00734200) is a potent, orally active, selective, and competitive inhibitor of DPP-IV, the enzyme mainly responsible for the degradation of the incretin peptides GLP-1 and glucose-dependent insulinotropic polypeptide. Gosogliptin demonstrates greater than 200-fold selectivity over other members of the DPP family (DPP-2, DPP-3, DPP-8, and DPP-9) and the related serine proteases, fibroblast activation protein, aminopeptidase P, and propyl oligopeptidase, enzymes that possess similar catalytic activities. Gosogliptin demonstrates rapid and reversible inhibition of plasma DPP-4 activity when administered orally to rats, dogs, and monkeys. In various nonclinical models, Gosogliptin stimulates insulin secretion and improves glucose tolerance.
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