For research use only. Not for therapeutic Use.
<p style=/line-height:25px/>Anagliptin is a potent and selective DPP-4 inhibitor(IC50= 3.8 nM); > 10 fold less potent for DPP-8 and DPP-9.<br>IC50 value: 3.8 nM [1]<br>Target: DPP-4 inhibitor<br>in vitro: In THP-1 cells, anagliptin reduced lipopolysaccharide-induced TNF-α production with inhibiting ERK phosphorylation and nuclear translocation of nuclear factor-κB [2]. lipopolysaccharide (LPS)- or palmitate-induced elevations of inflammatory cytokine mRNA expressions in RAW264.7 macrophages were shown to be significantly suppressed by co-incubation with a DPP-4 inhibitor, anagliptin (10μM), despite low DPP-4 expression in the RAW264.7 cells. Anagliptin also acted on 3T3-L1 adipocytes, weakly suppressing the inflammatory cytokine expressions induced by LPS and TNF-α. When 3T3-L1 and RAW cells were co-cultured and stimulated with LPS, the effects of anagliptin on the suppression of cytokine expressions in 3T3-L1 adipocytes were more marked, and became evident at the 10μM concentration [3].<br>in vivo: Treatment with anagliptin for 16 wk significantly reduced accumulation of monocytes and macrophages in the vascular wall, SMC content in plaque areas, and oil red O-stained area around the aortic valve without affecting glucose tolerance or body weight. Quantitative analysis also showed that anagliptin reduced the area of atherosclerotic lesion in apoE-deficient mice [2]. Anti-inflammatory effects of anagliptin were also observed in vivo on the elevated hepatic and adipose expressions and serum concentrations of inflammatory cytokines in association with the suppression of hepatic NF-κB transcriptional activity, in LPS-infused mice [3].</p>
| Catalog Number | I004746 |
| CAS Number | 739366-20-2 |
| Molecular Formula | C19H25N7O2 |
| Purity | ≥95% |
| Target | DPP-4 inhibitor |
| Solubility | DMSO: ≥ 36 mg/mL |
| Storage | Store at -20°C |
| IC50 | 3.8 nM [1] |
| InChI | InChI=1S/C19H25N7O2/c1-13-7-16-21-9-14(11-26(16)24-13)18(28)22-12-19(2,3)23-10-17(27)25-6-4-5-15(25)8-20/h7,9,11,15,23H,4-6,10,12H2,1-3H3,(H,22,28)/t15-/m0/s1 |
| InChIKey | LDXYBEHACFJIEL-HNNXBMFYSA-N |
| SMILES | O=C(C1=CN2C(N=C1)=CC(C)=N2)NCC(C)(NCC(N3[C@H](C#N)CCC3)=O)C |
| Reference | </br>1:Mechanism of lipid-lowering action of the dipeptidyl peptidase-4 inhibitor, anagliptin, in low-density lipoprotein receptor-deficient mice. Yano W, Inoue N, Ito S, Itou T, Yasumura M, Yoshinaka Y, Hagita S, Goto M, Nakagawa T, Inoue K, Tanabe S, Kaku K.J Diabetes Investig. 2017 Mar;8(2):155-160. doi: 10.1111/jdi.12593. Epub 2016 Dec 15. PMID: 27860391 Free PMC Article</br>2:Add-on therapy with anagliptin in Japanese patients with type-2 diabetes mellitus treated with metformin and miglitol can maintain higher concentrations of biologically active GLP-1/total GIP and a lower concentration of leptin. Osonoi T, Saito M, Hariya N, Goto M, Mochizuki K.Peptides. 2016 Dec;86:118-125. doi: 10.1016/j.peptides.2016.10.011. Epub 2016 Oct 22. PMID: 27780736 </br>3:Anagliptin increases insulin-induced skeletal muscle glucose uptake via an NO-dependent mechanism in mice. Sato H, Kubota N, Kubota T, Takamoto I, Iwayama K, Tokuyama K, Moroi M, Sugi K, Nakaya K, Goto M, Jomori T, Kadowaki T.Diabetologia. 2016 Nov;59(11):2426-34. doi: 10.1007/s00125-016-4071-8. Epub 2016 Aug 15. PMID: 27525648 </br>4:Anagliptin, A Dipeptidyl Peptidase-4 Inhibitor Ameliorates Arterial Stiffness in Association with Reduction of Remnant-Like Particle Cholesterol and Alanine Transaminase Levels in Type 2 Diabetic Patients. Tahara N, Yamagishi SI, Bekki M, Kodama N, Nakamura T, Sugiyama Y, Oshige T, Kumashiro Y, Honda A, Tahara A, Igata S, Fukumoto Y.Curr Vasc Pharmacol. 2016;14(6):552-562. PMID: 27357182 </br>5:Anagliptin, a dipeptidyl peptidase-4 inhibitor, decreases macrophage infiltration and suppresses atherosclerosis in aortic and coronary arteries in cholesterol-fed rabbits. Hirano T, Yamashita S, Takahashi M, Hashimoto H, Mori Y, Goto M.Metabolism. 2016 Jun;65(6):893-903. doi: 10.1016/j.metabol.2016.03.010. Epub 2016 Mar 18. PMID: 27173468 </br>6:Treatment with DPP-4I Anagliptin or α-GI Miglitol Reduces IGT Development and the Expression of CVD Risk Factors in OLETF Rats. Imai C, Harazaki T, Inoue S, Mochizuki K, Goda T.J Nutr Sci Vitaminol (Tokyo). 2015;61(4):313-21. doi: 10.3177/jnsv.61.313. PMID: 26440638 Free Article</br>7:Anagliptin, a potent dipeptidyl peptidase IV inhibitor: its single-crystal structure and enzyme interactions. Watanabe YS, Yasuda Y, Kojima Y, Okada S, Motoyama T, Takahashi R, Oka M.J Enzyme Inhib Med Chem. 2015 Dec;30(6):981-8. doi: 10.3109/14756366.2014.1002402. Epub 2015 Jul 6. PMID: 26147347 </br>8:Anagliptin decreases serum lathosterol level in patients with type 2 diabetes: a pilot study. Aoki K, Ijima T, Kamiyama H, Kamiko K, Terauchi Y.Expert Opin Pharmacother. 2015;16(12):1749-54. doi: 10.1517/14656566.2015.1057120. Epub 2015 Jun 22. PMID: 26098722 </br>9:High-fat diet feeding significantly attenuates anagliptin-induced regeneration of islets of Langerhans in streptozotocin-induced diabetic mice. Shinjo T, Nakatsu Y, Iwashita M, Sano T, Sakoda H, Ishihara H, Kushiyama A, Fujishiro M, Nishimura F, Asano T.Diabetol Metab Syndr. 2015 Jun 2;7:50. doi: 10.1186/s13098-015-0047-y. eCollection 2015. PMID: 26097511 Free PMC Article</br>10:DPP-IV inhibitor anagliptin exerts anti-inflammatory effects on macrophages, adipocytes, and mouse livers by suppressing NF-κB activation. Shinjo T, Nakatsu Y, Iwashita M, Sano T, Sakoda H, Ishihara H, Kushiyama A, Fujishiro M, Fukushima T, Tsuchiya Y, Kamata H, Nishimura F, Asano T.Am J Physiol Endocrinol Metab. 2015 Aug 1;309(3):E214-23. doi: 10.1152/ajpendo.00553.2014. Epub 2015 May 26. PMID: 26015438 Free Article |
