Trelagliptin

Catalog No.S7513

Trelagliptin is a highly selective, long-acting DPP-4 inhibitor. Phase 3.

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Trelagliptin Chemical Structure

Trelagliptin Chemical Structure
Molecular Weight: 357.38

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description Trelagliptin is a highly selective, long-acting DPP-4 inhibitor. Phase 3.
Targets DPP-4 [1]
In vitro
In vivo Trelagliptin improves glycaemic control by inhibition of DPP-4 activity. [1]
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Inagaki N, et al. Lancet Diabetes Endocrinol. 2014, 2(2), 125-132.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02771093 Recruiting Type 2 Diabetes Mellitus Takeda July 2016 Phase 4
NCT02512068 Recruiting Type 2 Diabetes Mellitus Takeda August 2015 Phase 3
NCT02372097 Completed Healthy Takeda March 2015 Phase 1
NCT02324569 Active, not recruiting Type 2 Diabetes Mellitus Takeda December 2014 Phase 3
NCT01751360 Completed Diabetes Mellitus Takeda April 2013 Phase 3

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Chemical Information

Molecular Weight (MW) 357.38
Formula

C18H20FN5O2

CAS No. 865759-25-7
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms SYR-472
Solubility (25°C) * In vitro DMSO 71 mg/mL (198.66 mM)
Ethanol 3 mg/mL warming (8.39 mM)
Water <1 mg/mL
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Benzonitrile, 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H) -pyrimidinyl]methyl]-4-fluoro-

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

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