InformationItanapraced (CHF 5074) Itanapraced (CHF 5074, CSP-1103) is a gamma-secretase modulator that reduces Aβ42 and Aβ40 secretion. The IC50s of CHF5074 for inhibition of COX-1 and COX-2 is above 100 μmol/L.Targetsγ secretaseIn vitroIn human neuroglioma cells over-expressing the Swedish mutated APP [human neuroglioma cell line expressing APPswe (H4swe)], CHF5074 preferentially lowers Aβ42 secretion with an IC50 of 3.6 µmol/L. CHF5074 does not display inhibitory activity on COX-1 and COX-2 enzymes when employed at concentrations up to 100 µmol/L and 300 µmol/L respectively.In vivoIn rats, CHF5074 is orally well absorbed (50%) and is slowly eliminated from plasma (t1/2 ≈ 20 h). In Tg2576 transgenic mice, chronic treatment with CHF5074 markedly reduces brain Aβ burden without histological signs of peripheral Notch-mediated toxicity. Specification: 10mM in DMSO Molecular Formula: C16H11Cl2FO2 Molecular Weight: 325.16 PubChem CID: 9996409 Isomeric SMILES: C1CC1(C2=CC(=C(C=C2)C3=CC(=C(C=C3)Cl)Cl)F)C(=O)O
- UPC:
- 12352005
- Condition:
- New
- Availability:
- 2 weeks
- Weight:
- 0.85 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- I425822-1ml
- CAS:
- 749269-83-8
- Product Size:
- 1ml
