| MK3102Novel long-acting DPP-4 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 = 98.16%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
MK3102 Dilution Calculator
calculate
MK3102 Molarity Calculator
calculate
| Cas No. | 1226781-44-7 | SDF | Download SDF |
| Chemical Name | (2R,3S,5R)-2-(2,5-difluorophenyl)-5-(2-(methylsulfonyl)pyrrolo[3,4-c]pyrazol-5(2H,4H,6H)-yl)tetrahydro-2H-pyran-3-amine | ||
| Canonical SMILES | CS(N1C=C2CN([C@](CO3)([H])C[C@@](N)([H])[C@@]3([H])C4=C(F)C=CC(F)=C4)CC2=N1)(=O)=O | ||
| Formula | C17H20F2N4O3S | M.Wt | 398.43 |
| Solubility | ≥17.15mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | 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. | ||
Dipeptidyl peptidase IV (DPP-4) inhibitors improve glycemic control in patients with type 2 diabetes by prolonging the half-life of incretin peptides, which stimulate insulin secretion and decrease glucagon release in a glucose-dependent manner. MK-3102 is a novel long-acting DPP-4 inhibitor.
In vitro: MK-3102 is a competitive, reversible inhibitor of DPP-4 and is more potent than sitagliptin. It is highly selective over all proteases tested, including QPP, FAP, PEP, DPP8, and DPP9. The compound has weak ion channel activity [1].
In vivo: MK-3102 was evaluated for its ability to improve glucose tolerance in lean mice. When orally administered 1 h prior to dextrose challenge in an oral glucose tolerance test, it significantly reduced blood glucose excursion in a dosedependent manner from 0.01 mg/kg to 0.3 mg/kg [1].
Clinical trial: MK-3102 is currently in phase 3 clinical trial for type 2 diabetes mellitus. Dose-dependent efficacy in 2 h post meal glucose reduction, fasting plasma glucose reduction, and HbA1c and safety profile similar to that seen with once daily DPP-4 inhibitor such as sitagliptin was observed in a 12-week phase IIB dose-rangefinding study [1].
Reference:[1] Biftu T, Sinha-Roy R, Chen P, Qian X, Feng D, Kuethe JT, Scapin G, Gao YD, Yan Y, Krueger D, Bak A, Eiermann G, He J, Cox J, Hicks J, Lyons K, He H, Salituro G, Tong S, Patel S, Doss G, Petrov A, Wu J, Xu SS, Sewall C, Zhang X, Zhang B, Thornberry NA, Weber AE. Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. J Med Chem. 2014 Apr 24;57(8):3205-12.
