Home Others CYP450 inhibitor Talarozole (R115866)

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Talarozole (R115866) CYP450 inhibitor

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

Purity & Quality Control

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Mechanism of Action

In Vivo
In vivo

A maximum 84% inhibition of CYP26 activity at 0.5 hours post-dose is predicted based on Talarozole (TLZ) Cmax of 80 nM and a Ki of 1 nM following a single dose of Talarozole. Due to the short Talarozole half-life (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 of Talarozole, 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.

References
  • https://pubmed.ncbi.nlm.nih.gov/10734183/
  • https://www.ncbi.nlm.nih.gov/25492813
  • http://www.fasebj.org/content/30/1_Supplement/934.3
  • https://www.ncbi.nlm.nih.gov/26921399
  • https://www.ncbi.nlm.nih.gov/17223865

Chemical Information

Molecular Weight 377.51 Formula

C21H23N5S
CAS No. 201410-53-9 SDF Download SDF
Synonyms R115866
Smiles CCC(CC)C(C1=CC=C(NC2=NC3=CC=CC=C3S2)C=C1)N4N=CN=C4

Storage and Stability

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