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 |
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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. |