Cas No.: | 1427782-89-5 |
Chemical Name: | N-(5-Phenyl-2-pyridinyl)-2-[(3,4,6,7-tetrahydro-4-oxo-3-phenylthieno[3,2-d]pyrimidin-2-yl)thio]acetamide |
Synonyms: | Porcn Inhibitor III,IWP-L6 |
SMILES: | O=C(NC1=NC=C(C2=CC=CC=C2)C=C1)CSC3=NC(CCS4)=C4C(N3C5=CC=CC=C5)=O |
Formula: | C25H20N4O2S2 |
M.Wt: | 472.58 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | IWP L6 is a Porcn inhibitor with EC50 of 0.5 nM. |
In Vivo: | IWP-L6 is stable in human plasma over 24 h, it was rapidly metabolized in rat plasma (t1/2 = 190 min), murine plasma (t1/2 = 2 min), and the murine liver S9 fractions (t1/2 = 26 min). The major metabolites are the amide cleavage products. Similar species-dependent metabolitic profiles due to the involvement of carboxylesterase (CES) have been reported with other drug candidates. Despite its modest metabolic stability in mouse-derived plasma, IWP-L6 was highly active in zebrafish. IWP-L6 exhibited more potent activity [1]. |
In Vitro: | IWP-L6 effectively suppressed the phosphorylation of dishevelled 2 (Dvl2) in HEK293 cells, a biochemical event associated with many Wnt-dependent cellular responses. IWP-L6 inhibits Wnt mediated branching morphogenesis in cultured embryonic kidneys [1].i |