ARN1468

• CAT Number: I043336
• CAS Number: 1381459-14-8
• Molecular Formula: C16H17F3N4O2
• Molecular Weight: 354.33
• Purity: ≥95%
• Synonyms: [5-amino-1-[4-(trifluoromethoxy)phenyl]pyrazol-4-yl]-piperidin-4-ylmethanone
• InChI: InChI=1S/C16H17F3N4O2/c17-16(18,19)25-12-3-1-11(2-4-12)23-15(20)13(9-22-23)14(24)10-5-7-21-8-6-10/h1-4,9-10,21H,5-8,20H2
• InChIKey: OOUGXIZAHWLQEM-UHFFFAOYSA-N
• SMILES: C1CNCCC1C(=O)C2=C(N(N=C2)C3=CC=C(C=C3)OC(F)(F)F)N

ARN1468 (compound 5) is an orally active and potent serpins inhibitor. ARN1468 can inhibit serpins activity would set the protease free to further reduce prion accumulation. ARN1468 shows anti-prion effect in ScGT1 RML, ScGT1 22L, ScN2a RML, and ScN2a 22L cell lines, with EC50 values of 8.64, 19.3, 11.2, and 6.27 μM[1].
ARN1468 (compound 5) (3 mg/kg, IV; 10 mg/kg, PO; once) reveals low brain concentrations and high plasma clearance in male C57BL/6 mice[1].

Reference

[1]. Colini Baldeschi A, et al. Innovative Non-PrP-Targeted Drug Strategy Designed to Enhance Prion Clearance. J Med Chem. 2022 Jun 30.
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