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| | Trelagliptin Basic information |
| Product Name: | Trelagliptin | | Synonyms: | Trelagliptin(syr472);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;(S)-2-((6-(3-aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-4-fluorobenzonitrile;Trelagliptin Isomer Impurity;Trelagliptin, >=98%;Trelagliptin free base;Trelagliptin | | CAS: | 865759-25-7 | | MF: | C18H20FN5O2 | | MW: | 357.38 | | EINECS: | 1592732-453-0 | | Product Categories: | API;Trelagliptin;Inhibitors | | Mol File: | 865759-25-7.mol |  |
| | Trelagliptin Chemical Properties |
| Boiling point | 519.0±60.0 °C(Predicted) | | density | 1.38±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | ≥11.6 mg/mL in DMSO; ≥3.68 mg/mL in EtOH with gentle warming and ultrasonic; ≥93.8 mg/mL in H2O | | pka | 9.88±0.20(Predicted) | | form | solid | | InChI | InChI=1S/C18H20FN5O2/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/h4-5,7-8,15H,2-3,6,10-11,21H2,1H3/t15-/m1/s1 | | InChIKey | IWYJYHUNXVAVAA-OAHLLOKOSA-N | | SMILES | C(#N)C1=CC=C(F)C=C1CN1C(=O)N(C)C(=O)C=C1N1CCC[C@@H](N)C1 |
| | Trelagliptin Usage And Synthesis |
| Uses | Trelagliptin is a highly selective, long-acting dipeptidyl peptidase IV (DPP-4) inhibitor. This inhibitor provides sustained reduction of plasma DPP-4 activity and lowering of blood glucose in animal models of diabetes. | | Definition | ChEBI: Trelagliptin is a member of benzenes and a nitrile. | | Biological Activity | trelagliptin (syr-472) is a selective inhibitor of dpp-4 and is developed for the treatment of type 2 diabetes mellitus (t2dm) [1].dipeptidyl peptidase (dpp)-4 also known as adenosine deaminase complexing protein 2 or cd26 is an antigenic enzyme that expressed on the surface of most cell types and plays an important role in regulating immune system, signal transduction and apoptosis [2, 3].trelagliptin (syr-472) is a potent dpp-4 inhibitor and can be administered once weekly which unlike its other class approved agents that be taken once daily [1]. in japan, | | target | DPP-4 | | references | [1]. mckeage, k., trelagliptin: first global approval. drugs, 2015. 75(10): p. 1161-4.
[2]. inagaki, n., et al., once-weekly trelagliptin versus daily alogliptin in japanese patients with type 2 diabetes: a randomised, double-blind, phase 3, non-inferiority study. lancet diabetes endocrinol, 2015. 3(3): p. 191-7.
[3]. inagaki, n., et al., syr-472, a novel once-weekly dipeptidyl peptidase-4 (dpp-4) inhibitor, in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial. lancet diabetes endocrinol, 2014. 2(2): p. 125-32. |
| | Trelagliptin Preparation Products And Raw materials |
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