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Tavaborole/他伐硼罗 {[allProObj[0].p_purity_real_show]}

货号:A200444 同义名: AN-2690

Tavaborole是一种广谱抗真菌药物,用于治疗甲癣(指甲真菌感染)。

Tavaborole/他伐硼罗 化学结构 CAS号:174671-46-6
Tavaborole/他伐硼罗 化学结构
CAS号:174671-46-6
Tavaborole/他伐硼罗 3D分子结构
CAS号:174671-46-6
Tavaborole/他伐硼罗 化学结构 CAS号:174671-46-6
Tavaborole/他伐硼罗 3D分子结构 CAS号:174671-46-6
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Tavaborole/他伐硼罗 纯度/质量文件 产品仅供科研

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Tavaborole/他伐硼罗 生物活性

描述 AN-2690 (Tavaborole) is an antifungal agent with activity against Trichophyton species, in a topical solution formulation for the potential treatment of onychomycosis. Tavaborole has a unique mechanism of action against fungal organisms and retains antifungal properties in the presence of keratin[3]. The low molecular weight, slight water solubility, and boron chemistry of tavaborole maximize nail penetration after topical application, allowing for effective targeting of the infection in the nail bed. The efficacy of tavaborole is associated with its novel mechanism of action, whereby it inhibits the fungal leucyl-tRNA synthetase (LeuRS) enzyme. Because LeuRS is an essential component in fungal protein synthesis, inhibition of LeuRS ultimately leads to fungal cell death[4]. The CP1 (connective peptide 1) domain of LeuRS (leucyl-tRNA synthetase) contains the editing active site, which is the proven target for the broad-spectrum drug AN2690. GlLeuRS (Giardia lamblia LeuRS) was completely resistant to the AN2690, which is an inhibitor of various LeuRSs[1].

Tavaborole/他伐硼罗 参考文献

[1]Zhou XL, Tan M, Wang M, Chen X, Wang ED. Post-transfer editing by a eukaryotic leucyl-tRNA synthetase resistant to the broad-spectrum drug AN2690. Biochem J. 2010;430(2):325‐333

[2]Baker SJ, Zhang YK, et al. Discovery of a new boron-containing antifungal agent, 5-fluoro-1,3-dihydro-1-hydroxy-2,1- benzoxaborole (AN2690), for the potential treatment of onychomycosis. J Med Chem. 2006 Jul 27;49(15):4447-50.

[3]Gupta AK, Daigle D. Tavaborole (AN-2690) for the treatment of onychomycosis of the toenail in adults. Expert Rev Anti Infect Ther. 2014;12(7):735‐742

[4]Markinson B, Ghannoum M, Winter T, Rycerz A, Rock F, Gupta AK. Examining the Benefits of the Boron-Based Mechanism of Action and Physicochemical Properties of Tavaborole in the Treatment of Onychomycosis. J Am Podiatr Med Assoc. 2018;108(1):12‐19

Tavaborole/他伐硼罗 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

6.58mL

1.32mL

0.66mL

32.91mL

6.58mL

3.29mL

65.82mL

13.16mL

6.58mL

Tavaborole/他伐硼罗 技术信息

CAS号174671-46-6
分子式C7H6BFO2
分子量 151.93
SMILES Code OB1OCC2=CC(F)=CC=C12
MDL No. MFCD10699483
别名 AN-2690
运输蓝冰
InChI Key LFQDNHWZDQTITF-UHFFFAOYSA-N
Pubchem ID 11499245
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, store in freezer, under -20°C

溶解方案

DMSO: 105 mg/mL(691.1 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

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