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Talarozole

CAT: 0804-HY-14531-01Size: 2 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-14531-01Size:2 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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.
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
CYP26

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