Talarozole

Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA) . Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively.

Product Specifications

CAS Number

[201410-53-9]

Product Name Alternative

R115866

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Autophagy; Cytochrome P450; RAR/RXR

Type

Reference compound

Related Pathways

Autophagy; Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/Talarozole.html

Purity

99.75

Solubility

DMSO : 33.33 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C21H23N5S

Molecular Weight

377.51

Precautions

H302, H315, H319, H335

References & Citations

[1]Diaz P, et al. Development and Characterization of Novel and Selective Inhibitors of Cytochrome P450 CYP26A1, theHuman Liver Retinoic Acid Hydroxylase. J Med Chem. 2016 Mar 24;59 (6) :2579-95.|[2]Topletz AR, et al. Induction of CYP26A1 by metabolites of retinoic acid: evidence that CYP26A1 is an important enzyme in theelimination of active retinoids. Mol Pharmacol. 2015;87 (3) :430-41.|[3]Faith Stevison, et al. CYP26 Inhibition Increases Retinoic Acid Concentrations in Target Tissues and Alters Retinoid Signaling|[4]Tripathy S, et al.All-Trans-Retinoic Acid Enhances Mitochondrial Function in Models of Human Liver. Mol Pharmacol. 2016 May;89 (5) :560-74.|[5]Bovenschen HJ, et al. Oral retinoic acid metabolism blocking agent Rambazole for plaque psoriasis: an immunohistochemical study. Br J Dermatol. 2007 Feb;156 (2) :263-70.