| CAS NO: | 1427782-89-5 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 472.58 |
|---|---|
| Formula | C25H20N4O2S2 |
| CAS No. | 1427782-89-5 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 25 mg/mL (52.9 mM) |
| Water: <1 mg/mL | |
| Ethanol: <1 mg/mL | |
| Other info | 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 InChi Key: QESQGTFWEQMCMH-UHFFFAOYSA-N InChi Code: InChI=1S/C25H20N4O2S2/c30-22(28-21-12-11-18(15-26-21)17-7-3-1-4-8-17)16-33-25-27-20-13-14-32-23(20)24(31)29(25)19-9-5-2-6-10-19/h1-12,15H,13-14,16H2,(H,26,28,30) SMILES Code: O=C(NC1=NC=C(C2=CC=CC=C2)C=C1)CSC3=NC(CCS4)=C4C(N3C5=CC=CC=C5)=O |
| Synonyms | IWP-L6; PORCN Inhibitor III; Wnt Pathway Inhibitor XIX; IWP L6; IWPL6; Porcn Inhibitor III |
| In Vitro | In vitro activity: IWP-L6 blocks the phosphorylation of the cytoplasmic Wnt pathway effector Dvl2 in HEK293 cells. In cultured embryonic kidneys, IWP-L6 also inhibits Wnt mediated branching morphogenesis by reversibly blocking Wnt signaling. |
|---|---|
| In Vivo | IWP-L6 is stable in human plasma over 24 h, while rapidly metabolized in rat plasma (t1/2 = 190 min), murine plasma (t1/2 = 2 min), and the murine liver S9 fractions. In embryonic zebrafish, IWP-L6 effectively inhibits posterior axis formation, a Wnt/β-catenin dependent developmental process. IWP-L6 (Porcn Inhibitor III) 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 |
| Animal model | Rats |
| Formulation & Dosage | |
| References | J Med Chem. 2013 Mar 28;56(6):2700-4. |
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