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ELOVL6 inhibitor Compound A

Chemical Structure : ELOVL6 inhibitor Compound A

CAS No.: 1185736-98-4

ELOVL6 inhibitor Compound A

Catalog No.: PC-20304Not For Human Use, Lab Use Only.

ELOVL6 inhibitor Compound-A is a potent, selective inhibitor of elongase of long-chain fatty acids family 6 (ELOVL6) with IC50 of 169 and 350 nM for human and mouse ELOVL6, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

ELOVL6 inhibitor Compound-A is a potent, selective inhibitor of elongase of long-chain fatty acids family 6 (ELOVL6) with IC50 of 169 and 350 nM for human and mouse ELOVL6, respectively.
Compound-A displays >30-fold selectivity over recombinant human ELOVL family enzymes (ELOVL1, -2, -3, and -5, IC50 values >5-10 uM), also shows negligible or very weak inhibitory effects on rat microsomal SCD, human ACC1 and -2, and human FAS.
Compound-A inhibits ELOVL6 in a noncompetitive manner for malonyl-CoA (Ki=994 nM) and in an uncompetitive manner for palmitoyl-CoA.
Compound-A effectively reduced the elongation index of fatty acids of hepatocytes.
Compound-A (100 mg/kg, oral) significantly reduced the elongation index of the total fatty acids of the liver in mice.

Physicochemical Properties

M.Wt 495.50
Formula C27H24F3N3O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5,5-dimethyl-3-(5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)-1-phenyl-3-(trifluoromethyl)-3,5,6,7-tetrahydro-1H-indole-2,4-dione

References

1. Ken Shimamura, et al. J Pharmacol Exp Ther. 2009 Jul;330(1):249-56.

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