- Vildagliptin (LAF-237)
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- Sitagliptin phosphate monohydrate
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| NVP DPP 728 dihydrochlorideDPP-IV inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 99.40%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Description | NVP DPP 728 dihydrochloride is a potent and orally active inhibitor of dipeptidyl peptidase (DPP)-IV with Ki and IC50 values of 11 nM and 14 nM, respectively. | |||||
| Targets | DPP-IV | |||||
| IC50 | 14 nM (Ki = 11 nM) | |||||
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| Cas No. | 247016-69-9 | SDF | Download SDF |
| Chemical Name | 6-[2-[[2-(2-cyanopyrrolidin-1-yl)-2-oxoethyl]amino]ethylamino]pyridine-3-carbonitrile;dihydrochloride | ||
| Canonical SMILES | C1CC(N(C1)C(=O)CNCCNC2=NC=C(C=C2)C#N)C#N.Cl.Cl | ||
| Formula | C15H18N6O.2HCl | M.Wt | 371.27 |
| Solubility | ≥17.75mg/mL in DMSO with gentle warming | Storage | Desiccate at RT |
| Physical Appearance | A yellow oil | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
NVP DPP 728 dihydrochlorideDescription:Ki: Inhibit human DPP-IV amidolytic activity with a Ki of 11 nM [1]Inhibitors of dipeptidyl peptidase 4, also known as DPP-4 inhibitors or gliptins, are a class of oral hypoglycemics that can be used to treat diabetes mellitus type 2. NVP DPP 728 dihydrochloride is a potent and orally active inhibitor of dipeptidyl peptidase (DPP)-IV.In vitro: NVP-DPP728 was found to inhibit human DPP-IV amidolytic activity with a Ki of 11 nM, a kon value of 1.3 x 105 M-1 s-1, and a koff of 1.3 x 10-3 s-1. NVP-DPP728 inhibited DPP-IV in a manner consistent with a two-step inhibition mechanism. Taken together, these data suggest that NVP-DPP728 inhibits DPP-IV through formation of a novel, reversible, nitrile-dependent complex with transition state characteristics [1]. In vivo: Aging caused a decrease in early insulin response after an oral glucose challenge in aged Wistar or DPP-IV(+) F344 rats, but not in aged DPP-IV(-) F344 rats, compared with young control groups. Glucose tolerance after an oral glucose challenge in aged DPP-IV(-) F344 rats was better than in aged DPP-IV(+) F344 and Wistar rats associated with the preservation of the early insulin response. NVP-DPP728 improved the glucose tolerance after an oral glucose challenge by potentiating the early insulin response throughout the inhibition of plasma DPP-IV activity in aged DPP-IV(+) Wistar andF34 4 rats. In contrast, NVP-DPP728 did not affect the glucose tolerance after an oral glucose challenge in aged DPP-IV(-) F344 rats. These results indicate that treatment with NVP-DPP728 ameliorated glucose tolerance in aged rats by the direct inhibition of plasma DPP-IV activity and presumably the subsequent increase in endogenous incretin action [2]. Clinical trial: NVP-DPP728 is currently in the preclinical development and no clinical trial is ongoing.Reference:[1] Hughes TE, Mone MD, Russell ME, Weldon SC, Villhauer EB. NVP-DPP728 (1-[[[2-[(5-cyanopyridin-2-yl)amino]ethyl]amino]acetyl]-2-cyano-(S)-pyrrolidine), a slow-binding inhibitor of dipeptidyl peptidase IV. Biochemistry. 1999;38(36):11597-603.[2] Mitani H, Takimoto M, Kimura M. Dipeptidyl peptidase IV inhibitor NVP-DPP728 ameliorates early insulin response and glucose tolerance in aged rats but not in aged Fischer 344 rats lacking its enzyme activity. Jpn J Pharmacol. 2002;88(4):451-8.
