Talarozole (R115866)

製品コードE2949

化学情報

	Synonyms	R115866	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C21H23N5S
	分子量	377.51	CAS No.	201410-53-9
Solubility (25°C)*	体外


* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

生物活性

製品説明	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.
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.

製品説明

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.

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.

プロトコル(参考用のみ)

参考

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

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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