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  4. PPI-1040

PPI-1040 is an orally bioavailable vinyl ether synthetic plasmalogen. PPI-1040 acts as a precursor of plasmalogen. PPI-1040 increases plasmalogen levels in plasmalogen-deficient mice and normalizes hyperactive behaviors in these mice. In wild-type mice, PPI-1040 retains the sn-1 vinyl ether group and sn-3 phosphoethanolamine group, and is converted into endogenous ethanolamine plasmalogen. PPI-1040 can be used in studies related to rhizomelic chondrodysplasia punctata.

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PPI-1040

PPI-1040 Chemical Structure

CAS No. : 1436673-69-6

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Description

PPI-1040 is an orally bioavailable vinyl ether synthetic plasmalogen. PPI-1040 acts as a precursor of plasmalogen. PPI-1040 increases plasmalogen levels in plasmalogen-deficient mice and normalizes hyperactive behaviors in these mice. In wild-type mice, PPI-1040 retains the sn-1 vinyl ether group and sn-3 phosphoethanolamine group, and is converted into endogenous ethanolamine plasmalogen. PPI-1040 can be used in studies related to rhizomelic chondrodysplasia punctata[1].

In Vivo

PPI-1040 (100 mg/kg; p.o.; single dose) is absorbed in wild-type C57BL/6 mice in the form of open-chain plasmalogens, which retain intact sn-1 vinyl ether bonds and sn-3 phosphoethanolamine bonds while undergoing sn-2 fatty acid remodeling[1].
PPI-1040 (50 mg/kg; p.o.; daily, 5 days per week; for 4 consecutive weeks) restores plasmalogen levels in plasma and some peripheral tissues, normalizes hyperactive behaviors in plasmalogen-deficient Pex7hypo/null RCDP model mice, and plasma plasmalogen levels are negatively correlated with activity indicators[1].

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

Animal Model: C57BL/6 (both sexes)[1]
Dosage: 100 mg/kg
Administration: p.o.; single dose
Result: Did not detect the closed-ring form of PPI-1050 in plasma.
Showed a time-dependent increase of the open-ring version (identical to endogenous PlsEtn 16:0/22:6), reaching a fold change of 250 at 6 hours.
Detected plasmalogens with various sn-2 fatty acids (18:1, 18:2, 22:4, 20:4, 20:5) containing the full 13C6 label, with fold changes mirroring the time-dependent increase of the target PlsEtn 16:0/22:6.
Did not detect metabolites with only 3 13C labels or vinyl-acyl glycerols.
Animal Model: Pex7hypo/null (B6;6NCrl;129S6-Pex7tm2.3Brav, 3-4 months old, both sexes); Pex7WT/WT and Pex7WT/hypo (control littermates)[1]
Dosage: 50 mg/kg
Administration: p.o.; daily, 5 days/week; 4 weeks
Result: Augmented plasma levels of most 16:0 (sn-1) PlsEtn species to near wild-type levels (except PlsEtn 16:0/22:4), restoring total 16:0 PlsEtn pool to ~50% of wild-type levels.
Increased PlsEtn levels in peripheral tissues: liver showed significant increases in 16:0/18:1, 16:0/18:2, and 16:0/22:6 species; skeletal muscle showed a significant increase in 16:0/22:6; small intestine showed significant increases in 16:0/18:1 and 16:0/18:2; heart showed significant increases in 16:0/18:1 and 16:0/20:4; erythrocytes showed significant increases in 16:0/18:1, 16:0/20:4, 16:0/22:6, and total 16:0 pool.
Did not observe plasmalogen augmentation in lung, kidney, cortex, or cerebellum.
Normalized hyperactive behavior in Pex7hypo/null mice, with distance traveled (0.74 meters) and time active (141 seconds) matching control levels.
Showed a significant inverse correlation between plasma PlsEtn 16:0/22:6 levels and distance traveled and time active.
Showed significant inverse correlations between total 16:0 PlsEtn pool levels and distance traveled and time active.
Molecular Weight

730.01

Formula

C43H72NO6P
CAS No.
SMILES

CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(OC(CO/C=C\CCCCCCCCCCCCCC)COP1(NCCO1)=O)=O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PPI-1040 Related Classifications

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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:

PPI-10401436673-69-6PPI1040PPI 1040Drug DerivativeDrug derivativeliverwild-type C57BL/6 miceskeletal musclePex7hypo/null miceerythrocytesopen field testrhizomelic chondrodysplasia punctataheartethanolamine plasmalogensmall intestinesynthetic vinyl ether plasmalogenInhibitorinhibitorinhibit

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