WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H319936
CAS#: 1029877-94-8 (succinate)
Description: Trelagliptin, also known as SYR-472, is a long acting dipeptidyl peptidase-4 (DPP-4) inhibitor that is being developed by Takeda for the treatment of type 2 diabetes (T2D). Once-weekly SYR-472 treatment produced clinically and statistically significant improvements in glycaemic control in patients with type 2 diabetes. It was well tolerated and might be a new treatment option for patients with this disease. Trelagliptin (Zafatek(®)) was approved in Japan for the treatment of type 2 diabetes mellitus.
Hodoodo Cat#: H319936
Name: Trelagliptin succinate
CAS#: 1029877-94-8 (succinate)
Chemical Formula: C22H26FN5O6
Exact Mass: 0.00
Molecular Weight: 475.477
Elemental Analysis: C, 55.57; H, 5.51; F, 4.00; N, 14.73; O, 20.19
Related CAS #: 1029877-94-8 (succinate) 865759-25-7 (free base)
Synonym: SYR472; SYR472; SYR 472; Trelagliptin, Trelagliptin succinate; brand name: Zafatek.
IUPAC/Chemical Name: (R)-2-((6-(3-aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-4-fluorobenzonitrile succinate
InChi Key: OGCNTTUPLQTBJI-XFULWGLBSA-N
InChi Code: 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
SMILES Code: O=C(O)CCC(O)=O.N#CC1=CC=C(F)C=C1CN(C(N2C)=O)C(N3C[C@H](N)CCC3)=CC2=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 475.48 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Harada N, Inagaki N. [Once-weekly DPP-4 inhibitor]. Nihon Rinsho. 2015 Dec;73(12):2096-102. Japanese. PubMed PMID: 26666159.
2: Deacon CF, Lebovitz HE. Comparative review of dipeptidyl peptidase-4 inhibitors and sulphonylureas. Diabetes Obes Metab. 2016 Apr;18(4):333-47. doi: 10.1111/dom.12610. Epub 2016 Jan 8. Review. PubMed PMID: 26597596.
3: Kaku K. First novel once-weekly DPP-4 inhibitor, trelagliptin, for the treatment of type 2 diabetes mellitus. Expert Opin Pharmacother. 2015;16(16):2539-47. doi: 10.1517/14656566.2015.1099630. Epub 2015 Nov 2. Review. PubMed PMID: 26523434.
4: McKeage K. Trelagliptin: First Global Approval. Drugs. 2015 Jul;75(10):1161-4. doi: 10.1007/s40265-015-0431-9. PubMed PMID: 26115728.
5: Kamiyama H, Terauchi Y. [Current status of clinical development of novel anti-diabetic drugs]. Nihon Rinsho. 2015 Mar;73(3):517-22. Japanese. PubMed PMID: 25812383.
6: Inagaki N, Onouchi H, Maezawa H, Kuroda S, Kaku K. 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 Mar;3(3):191-7. doi: 10.1016/S2213-8587(14)70251-7. Epub 2015 Jan 19. PubMed PMID: 25609193.
7: Inagaki N, Onouchi H, Sano H, Funao N, Kuroda S, Kaku K. 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 Feb;2(2):125-32. doi: 10.1016/S2213-8587(13)70149-9. Epub 2013 Nov 1. PubMed PMID: 24622716.
8: Garber AJ. The importance of incretin therapies for managing type 2 diabetes. Lancet Diabetes Endocrinol. 2014 Feb;2(2):95-7. doi: 10.1016/S2213-8587(13)70157-8. Epub 2013 Nov 1. PubMed PMID: 24622701.
