产品说明书

Tavaborole

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Chemical Structure| 174671-46-6 同义名 : AN-2690
CAS号 : 174671-46-6
货号 : A200444
分子式 : C7H6BFO2
纯度 : 98%
分子量 : 151.931
MDL号 : MFCD10699483
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

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
动物实验配方：
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].
实验方案
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
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