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Trelagliptin succinate

DPP-4 inhibitor CAS# 1029877-94-8

Trelagliptin succinate

Catalog No. BCC2015----Order now to get a substantial discount!

Product Name & Size Price Stock
Trelagliptin succinate: 5mg $242 In Stock
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Chemical structure

Trelagliptin succinate

3D structure

Chemical Properties of Trelagliptin succinate

Cas No. 1029877-94-8 SDF Download SDF
PubChem ID 44183569 Appearance Powder
Formula C22H26FN5O6 M.Wt 475.47
Type of Compound N/A Storage Desiccate at -20°C
Synonyms SYR-472 succinate
Solubility DMSO : ≥ 50 mg/mL (105.16 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 2-[[6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]-4-fluorobenzonitrile;butanedioic acid
SMILES CN1C(=O)C=C(N(C1=O)CC2=C(C=CC(=C2)F)C#N)N3CCCC(C3)N.C(CC(=O)O)C(=O)O
Standard InChIKey OGCNTTUPLQTBJI-XFULWGLBSA-N
Standard InChI InChI=1S/C18H20FN5O2.C4H6O4/c1-22-17(25)8-16(23-6-2-3-15(21)11-23)24(18(22)26)10-13-7-14(19)5-4-12(13)9-20;5-3(6)1-2-4(7)8/h4-5,7-8,15H,2-3,6,10-11,21H2,1H3;1-2H2,(H,5,6)(H,7,8)/t15-;/m1./s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Trelagliptin succinate

DescriptionTrelagliptin(SYR-472) is a long acting dipeptidyl peptidase-4 (DPP-4) inhibitor that is being developed for the treatment of type 2 diabetes (T2D). IC50 value: Target: DPP4 Two Phase II clinical studies have been completed with Efficacy and Safety of SYR-472 in Subjects With Type 2 Diabetes Mellitus. Phase III clinical studies with trelagliptin in Japan to evaluate its safety and efficacy in a once-weekly oral treatment regimen. Currently, all available DPP-4 inhibitors are dosed once-daily. A once-weekly treatment, such as trelagliptin, would provide patients with a convenient treatment alternative and has the potential to improve treatment compliance.

References:
[1]. Efficacy of SYR-472 in Subjects With Type 2 Diabetes Mellitus [2]. Efficacy and Safety of SYR-472 in Subjects With Type 2 Diabetes Mellitus [3]. Long-term Study of SYR-472 [4]. SYR-472 Open-label Study

Trelagliptin succinate Dilution Calculator

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Trelagliptin succinate Molarity Calculator

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Preparing Stock Solutions of Trelagliptin succinate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.1032 mL 10.5159 mL 21.0318 mL 42.0636 mL 52.5796 mL
5 mM 0.4206 mL 2.1032 mL 4.2064 mL 8.4127 mL 10.5159 mL
10 mM 0.2103 mL 1.0516 mL 2.1032 mL 4.2064 mL 5.258 mL
50 mM 0.0421 mL 0.2103 mL 0.4206 mL 0.8413 mL 1.0516 mL
100 mM 0.021 mL 0.1052 mL 0.2103 mL 0.4206 mL 0.5258 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Trelagliptin succinate

Trelagliptin is a long acting dipeptidyl peptidase-4 (DPP-4) inhibitor that is being developed for the treatment of type 2 diabetes (T2D). Two Phase II clinical studies have been completed with Efficacy and Safety of SYR-472 in Subjects With Type 2 Diabetes Mellitus. Phase III clinical studies with trelagliptin in Japan to evaluate its safety and efficacy in a once-weekly oral treatment regimen. Currently, all available DPP-4 inhibitors are dosed once-daily. A once-weekly treatment, such as trelagliptin, would provide patients with a convenient treatment alternative and has the potential to improve treatment compliance.

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References on Trelagliptin succinate

Identification, characterization and HPLC quantification of process-related impurities in Trelagliptin succinate bulk drug: Six identified as new compounds.[Pubmed:27209451]

J Pharm Biomed Anal. 2016 Sep 5;128:18-27.

A sensitive, selective and stability indicating reversed-phase LC method was developed for the determination of process related impurities of Trelagliptin succinate in bulk drug. Six impurities were identified by LC-MS. Further, their structures were characterized and confirmed utilizing LC-MS/MS, IR and NMR spectral data. The most probable mechanisms for the formation of these impurities were also discussed. To the best of our knowledge, six structures among these impurities are new compounds and have not been reported previously. The superior separation was achieved on an InertSustain C18 (250mmx4.6mm, 5mum) column in a gradient mixture of acetonitrile and 20mmol potassium dihydrogen phosphate with 0.25% triethylamine (pH adjusted to 3.5 with phosphate acid). The method was validated as per regulatory guidelines to demonstrate system suitability, specificity, sensitivity, linearity, robustness, and stability.

Description

Trelagliptin succinate (SYR-472 succinate) is a long acting dipeptidyl peptidase-4 (DPP-4) inhibitor that is being developed for the treatment of type 2 diabetes (T2D).

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