Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C28H29N2O6.Na |
Molecular Weight | 512.5294 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[Na+].CC[C@@H](OC1=CC=CC(CN(CCCOC2=CC=C(OC)C=C2)C3=NC4=CC=CC=C4O3)=C1)C([O-])=O
InChI
InChIKey=JSNXVHCVJMDNKW-VQIWEWKSSA-M
InChI=1S/C28H30N2O6.Na/c1-3-25(27(31)32)35-23-9-6-8-20(18-23)19-30(28-29-24-10-4-5-11-26(24)36-28)16-7-17-34-22-14-12-21(33-2)13-15-22;/h4-6,8-15,18,25H,3,7,16-17,19H2,1-2H3,(H,31,32);/q;+1/p-1/t25-;/m1./s1
Molecular Formula | C28H29N2O6 |
Molecular Weight | 489.5397 |
Charge | -1 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Molecular Formula | Na |
Molecular Weight | 22.9898 |
Charge | 1 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Pemafibrate (Parmodia®) is a novel, highly selective peroxisome proliferator-activated receptor (PPAR)-α modulator (SPPARM). It acts by binding to PPAR-α and regulating the expression of target genes that modulate lipid metabolism, thereby decreasing plasma triglyceride levels and increasing high-density lipoprotein cholesterol levels. Developed by Kowa Company, Ltd., oral pemafibrate has been approved in Japan for the treatment of hyperlipidaemia (including familial hyperlipidaemia). Pemafibrate is undergoing phase III development in a
number of countries for the treatment of dyslipidaemias
and is also in phase III development for the treatment of
hypertriglyceridaemia.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL239 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17553678 |
1.0 nM [EC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Parmodia Approved UseIndicated for the treatment of hyperlipidaemia. Launch Date2017 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28929345
The recommended
dosage of oral pemafibrate is 0.1 mg twice daily
(administered in the morning and evening); this dosage can
be adjusted according to age and symptoms to a maximum
dosage of 0.2 mg twice daily.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27108950
Curator's Comment: To test for a direct effect on apoB secretion by intestinal epithelial cells, polarized
Caco-2/TC7 cells grown and polarized on a porous filter to mimic the human
intestinal barrier, were treated with the different PPARα ligands added to the apical
side. After 24 hours, medium in the basolateral compartment was collected,
chylomicrons isolated by centrifugation and apoB quantified by ELISA.
Pemafibrate (K-877) (10uM) significantly decreased apoB
secretion.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 11:20:12 GMT 2023
by
admin
on
Sat Dec 16 11:20:12 GMT 2023
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Record UNII |
321L8P020Q
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Record Status |
Validated (UNII)
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Record Version |
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321L8P020Q
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admin on Sat Dec 16 11:20:12 GMT 2023 , Edited by admin on Sat Dec 16 11:20:12 GMT 2023
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