[CAS NO. 608141-41-9] Apremilast (CC-10004)

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Catalog:	SLK-S8034
Brand:	Selleck
CAS:	608141-41-9

Overview

MDL	MFCD18782607
Molecular Weight	460.5
Molecular Formula	C22H24N2O7S
SMILES	[C@H](CS(C)(=O)=O)(N1C(=O)C=2C(C1=O)=CC=CC2NC(C)=O)C3=CC(OCC)=C(OC)C=C3

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

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Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.1716 mL	10.8578 mL	21.7155 mL
5 mM	0.4343 mL	2.1716 mL	4.3431 mL
10 mM	0.2172 mL	1.0858 mL	2.1716 mL
50 mM	0.0434 mL	0.2172 mL	0.4343 mL

Description

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

Targets

PDE4 ^[1]	TNF-α ^[1]
74 nM	77 nM

In vitro

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. .

In vivo

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.

References

[1] Man HW, et al. J Med Chem, 2009,52(6), 1522-1524.
[2] Muller GW, et al. Bioorg Med Chem Lett, 1998,8(19), 2669-2674.
[3] PH Schafer, et al. Br J Pharmacol, 2010, 159(4), 842–855.
[4] Fiona E McCann,et al. Arthritis Res Ther, 2010, 12(3), R107.

Synonyms

Acetamide, N-[2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]-

N-[2-[(1S)-1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]acetamide

(S)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione

Apremilast

CC 10004

(S)-N-[2-[1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl]ethyl]-1,3-dioxoisoindolin-4-yl)acetamide

Otezla

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