Apremilast (CC-10004) 608141-41-9

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Molecular Weight:

460.5 Apremilast (CC-10004) is a potent and orally active PDE4 and TNF-α inhibitor with IC50 of 74 nM and 77 nM, respectively.






Biological Activity


Apremilast is more potent for inhibition of PDE4 compared with cAMP or
cGMP hydrolysing enzymes from other PDE families. Apremilast displays a
broad pattern of anti-inflammatory activity in a variety of cell types,
inhibits TNF-α, IL-12 and IL-23 production, as well as NK and
keratinocyte responses. Apremilast is found to inhibit the
zymosan-induced PMN production of IL-8 with IC50 of 94 nM.


Apremilast
inhibits fMLF-induced PMN CD18 and CD11b expression with IC50 of 390 nM
and 74 nM, respectively, and inhibits fMLF-induced adhesion of PMN to
HUVECs with IC50 of 150 nM. Apremilast inhibits keratinocyte
TNF-αproduction, with no effect on keratinocyte cell viability as
measured by intracellular ATP levels.


Apremilast is stable in the presence of human microsomes (t1/2 > 60
min). It is 90% protein bound in human plasma. Oral and intravenous
administration of it in female rats showed that it have good
pharmacokinetics with low clearance, a moderate volume of distribution,
and a 64% oral bioavailability.


In a LPS-induced TNF-αinhibition model
in rats, examined the TNF-α inhibitory ability of Apremilast in vivo,
and the ED50 is determined to be 0.03 mg/kg. In another LPS-induced
neutrophilia model in rats, Apremilast exhibited an ED50 range from 0.3
mg/kg to 0.9 mg/kg.

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Product Categories : Metabolism > PDE Inhibitor