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Volumn 21, Issue 12, 2011, Pages 3809-3812

Discovery of DA-1229: A potent, long acting dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes

Author keywords

DA 1229; Dipeptidyl peptidase IV; DPP 4; DPP 4 inhibitor; DPP IV; GLP 1

Indexed keywords

4 [3 AMINO 4 (2,4,5 TRIFLUOROPHENYL)BUTANOYL] 3 (TERT BUTOXYMETHYL)PIPERAZIN 2 ONE; ANTIDIABETIC AGENT; DA 1229; DIPEPTIDYL PEPTIDASE IV; DIPEPTIDYL PEPTIDASE IV INHIBITOR; GLUCOSE; PIPERAZINE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 79957865337     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.04.029     Document Type: Article
Times cited : (52)

References (22)
  • 5
    • 17844362518 scopus 로고    scopus 로고
    • For recent reviews, see
    • For recent reviews, see: (a) Mest, H.-J.; Mentlein, R. Diabetologia 2005, 48, 616;
    • (2005) Diabetologia , vol.48 , pp. 616
    • Mest, H.-J.1    Mentlein, R.2
  • 18
    • 79957856707 scopus 로고    scopus 로고
    • note
    • DPP-4 inhibition assay: Inhibitors at various concentrations were incubated with 20 ng/ml rhDPP-4 enzyme and 50 μMH-Gly-Pro-AMC for 1 h at 25 °C. The fluorescence (360 nm excitation/465 nm emission) was measured after 1 h.
  • 20
    • 79957869570 scopus 로고    scopus 로고
    • note
    • Compound 5f or vehicle (0.5% methylcellulose) was treated orally and then challenged with glucose (2 g/kg) 30 min post-dose. The blood glucose excursion profile from 0 to 120 min was used to integrate an area under for curve (AUC) and percent inhibition values for each treatment were generated from the AUC data normalized to the non-glucose controls.
  • 21
    • 79957826060 scopus 로고    scopus 로고
    • note
    • Off target selectivity was screened by MDS pharm service pharmacology packages: LeadProfilingScreen®, EnzymeProfilingScreen®.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.