elovl6

ELOVL6-IN-1 is a potent, orally active, and selective ELOVL6 inhibitor that dose-dependently inhibits mouse ELOVL6 activities with an IC50 value of 0.350 μM. It inhibits ELOVL6 in a noncompetitive manner for malonyl-CoA (Ki=994 nM) and palmitoyl-CoA[1].

ELOVL6-IN-1 is a potent, selective, and orally active inhibitor of ELOVL6, exhibiting dose-dependent inhibition of mouse ELOVL6 with an IC50 of 0.350 μM and acting as a noncompetitive inhibitor with respect to malonyl-CoA (Ki=994 nM) and palmitoyl-CoA [1].

ELOVL6-IN-4 is a potent and selective long chain fatty acid elongase 6 (ELOVL6) inhibitor that is orally active, with IC50 values of 79 nM for human ELOVL6 and 94 nM for mouse ELOVL6. It demonstrates excellent selectivity over other human ELOVL subtypes (ELOVL1, -2, -3, and -5) and mouse ELOVL3 [1].

ELOVL6-IN-2 is a orally active and selective ELOVL6 inhibitor.

ELOVL6-IN-5 (compound B) acts as an inhibitor targeting the elongase enzyme of the long-chain fatty acid family 6 (ELOVL6). This enzyme is pivotal in the elongation process of saturated and monounsaturated long-chain fatty acids, marking it as a strategic target for diabetes intervention. In a mouse model of diet-induced obesity (DIO), ELOVL6-IN-5 effectively reduces hepatic fatty acid levels. However, it fails to enhance insulin sensitivity.

PF-3774076 is a CNS penetrant, potent, selective, partial agonist at the human α1A adrenoceptor. PF-3774076 is selective over α1B and α1D adrenoceptors.

AJ-108235 is a novel inhibitor of long chain fatty acid elongase 6 (ELOVL6).