Home Others CYP450 inhibitor Talarozole (R115866)

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Talarozole (R115866) CYP450 inhibitor

Cat.No.E2949

Talarozole (R115866) is a potent, orally active inhibitor of cytochrome P450 (CYP26)-mediated metabolism of All-trans-retinoic acid (RA). It inhibits the conversion of RA by CYP26, with an IC50 of 0.004 µM, and enhances endogenous RA levels and All-trans-retinoic acid receptor (RAR) activation, showing potential as a targeted agent for dermatological therapy.
Talarozole (R115866) CYP450 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 377.51

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Chemical Information, Storage & Stability

Molecular Weight 377.51 Formula

C21H23N5S

 Storage (From the date of receipt)
CAS No. 201410-53-9 Download SDF Storage of Stock Solutions

Synonyms R115866 Smiles CCC(CC)C(C1=CC=C(NC2=NC3=CC=CC=C3S2)C=C1)N4N=CN=C4

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Mechanism of Action

In vivo

Based on a single dose of Talarozole (R115866), a maximum 84% inhibition of CYP26 activity at 0.5 hours post-dose is predicted, using its Cmax of 80 nM and a Ki of 1 nM. Due to the short half-life of this compound (2.2 hrs), CYP26 activity is predicted to return to 100% by 12 hours. In agreement with the predictions, atRA concentrations are increased by 82, 63 and 60% at 4 hours post-dose in the serum, liver and testes, respectively, and concentrations returned to baseline by 24 hours. Following multiple doses, liver CYP26 mRNA and activity are increased suggesting autoinduction of CYP26 due to increased atRA concentrations. In agreement, atRA concentrations are elevated in serum and liver at all timepoints measured. This increase in atRA concentrations is associated with increased mRNA of the mitochondrial biogenesis markers PGC-1β and NRF-1 in comparison to control mice.
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