Talarozole
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Talarozole是细胞色素P450的选择性抑制剂，IC50值为4 nM[1]。
在外部和内部环境中，细胞色素P450参与许多结构多样的有机化学物质的氧化代谢。细胞色素P450催化的反应具有多样性，作用底物的范围较广。
Talarozole是细胞色素P450介导的内源性全反视黄酸分解的选择性抑制剂，用于治疗皮癣和痤疮。Talarozole可以增加CRABP2、KRT4、CYP26A1和CYP26B1 mRNA的表达，与此同时，与对照处理的皮肤相比，降低KRT2和IL-1α的表达，视黄醇代谢酶的mRNA没有发生改变。在talarozole治疗的皮肤中，没有表皮增厚或明显的皮肤炎症。免疫荧光分析证实了KRT4蛋白的上调，但是， CYP26B1和CYP26A1的表达没有上调[1,2]。
12-24小时后，皮肤中仍有0.1％的剂量残留。80％的talarozole分布在皮肤的表皮层，剩余的20％是在真皮层中[3]。
参考文献：
[1] Pavez Loriè E, Cools M, Borgers M, Topical treatment with CYP26 inhibitor talarozole (R115866) dose dependently alters the expression of retinoid-regulated genes in normal human epidermis.The British Journal of Dermatology,2009,160(1):26-36.
[2] Geria AN, Scheinfeld NS.Talarozole, a selective inhibitor of P450-mediated all-trans retinoic acid for the treatment of psoriasis and acne. Current Opinion In Investigational Drugs,2008 ,9(11):1228-1237.
[3] Baert B, De Spiegeleer B.Local skin pharmacokinetics of talarozole, a new retinoic acid metabolism-blocking agent. Skin Pharmacol Physiol,2011,24(3):151-159
| Storage | Store at -20°C |
| M.Wt | 377.51 |
| Cas No. | 201410-53-9 |
| Formula | C21H23N5S |
| Synonyms | Rambazole;R115866;R-115866;R 115866 |
| Solubility | ≥48 mg/mL in DMSO; ≥9.34 mg/mL in EtOH; insoluble in H2O |
| Chemical Name | N-[4-[2-ethyl-1-(1,2,4-triazol-1-yl)butyl]phenyl]-1,3-benzothiazol-2-amine |
| SDF | Download SDF |
| Canonical SMILES | CCC(CC)C(C1=CC=C(C=C1)NC2=NC3=CC=CC=C3S2)N4C=NC=N4 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 描述 | Talarozole是细胞色素P450的有效选择性抑制剂。 | |||||
| 靶点 | cytochrome P450 | |||||
| IC50 | ||||||
质量控制和MSDS
- 批次:
化学结构
