Talarozole (R enantiomer)
Modify Date: 2024-01-03 12:36:25
Talarozole (R enantiomer) structure
|
Common Name | Talarozole (R enantiomer) | ||
|---|---|---|---|---|
| CAS Number | 870093-23-5 | Molecular Weight | 377.50600 | |
| Density | 1.26 | Boiling Point | 561.016ºC at 760 mmHg | |
| Molecular Formula | C21H23N5S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 293.092ºC | |
Use of Talarozole (R enantiomer)Talarozole R enantiomer is a potent and selective inhibitor of cytochrome P450 26-mediated breakdown of endogenous all-trans retinoic acid for the treatment of psoriasis and acne.Target: CYP26in vitro: Talarozole R enantiomer treatment increased the mRNA expression of CRABP2, KRT4, CYP26A1 and CYP26B1 dose dependently, and decreased theexpression of KRT2 and IL-1alpha compared with vehicle-treated skin. No mRNA change in retinol-metabolizing enzymes was obtained. There was no induction of epidermal thickness or overt skin inflammation in talarozole-treated skin. Immunofluorescence analysis confirmed an upregulation of KRT4 protein, but no upregulation of CYP26A1 and CYP26B1 expression was detected [1] [2].in vivo: Talarozole R enantiomer slightly diffused into the skin only when dissolved in propylene glycol, isopropyl myristate or ethanol. Although only 0.1% of the dose applied was found in the skin itself after 12-24 h, this was sufficient to achieve local concentrations well above the half-maximal inhibitory concentration value for talarozole. The distribution of talarozole within the skin was investigated: 80% was located in the epidermis, while the remaining 20% was found in the dermis [3]. |
| Name | N-[4-[(1R)-2-ethyl-1-(1,2,4-triazol-1-yl)butyl]phenyl]-1,3-benzothiazol-2-amine |
|---|---|
| Synonym | More Synonyms |
| Description | Talarozole R enantiomer is a potent and selective inhibitor of cytochrome P450 26-mediated breakdown of endogenous all-trans retinoic acid for the treatment of psoriasis and acne.Target: CYP26in vitro: Talarozole R enantiomer treatment increased the mRNA expression of CRABP2, KRT4, CYP26A1 and CYP26B1 dose dependently, and decreased theexpression of KRT2 and IL-1alpha compared with vehicle-treated skin. No mRNA change in retinol-metabolizing enzymes was obtained. There was no induction of epidermal thickness or overt skin inflammation in talarozole-treated skin. Immunofluorescence analysis confirmed an upregulation of KRT4 protein, but no upregulation of CYP26A1 and CYP26B1 expression was detected [1] [2].in vivo: Talarozole R enantiomer slightly diffused into the skin only when dissolved in propylene glycol, isopropyl myristate or ethanol. Although only 0.1% of the dose applied was found in the skin itself after 12-24 h, this was sufficient to achieve local concentrations well above the half-maximal inhibitory concentration value for talarozole. The distribution of talarozole within the skin was investigated: 80% was located in the epidermis, while the remaining 20% was found in the dermis [3]. |
|---|---|
| Related Catalog | |
| References |
| Density | 1.26 |
|---|---|
| Boiling Point | 561.016ºC at 760 mmHg |
| Molecular Formula | C21H23N5S |
| Molecular Weight | 377.50600 |
| Flash Point | 293.092ºC |
| Exact Mass | 377.16700 |
| PSA | 83.87000 |
| LogP | 5.73000 |
| Talarozole (R enantiomer) |