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Gosogliptin

Catalog No. T11450 CAS 869490-23-3

Synonyms: PF-00734200, PF-734200

Gosogliptin is a potent and selective dipeptidyl peptidase-IV (DPP-IV) inhibitor.

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Gosogliptin, CAS 869490-23-3

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,520.00
50 mg	6-8 weeks	$ 1,980.00
100 mg	6-8 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

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Description	Gosogliptin is a potent and selective dipeptidyl peptidase-IV (DPP-IV) inhibitor.
In vitro	Gosogliptin is a potent, orally active inhibitor of DPP-IV, displaying over 200-fold selectivity against other DPP family members (DPP-2, DPP-3, DPP-8, and DPP-9) and related serine proteases, such as fibroblast activation protein, aminopeptidase P, and propyl oligopeptidase. This compound effectively inhibits plasma DPP-4 activity in a rapid and reversible manner following oral administration to rats, dogs, and monkeys. Gosogliptin enhances insulin secretion and glucose tolerance in various nonclinical models. Its mechanism involves competitive and selective inhibition of DPP-IV, key for degrading incretin peptides GLP-1 and glucose-dependent insulinotropic polypeptide, thereby influencing glucose homeostasis.
In vivo	The objectives of the present study are to characterize the metabolism, pharmacokinetics, and excretion of Gosogliptin in Sprague-Dawley ?rats, beagle dogs, and humans.?A single dose of ?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 ?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.

Synonyms	PF-00734200, PF-734200
Molecular Weight	366.41
Formula	C17H24F2N6O
CAS No.	869490-23-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Dai H, et al. The pharmacokinetics of PF-734200, a DPP-IV inhibitor, in subjects with renal insufficiency. Br J Clin Pharmacol. 2011 Jul;72(1):85-91. 2. Sharma R, et al. Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human. Drug Metab Dispos. 2012 Nov;40(11):2143-61.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Gosogliptin 869490-23-3 Others PF00734200 PF-00734200 PF 00734200 PF-734200 PF 734200 PF734200 inhibitor inhibit

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