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Chemical Structure| 1226781-44-7 Chemical Structure| 1226781-44-7

Structure of Omarigliptin
CAS No.: 1226781-44-7

Chemical Structure| 1226781-44-7

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Omarigliptin, also called MA-3102, is an selective inhibitor of DPP-4 with IC50 of 1.6 nM and Ki of 0.8 nM. Its selectivity is higher than other 168 proteasomes.

Synonyms: MK-3102

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Product Details of Omarigliptin

CAS No. :1226781-44-7
Formula : C17H20F2N4O3S
M.W : 398.43
SMILES Code : N[C@@H]1[C@@H](C2=CC(F)=CC=C2F)OC[C@H](N3CC4=NN(S(=O)(C)=O)C=C4C3)C1
Synonyms :
MK-3102
MDL No. :MFCD22573261
InChI Key :MKMPWKUAHLTIBJ-ISTRZQFTSA-N
Pubchem ID :46209133

Safety of Omarigliptin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
PC12 cells 3, 10, 30, 50 µM 6 h To evaluate the effect of OMG on 6-OHDA or rotenone-induced ROS generation in PC12 cells, results showed that OMG significantly reduced ROS production induced by 6-OHDA and rotenone. PMC9598347
PC12 cells 3, 10, 30, 50 µM 24 h To evaluate the protective effects of OMG against 6-OHDA or rotenone-induced toxicity in PC12 cells, results showed that OMG significantly reversed the toxicity induced by 6-OHDA and rotenone. PMC9598347
PC12 cells 3, 10, 30, 50, 100 µM 24 h To evaluate the cytotoxicity of OMG on PC12 cells, results showed that OMG did not significantly alter cell viability at the tested concentrations. PMC9598347
Primary cortical neurons 10 μM 24 h MK3102 significantly reduced hemin-induced ferroptosis in vitro by upregulating GPX4 and AIFM2 expression, and decreasing FACL4 expression, thereby reducing ROS, iron, and lipid peroxidation levels. PMC10474264

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Intracerebral hemorrhage model Gavage 7 mg/kg Once daily for 3 days To evaluate the protective effects of Omarigliptin on the integrity of the blood-brain barrier after intracerebral hemorrhage. The results showed that Omarigliptin significantly reduced hematoma formation and neurobehavioral deficits, lowered the activation of microglia/macrophages and infiltration of neutrophils, and protected the integrity of the blood-brain barrier. PMC10278948
C57BL/6 mice Intracerebral hemorrhage model Gastric injection 7 mg/kg Once daily for 3 days MK3102 significantly reduced brain damage area and neuronal death after ICH in mice, upregulated GLP-1R expression, and inhibited the expression of ferroptosis-related markers. PMC10474264

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01767688 Diabetes Mellitus, Type 2 PHASE1 COMPLETED 2013-03-07 -
NCT01407276 Chronic Renal Insufficiency|Ty... More >>pe 2 Diabetes Mellitus Less << PHASE1 COMPLETED 2012-03-23 -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.51mL

0.50mL

0.25mL

12.55mL

2.51mL

1.25mL

25.10mL

5.02mL

2.51mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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