MK3102
Catalog No.: GC17012Purity:>99.00%Synonyms: Omarigliptin
MK3102 (Omarigliptin) is a novel once-weekly dipeptidyl peptidase-4 (DPP-4) inhibitor (IC50: 2.2 nM) developed for the treatment of type 2 diabetes.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1226781-44-7
10mM (in 1mL DMSO)In Stock
$20.00
1
5mgIn Stock
$109.00
1
2mgIn Stock
$113.00
1
10mgIn Stock
$162.00
1
50mgIn Stock
$437.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $20.00 | In Stock | 1 | |
| 5mg | $109.00 | In Stock | 1 | |
| 2mg | $113.00 | In Stock | 1 | |
| 10mg | $162.00 | In Stock | 1 | |
| 50mg | $437.00 | In Stock | 1 |
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com
Citations
2 publicationsPublications from researchers using this productDescription
MK3102 (Omarigliptin) is a novel once-weekly dipeptidyl peptidase-4 (DPP-4) inhibitor (IC50: 2.2 nM) developed for the treatment of type 2 diabetes [1,2]. MK3102 crossed the blood brain barrier (BBB) due to its low molecular weight and lipophilic properties [3].
MK3102 (3, 10, 30, and 50 µM, 4 h) pretreated PC12 cells were attenuated 6-OHDA (50 µM, 24h) - or rotenone (1 µM, 24h) - induced cytotoxicity. MK3102 inhibited the 6-OHDA- or rotenone-induced production of intracellular ROS in PC12 cells [4]. MK3102 decreased the 6-OHDA- and rotenone-induced IκBα phosphorylation and nuclear translocation of NF-κB, resulting in reduced production of the inflammatory mediator NO and iNOS expression [4]. MK3102 suppressed the release of HMGB-1, and decreased the permeability of endothelial monolayer in bEnd.3 brain endothelial cells [1].
MK3102 has a long half-life (rat, 11 h; dog, 22 h) and lower clearance (rat, 1.1 mL min-1 kg-1; dog, 0.9 mL min-1 kg-1) in preclinical species [5]. Concentration of MK3102 in rats' plasma (5 mg/kg, after 2 h, p.o) were found to be 2688.79 ng/mL, MK3102 crossed the BBB after the oral administration showing concentration of 621.75 ng/g in brain tissue. Intra-nasal administration of OG showed significant higher brain/plasma concentration ratio of 0.76 enhancing the ratio by 3.3 folds compared to the oral route [3]. MK3102 (5 mg/kg/d) suppressed the release of inflammatory factors in the brains of LPS-Stimulated mice and protected the BBB integrity destroyed by LPS stimulation [1].
References:
[1]. Du H, Wang S. Omarigliptin Mitigates Lipopolysaccharide-Induced Neuroinflammation and Dysfunction of the Integrity of the Blood-Brain Barrier. ACS Chemical Neuroscience. 2020 Nov 25;11(24):4262-9.
[2]. Hussain H, Abbas G, Green IR, Ali I. Dipeptidyl peptidase IV inhibitors as a potential target for diabetes: patent review (2015-2018). Expert opinion on therapeutic patents. 2019 Jul 3;29(7):535-53.
[3]. Ayoub BM, Mowaka S, Safar MM, Ashoush N, Arafa MG, Michel HE, Tadros MM, Elmazar MM, Mousa SA. Repositioning of omarigliptin as a once-weekly intranasal anti-parkinsonian agent. Scientific Reports. 2018 Jun 12;8(1):8959.
[4]. Gouda NA, Cho J. Omarigliptin Mitigates 6-Hydroxydopamine-or Rotenone-Induced Oxidative Toxicity in PC12 Cells by Antioxidant, Anti-Inflammatory, and Anti-Apoptotic Actions. Antioxidants. 2022 Sep 28;11(10):1940.
[5]. Biftu T, Sinha-Roy R, Chen P, Qian X, Feng D, Kuethe JT, Scapin G, Gao YD, Yan Y, Krueger D, Bak A. Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.
Protocol
| Cell experiment [1]: | |
|
Cell lines |
PC12 cells |
|
Preparation Method |
PC12 cells were treated with MK3102 at a series of concentrations in culture media containing low serum (1% FBS, 1% HS, 100 IU/mL penicillin, and 100 µg/mL streptomycin) for 24 h. Control cells were treated with the same media containing low serum and an equivalent volume of DMSO (0.5%). The protective effects of MK3102 against 6-OHDA- or rotenone-induced toxicity in PC12 cells were evaluated. Briefly, cells were pretreated with MK3102 at various concentrations for 4 h and subsequently exposed to 6-OHDA (50 µM) or rotenone (1 µM) for 24 h. The effect of ZnPP, an HO-1 inhibitor, on the protective effects of MK3102 against 6-OHDA- or rotenone-induced toxicity was evaluated. In brief, the cells were pretreated with 0.2 µM ZnPP for 30 min and exposed to MK3102 for 4 h. Then, 6-OHDA or rotenone was added at the final concentrations of 50 and 1 µM, respectively, and incubated for 24 h. |
|
Reaction Conditions |
0-100µM for 24 hours; 0-50µM pretreat for 4 hours |
|
Applications |
Pretreatment with MK3102 presented a significant reversal of the 6-OHDA-induced toxicity at concentrations of 30 and 50 µM. |
| Animal experiment [2]: | |
|
Animal models |
Male C57BL/6 mice |
|
Preparation Method |
The 24 mice (6- to 8-week-old) were divided into 4 groups: the vehicle, MK3102, LPS, and LPS + MK3102 groups. The animals were orally administered with either vehicle (saline) or MK3102 at 5 mg/kg/d for 15 days. On the last day, the animals in the LPS and the LPS + MK3102 groups were intraperitoneally injected with LPS (5 mg/kg). The control and the MK3102 groups were intraperitoneally injected with the same amounts of saline. |
|
Dosage form |
5 mg/kg/d, oral, for 15 days. |
|
Applications |
Compared with the vehicle group, the expression levels of TNF-α, IL-6, and IL-8 were elevated significantly in the brain of LPS stimulated mice but were greatly suppressed by the coadministration of MK3102. |
|
References: [1]: Gouda NA, Cho J. Omarigliptin Mitigates 6-Hydroxydopamine-or Rotenone-Induced Oxidative Toxicity in PC12 Cells by Antioxidant, Anti-Inflammatory, and Anti-Apoptotic Actions. Antioxidants. 2022 Sep 28;11(10):1940. | |
Product Documents
Purity:>99.00%Appearance:A solid
Biological Data
1 / 2
Chemical Properties
CAS No.
1226781-44-7
Synonyms
Omarigliptin
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
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
Molecular Formula
C17H20F2N4O3S
Molecular Weight
398.43
Solubility
≥ 17.15mg/mL in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
Reviews
Review for MK3102
Rating: 5
- 5 Star100%
- 4 Star0%
- 3 Star0%
- 2 Star0%
- 1 Star0%