DMT1 blocker 2

• CAT Number: I018678
• CAS Number: 1062648-63-8
• Molecular Formula: C16H13N3O
• Molecular Weight: 263.29
• Purity: ≥95%
• Synonyms: 2-pyridin-2-yl-4,5-dihydro-3H-benzo[e]indazol-1-one
• InChI: InChI=1S/C16H13N3O/c20-16-15-12-6-2-1-5-11(12)8-9-13(15)18-19(16)14-7-3-4-10-17-14/h1-7,10,18H,8-9H2
• InChIKey: BKZBNMNLRQXSHY-UHFFFAOYSA-N
• SMILES: C1CC2=C(C3=CC=CC=C31)C(=O)N(N2)C4=CC=CC=N4

DMT1 blocker 2 is a direct inhibitor of divalent metal transporter 1 (DMT1), with an IC50 of 0.83 μM. DMT1 blocker 2 can block iron uptake by enterocytes in vivo[1].
DMT1 blocker 2 (Compound 12f) (10 μM; 24 h) has no cytotoxic to HepG2 cells[1].
DMT1 blocker 2 (10 μM) inhibits 44% of CYP3A4 activity[1].
DMT1 blocker 2 (50 mg/kg; p.o.) blocks iron uptake by enterocytes in an acute rat model of iron hyperabsorption[1].

Reference

[1]. Cadieux JA, et, al. Synthesis and biological evaluation of substituted pyrazoles as blockers of divalent metal transporter 1 (DMT1). Bioorg Med Chem Lett. 2012 Jan 1;22(1):90-5.
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