SYR-472 MedChemExpress (MCE)

Product Name	Trelagliptin
Synonyms	Trelagliptin Trelagliptin(syr472) Trelagliptin free base Trelagliptin Isomer Impurity (S)-2-((6-(3-aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-4-fluorobenzonitrile Synonyms Trelagliptin Trelagliptin(syr472) Trelagliptin free base Trelagliptin Isomer Impurity (S)-2-((6-(3-aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-4-fluorobenzonitrile Benzonitrile, 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H) -pyrimidinyl]methyl]-4-fluoro- Trelagliptin (R)-2-[[6-(3-Aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl]methyl]-4-fluorobenzonitrile
CAS	865759-25-7
EINECS	1592732-453-0
Chemical Formula	C18H20FN5O2
Molecular Weight	357.38
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Package	10 mM * 1 mL;1 mg;5 mg;10 mg;50 mg;100 mg;500 mg
Price	Get quote
Descriptions	Trelagliptin Trelagliptin MedChemExpress (MCE) HY-15408 865759-25-7 SYR-472 99.54% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions Trelagliptin Trelagliptin MedChemExpress (MCE) HY-15408 865759-25-7 SYR-472 99.54% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. Trelagliptin (SYR-472) is a potent, orally active and highly selective DPP-4 inhibitor with an IC50 of 4 nM. Trelagliptin succinate improves glycemic control in vivo and can be used for the study of type 2 diabetes mellitus (T2DM). Dipeptidyl peptidase-4 (DPP-4) is one of the widely explored novel targets for type 2 diabetes mellitus (T2DM)?strategy to preserve the endogenous glucagon like peptide (GLP)-1 activity by inhibiting the DPP-4 action[1].Trelagliptin exhibits potent inhibitory activity toward DPP-4 prepared from Caco-2 cells with an IC50?value of 5.4 nM. Trelagliptin also inhibits human, dog, and rat plasma DPP-4 activity with IC50?values of 4.2 nM, 6.2 nM, and 9.7 nM, respectively[2].Trelagliptin is highly selective for DPP-4 and displays IC50?values >100,000 nM corresponding to >10,000-fold selectivity over DPP-2, DPP-8, DPP-9, PEP and FAPα activities. Trelagliptin shows DPP4 selective about 4- and 12-fold more potent than alogliptin (HY-A0023) and sitagliptin (HY-13749), respectively[2]. Trelagliptin (oral gavage 7 mg/kg single dose) shows sustained PD effect in dogs and gives >80% inhibition of DPP-4 activity even after 24h[1].Trelagliptin (oral gavage 3 mg/kg single dose 60 min prior to oral glucose) significantly improves the glucose tolerance capacity by decreasing the AUC0?120min of 19.3% compared with the vehicle group in ob/ob mice[3]. Trelagliptin (oral gavage 10 mg/kg once a week 8 weeks) caused significant reductions in fasting blood glucose (FBG) levels, and the average reduction during the entire treatment period is 16.8% compared to the control.It also increases insulin level and raised it by 1.7-fold in AUC0?120min in ob/ob mice[3]. DPP-4 \| \| \| \| \| \| \| \| \| \| [1]. Bhumika D Patel, et al. Recent approaches to medicinal chemistry and therapeutic potential of dipeptidyl peptidase-4 (DPP-4) inhibitors. Eur J Med Chem. 2014 Mar 3 74:574-605. [Content Brief] [2]. Charles E Grimshaw, et al. Trelagliptin (SYR-472, Zafatek), Novel Once-Weekly Treatment for Type 2 Diabetes, Inhibits Dipeptidyl Peptidase-4 (DPP-4) via a Non-Covalent Mechanism. PLoS One. 2016 Jun 21 11(6):e0157509. [Content Brief] [3]. Shiliang Li, et al. Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. J Med Chem. 2019 Mar 14 62(5):2348-2361. [Content Brief]
Last Update	2025-04-01 14:45:47

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