MK3102Novel long-acting DPP-4 inhibitor CAS# 1226781-44-7 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 1226781-44-7 | SDF | Download SDF |
| PubChem ID | 46209133 | Appearance | Powder |
| Formula | C17H20F2N4O3S | M.Wt | 398.43 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | MK-3102 | ||
| Solubility | DMSO : 50 mg/mL (125.49 mM; Need ultrasonic) | ||
| Chemical Name | (2R,3S,5R)-2-(2,5-difluorophenyl)-5-(2-methylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl)oxan-3-amine | ||
| SMILES | CS(=O)(=O)N1C=C2CN(CC2=N1)C3CC(C(OC3)C4=C(C=CC(=C4)F)F)N | ||
| Standard InChIKey | MKMPWKUAHLTIBJ-ISTRZQFTSA-N | ||
| Standard InChI | InChI=1S/C17H20F2N4O3S/c1-27(24,25)23-7-10-6-22(8-16(10)21-23)12-5-15(20)17(26-9-12)13-4-11(18)2-3-14(13)19/h2-4,7,12,15,17H,5-6,8-9,20H2,1H3/t12-,15+,17-/m1/s1 | ||
| 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. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Omarigliptin(MK-3102) is a potent, selective and long-acting DPP-4 inhibitor with IC50 of 1.6 nM; highly selective over all
proteases tested (IC50 > 67 μM).
IC50 value: 1.6 nM [1]
Target: DPP-4 inhibitor
in vitro: Omarigliptin has weak ion channel activity (IC50 > 30 μM at IKr, Cav1.2, and Nav1.5). An expansive selectivity counterscreen (168 radioligand binding or enzymatic assays) was carried out at MDS Pharma. An IC50 > 10 μM was obtained in all assays.
in vivo: When orally administered 1 h prior to dextrose challenge in an oral glucose tolerance test (OGTT), it significantly reduced blood glucose excursion in a dose-dependent manner from 0.01 mg/kg (7% reduction in glucose AUC) to 0.3 mg/kg (51% reduction). References: | |||||
MK3102 Dilution Calculator
MK3102 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.5099 mL | 12.5493 mL | 25.0985 mL | 50.197 mL | 62.7463 mL |
| 5 mM | 0.502 mL | 2.5099 mL | 5.0197 mL | 10.0394 mL | 12.5493 mL |
| 10 mM | 0.251 mL | 1.2549 mL | 2.5099 mL | 5.0197 mL | 6.2746 mL |
| 50 mM | 0.0502 mL | 0.251 mL | 0.502 mL | 1.0039 mL | 1.2549 mL |
| 100 mM | 0.0251 mL | 0.1255 mL | 0.251 mL | 0.502 mL | 0.6275 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
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