产品介绍
Product Description
Biochem/physiol Actions
Orally active, potent and selective phosphodiesterase 4 (PDE4) inhibitor in vitro and in vivo.
Apremilast (CC-10004) is an orally active, potent and selective phosphodiesterase 4 (PDE4) inhibitor (IC50 = 20/49/50/30 nM with recombinant human PDE4A4/B2/C2/D3 and 1 μM cAMP; no significant PDE1/2/3/5/7/8/9/10/11 inhibition at 10 μM). Apremilast effectively inhibits LPS-induced cytokine and chemokine protein expression from purified human PBMCs (TNFα/IFNγ/IL12 IC50 = 13/110/120 nM, IP10/MIG/MIP1α IC50 = 10/28/40 nM) in vitro and exhibits therapeutic efficacy in a psoriasis mouse model in vivo (2.5/mg/kg b.i.d. p.o.)
技术参数
Specifications
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | -10 to -25°C |
| SMILES string | [S](=O)(=O)(C[C@@H](N2C(=O)c3c(cccc3NC(=O)C)C2=O)c1cc(c(cc1)OC)OCC)C |
| InChI | 1S/C22H24N2O7S/c1-5-31-19-11-14(9-10-18(19)30-3)17(12-32(4,28)29)24-21(26)15-7-6-8-16(23-13(2)25)20(15)22(24)27/h6-11,17H,5,12H2,1-4H3,(H,23,25)/t17-/m1/s1 |
| InChI key | IMOZEMNVLZVGJZ-QGZVFWFLSA-N |
