1246960-27-9|Evogliptin HCl|(R)-4-((R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl)-3-(tert-butoxymethyl)piperazin-2-one hydrochloride|-范德生物科技公司

Evogliptin HCl

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names：
(R)-4-((R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl)-3-(tert-butoxymethyl)piperazin-2-one hydrochloride
CAS号：
1246960-27-9
MDL Number：
MF(分子式)： C19H27ClF3N3O3 MW(分子量)： 437.8882
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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询价

中文别名	Evogliptin HCl
英文别名	DA-1229; DA 1229; DA1229; Evogliptin; Evogliptin hydrochloride.
CAS号	1246960-27-9
Inchi	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
InchiKey	QHQXWMKKQNSBTC-VQZRABBESA-N
分子式 Formula	C19H27ClF3N3O3
分子量 Molecular Weight	437.8882
溶解度Solubility
性状	Solid powder
储藏条件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

产品说明	Evogliptin HCl(CAS:1246960-27-9 ):仅限应用于工业或者科学研究过程中非医疗目的，不应用于人类或动物的临床诊断以及治过程疗，该产品非药用，非食用。
Introduction	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.
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备注

[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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