PeptideDB

DMT1 blocker 2

CAS: 1062648-63-8 F: C16H13N3O W: 263.29

DMT1 blocker 2 is a direct inhibitor of divalent metal transporter 1 (DMT1), with an IC50 of 0.83 μM. DMT1 blocker 2 ca
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Bioactivity 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].
Target IC50: 0.83 μM (divalent metal transporter 1)
Invitro 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].
In Vivo DMT1 blocker 2 (50 mg/kg; p.o.) blocks iron uptake by enterocytes in an acute rat model of iron hyperabsorption[1]. Animal Model:
Name DMT1 blocker 2
CAS 1062648-63-8
Formula C16H13N3O
Molar Mass 263.29
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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.