Talarozole

Name: Talarozole
Brand: TargetMol
SKU: T7370
Price: 497 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 97.51%

货号 T7370Cas号 201410-53-9

别名 他拉罗唑, R115866

Talarozole (R115866) 是一种口服性全反式维甲酸代谢阻断剂，可抑制 CYP26A1 和 CYP26B1，IC50 分别为 5.4 和 0.46 nM。它用于治疗痤疮、牛皮癣和其他角化疾病。

Talarozole

一键复制产品信息

很棒

纯度: 97.51%

货号 T7370 别名 他拉罗唑, R115866Cas号 201410-53-9

Talarozole (R115866) 是一种口服性全反式维甲酸代谢阻断剂，可抑制 CYP26A1 和 CYP26B1，IC50 分别为 5.4 和 0.46 nM。它用于治疗痤疮、牛皮癣和其他角化疾病。

规格	价格	库存
1 mg	¥ 497	现货
5 mg	¥ 1,070	现货
10 mg	¥ 1,490	现货
25 mg	¥ 2,420	现货
50 mg	¥ 3,480	现货
100 mg	¥ 4,890	现货
200 mg	¥ 6,780	5日内发货
1 mL x 10 mM (in DMSO)	¥ 893	现货

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COA HNMR LCMS 产品操作手册

产品介绍

Talarozole AI Summary

Talarozole shows potent inhibition of human CYP26B1 and CYP26A1 enzymes, with IC50 values of 0.46 nM and 5.1 nM, respectively, and effectively inhibits the metabolism of 9-cis-RA, as indicated by HPLC analyses in the presence of rat P450 reductase. This suggests its potential as a CYP26 inhibitor with implications for retinoic acid metabolism. Additionally, Talarozole exhibits antiviral activity against SARS-CoV-2 by inhibiting virus-induced cytotoxicity in both Caco-2 cells and VERO-6 cells at a concentration of 10 µM, though the inhibition rates varied across different assays and conditions. It inhibits SARS-CoV-2 3CL-Pro protease at 20 µM with inhibition rates reported between -0.02% and 20.95%. Despite varying IC50 values, some assays indicated values greater than 20,000 nM. The compound also shows inhibitory activity against human HDAC6 with inhibition percentages of 11.88% and 23.24% in enzymatic assays using different substrates, suggesting potential as an HDAC6 inhibitor. Talarozole additionally demonstrates cytotoxicity against human HepG2 cells, with an IC50 value of 14400 nM as assessed by the CellTiter-Glo luminescent cell viability assay..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively.Talarozole for the treatment of acne, psoriasis and other keratinization disorders.
靶点活性	CYP26B1/A1:0.46/5.1 nM (IC50)
别名	他拉罗唑, R115866

化学信息

分子量	377.51
分子式	C₂₁H₂₃N₅S
CAS No.	201410-53-9
Smiles	CCC(CC)C(c1ccc(Nc2nc3ccccc3s2)cc1)n1cncn1
密度	1.26 g/cm3 (Predicted)
颜色	White
物理性状	Solid

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 36 mg/mL (95.36 mM), Sonication is recommended.

体内实验配方

10% DMSO+90% Corn Oil: 2 mg/mL (5.3 mM), Sonication is recommeded.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6489 mL	13.2447 mL	26.4894 mL	132.4468 mL
5 mM	0.5298 mL	2.6489 mL	5.2979 mL	26.4894 mL
10 mM	0.2649 mL	1.3245 mL	2.6489 mL	13.2447 mL
20 mM	0.1324 mL	0.6622 mL	1.3245 mL	6.6223 mL
50 mM	0.0530 mL	0.2649 mL	0.5298 mL	2.6489 mL