Trelagliptin free base | SYR-472 | CAS#865759-25-7 | 1029877-94-8 | DPP-4 inhibitor

Trelagliptin
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 314244

CAS#: 865759-25-7 (free base)

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 (T2DM).

Chemical Structure

Trelagliptin

CAS# 865759-25-7 (free base)

Instruction

Theoretical Analysis

MedKoo Cat#: 314244
Name: Trelagliptin
CAS#: 865759-25-7 (free base)
Chemical Formula: C18H20FN5O2
Exact Mass: 357.16
Molecular Weight: 357.380
Elemental Analysis: C, 60.49; H, 5.64; F, 5.32; N, 19.60; O, 8.95

Price and Availability

Size	Price	Availability
25mg	USD 90	Ready to ship
50mg	USD 150	Ready to Ship
100mg	USD 250	Ready to ship
200mg	USD 450	Ready to ship
500mg	USD 950	Ready to ship
1g	USD 1650	Ready to ship
2g	USD 2950	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: SYR472; SYR472; SYR 472; Trelagliptin, 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.

InChi Key: IWYJYHUNXVAVAA-OAHLLOKOSA-N

InChi Code: 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

SMILES Code: 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.

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: Related CAS# 865759-25-7 (free base); 1029877-94-8 (succinate).

Certificate of Analysis:

View CoA: current batch, Lot#BBC51019

QC Data:

View QC data: current batch, Lot#BBC51019

Safety Data Sheet (SDS):

View Safety Data Sheet (SDS)

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 357.38 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:

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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.

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