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MedKoo Cat#: 319714 | Name: Evogliptin HCl

Description:

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

Evogliptin, also known as DA-1229, is a potent and selective DPP4 inhibitor (dipeptidyl peptidase 4 inhibitor). Evogliptin improves insulin resistance and delays the onset of diabetes. Evogliptin improves the insulin sensitivity in HF mice and delays the onset of diabetes in young db/db mice. DA-1229 monotherapy (5 mg for 12 weeks) improved HbA1c, fasting plasma glucose level, OGTT results and β-cell function. This drug was well tolerated in Korean subjects with type 2 diabetes mellitus.

Chemical Structure

Evogliptin HCl
Evogliptin HCl
CAS#1246960-27-9 (HCl)

Theoretical Analysis

MedKoo Cat#: 319714

Name: Evogliptin HCl

CAS#: 1246960-27-9 (HCl)

Chemical Formula: C19H27ClF3N3O3

Exact Mass: 401.1926

Molecular Weight: 437.89

Elemental Analysis: C, 52.12; H, 6.22; Cl, 8.10; F, 13.02; N, 9.60; O, 10.96

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
1222102-29-5 (free base) 1246960-27-9 (HCl)
Synonym
DA-1229; DA 1229; DA1229; Evogliptin; Evogliptin hydrochloride.
IUPAC/Chemical Name
(R)-4-((R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl)-3-(tert-butoxymethyl)piperazin-2-one hydrochloride
InChi Key
QHQXWMKKQNSBTC-VQZRABBESA-N
InChi Code
InChI=1S/C19H26F3N3O3.ClH/c1-19(2,3)28-10-16-18(27)24-4-5-25(16)17(26)8-12(23)6-11-7-14(21)15(22)9-13(11)20;/h7,9,12,16H,4-6,8,10,23H2,1-3H3,(H,24,27);1H/t12-,16-;/m1./s1
SMILES Code
O=C1NCCN(C(C[C@H](N)CC2=CC(F)=C(F)C=C2F)=O)[C@@H]1COC(C)(C)C.[H]Cl
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

Preparing Stock Solutions

The following data is based on the product molecular weight 437.89 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.

Recalculate based on batch purity %
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
1: Jung CH, Park CY, Ahn KJ, Kim NH, Jang HC, Lee MK, Park JY, Chung CH, Min KW, Sung YA, Park JH, Kim SJ, Lee HJ, Park SW. A randomized, double-blind, placebo-controlled, phase II clinical trial to investigate the efficacy and safety of oral DA-1229 in patients with type 2 diabetes mellitus who have inadequate glycaemic control with diet and exercise. Diabetes Metab Res Rev. 2015 Mar;31(3):295-306. doi: 10.1002/dmrr.2613. Epub 2014 Dec 5. PubMed PMID: 25362864; PubMed Central PMCID: PMC4670720. 2: Gu N, Park MK, Kim TE, Bahng MY, Lim KS, Cho SH, Yoon SH, Cho JY, Jang IJ, Yu KS. Multiple-dose pharmacokinetics and pharmacodynamics of evogliptin (DA-1229), a novel dipeptidyl peptidase IV inhibitor, in healthy volunteers. Drug Des Devel Ther. 2014 Oct 6;8:1709-21. doi: 10.2147/DDDT.S65678. eCollection 2014. PubMed PMID: 25336915; PubMed Central PMCID: PMC4199987. 3: Kim DH, Lee JC, Lee MK, Kim KW, Lee MS. Treatment of autoimmune diabetes in NOD mice by Toll-like receptor 2 tolerance in conjunction with dipeptidyl peptidase 4 inhibition. Diabetologia. 2012 Dec;55(12):3308-17. doi: 10.1007/s00125-012-2723-x. Epub 2012 Sep 27. PubMed PMID: 23011352. 4: Kim TE, Lim KS, Park MK, Yoon SH, Cho JY, Shin SG, Jang IJ, Yu KS. Evaluation of the pharmacokinetics, food effect, pharmacodynamics, and tolerability of DA-1229, a dipeptidyl peptidase IV inhibitor, in healthy volunteers: first-in-human study. Clin Ther. 2012 Sep;34(9):1986-98. doi: 10.1016/j.clinthera.2012.08.006. Epub 2012 Sep 1. PubMed PMID: 22943970. 5: Kim MK, Chae YN, Kim HD, Yang EK, Cho EJ, Choi SH, Cheong YH, Kim HS, Kim HJ, Jo YW, Son MH, Kim SH, Shin CY. DA-1229, a novel and potent DPP4 inhibitor, improves insulin resistance and delays the onset of diabetes. Life Sci. 2012 Jan 2;90(1-2):21-9. doi: 10.1016/j.lfs.2011.10.007. Epub 2011 Oct 20. PubMed PMID: 22056373. 6: Kim HJ, Kwak WY, Min JP, Lee JY, Yoon TH, Kim HD, Shin CY, Kim MK, Choi SH, Kim HS, Yang EK, Cheong YH, Chae YN, Park KJ, Jang JM, Choi SJ, Son MH, Kim SH, Yoo M, Lee BJ. Discovery of DA-1229: a potent, long acting dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3809-12. doi: 10.1016/j.bmcl.2011.04.029. Epub 2011 Apr 13. PubMed PMID: 21570283. 7: Cho JM, Jang HW, Cheon H, Jeong YT, Kim DH, Lim YM, Choi SH, Yang EK, Shin CY, Son MH, Kim SH, Kim HJ, Lee MS. A novel dipeptidyl peptidase IV inhibitor DA-1229 ameliorates streptozotocin-induced diabetes by increasing β-cell replication and neogenesis. Diabetes Res Clin Pract. 2011 Jan;91(1):72-9. doi: 10.1016/j.diabres.2010.10.012. Epub 2010 Nov 18. PubMed PMID: 21093089.

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