Omarigliptin (Synonyms: MK-3102)

Name: Omarigliptin
Brand: MedChemExpress
SKU: HY-15981
Rating: 4.5 (1 reviews)

Cat. No.: HY-15981 Purity: 99.88%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Omarigliptin (MK-3102) is a potent, selective, orally active and cross the blood-brain barrier dipeptidyl peptidase 4 (DPP-4) inhibitor. Omarigliptin shows anti-parkinsonian activity. Omarigliptin has the neuroprotective effect to improve diabetes-associated cognitive dysfunction.

For research use only. We do not sell to patients.

Omarigliptin Chemical Structure

CAS No. : 1226781-44-7

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 185	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 185	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	USD 61	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 99	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 165	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 495	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 715	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Omarigliptin:

Omarigliptin (Standard) Get quote

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View All Isoforms

DPP-1 DPP-2 DPP-4 DPP-8 DPP-9

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

DPP-4

Cellular Effect

Cell Line	Type	Value	Description	References
COS-7	IC₅₀	> 100000 nM Compound: 20	Inhibition of C-terminal His-tagged DPP8 (unknown origin) expressed in COS7 cells using H-Ala-Pro-pNA substrate preincubated for 15 mins Inhibition of C-terminal His-tagged DPP8 (unknown origin) expressed in COS7 cells using H-Ala-Pro-pNA substrate preincubated for 15 mins	[PMID: 26546218]
Sf9	IC₅₀	> 100000 nM Compound: 20	Inhibition of N-terminal FLAG tagged human QPP expressed in Sf9 cells using Nle-Pro-AMC substrate after 30 mins by plate reader analysis Inhibition of N-terminal FLAG tagged human QPP expressed in Sf9 cells using Nle-Pro-AMC substrate after 30 mins by plate reader analysis	[PMID: 26546218]
Sf9	IC₅₀	2.22 nM Compound: 5; MK-3102	Inhibition of DPP4 (unknown origin) expressed in Sf9 cells using Gly-Pro-AMC substrate Inhibition of DPP4 (unknown origin) expressed in Sf9 cells using Gly-Pro-AMC substrate	[PMID: 27396490]
Sf9	IC₅₀	2.6 nM Compound: 20	Inhibition of recombinant human DPP4 expressed in Sf9 cells using Gly-Pro-AMC substrate after 30 mins by plate reader analysis Inhibition of recombinant human DPP4 expressed in Sf9 cells using Gly-Pro-AMC substrate after 30 mins by plate reader analysis	[PMID: 26546218]

In Vivo

Omarigliptin (5 mg/kg; p.o.) enhances the intestinal glucagon like peptide-1 and crosses BBB in rats^[1].
Omarigliptin (2.5, 5 mg/kg; p.o.; once a week for 8 weeks) shows anti-diabetic activity in STZ-induced diabetic mice^[2].
Omarigliptin (5 mg/kg; p.o.; daily for 28 days) shows anti-parkinsonian activity in rats^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	12 weeks, C57BL/6 male mice^[2]
Dosage:	2.5, 5 mg/kg
Administration:	P.o.; once a week for 8 weeks (50 mg/kg streptozotocin (STZ); i.p.; daily for five days)
Result:	Reduced the food and water intake, and caused a significant decrease in blood glucose, accompanied by increased serum insulin levels, improved insulin sensitivity and cognitive function, ameliorated diabetes-induced mitochondrial dysfunction in the brain.

Animal Model:	250±35 g , rats^[3]
Dosage:	5 mg/kg
Administration:	P.o.; daily for 28 days
Result:	Increased in brain GLP-1 concentration and passed through the BBB following oral administration.

Clinical Trial

Molecular Weight

398.43

Formula

C₁₇H₂₀F₂N₄O₃S

CAS No.

1226781-44-7

Appearance

Solid

Color

White to off-white

SMILES

N[C@@H]1[C@@H](C2=CC(F)=CC=C2F)OC[C@H](N3CC4=NN(S(=O)(C)=O)C=C4C3)C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (125.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5099 mL	12.5493 mL	25.0985 mL
5 mM	0.5020 mL	2.5099 mL	5.0197 mL
10 mM	0.2510 mL	1.2549 mL	2.5099 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.27 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.27 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.27 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.88%

Select Batch:

Data Sheet (273 KB) SDS (393 KB)

COA (247 KB) HNMR (170 KB) RP-HPLC (217 KB)

Handling Instructions (2659 KB)

References

[1]. Ayoub BM, et al. Repositioning of Omarigliptin as a once-weekly intranasal Anti-parkinsonian Agent. Sci Rep. 2018 Jun 12;8(1):8959. [Content Brief]

[2]. Li X, et al. Omarigliptin alleviates cognitive dysfunction in Streptozotocin-induced diabetic mouse. Bioengineered. 2022 Apr;13(4):9387-9396. [Content Brief]

[3]. Ayoub BM, et al. Repurposing of Omarigliptin as a Neuroprotective Agent Based on Docking with A2A Adenosine and AChE Receptors, Brain GLP-1 Response and Its Brain/Plasma Concentration Ratio after 28 Days Multiple Doses in Rats Using LC-MS/MS. Molecules. 2021 Feb 8;26(4):889. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5099 mL	12.5493 mL	25.0985 mL	62.7463 mL
	5 mM	0.5020 mL	2.5099 mL	5.0197 mL	12.5493 mL
	10 mM	0.2510 mL	1.2549 mL	2.5099 mL	6.2746 mL
	15 mM	0.1673 mL	0.8366 mL	1.6732 mL	4.1831 mL
	20 mM	0.1255 mL	0.6275 mL	1.2549 mL	3.1373 mL
	25 mM	0.1004 mL	0.5020 mL	1.0039 mL	2.5099 mL
	30 mM	0.0837 mL	0.4183 mL	0.8366 mL	2.0915 mL
	40 mM	0.0627 mL	0.3137 mL	0.6275 mL	1.5687 mL
	50 mM	0.0502 mL	0.2510 mL	0.5020 mL	1.2549 mL
	60 mM	0.0418 mL	0.2092 mL	0.4183 mL	1.0458 mL
	80 mM	0.0314 mL	0.1569 mL	0.3137 mL	0.7843 mL
	100 mM	0.0251 mL	0.1255 mL	0.2510 mL	0.6275 mL

Omarigliptin Related Classifications

Neurological Disease Metabolic Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Omarigliptin1226781-44-7MK-3102MK3102MK 3102Dipeptidyl PeptidaseDPPorally activeblood-brain barrieranti-parkinsoniananti-diabeticglucagon like peptide-1Inhibitorinhibitorinhibit

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Omarigliptin (Synonyms: MK-3102)

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Other Forms of Omarigliptin:

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View All Dipeptidyl Peptidase Isoform Specific Products:

Biological Activity

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References

Customer Review

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Complete Stock Solution Preparation Table

Omarigliptin Related Classifications

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