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CAS No.: 174671-46-6

Tavaborole/他伐硼罗 Catalog No. CSN13870

Synonyms: AN-2690;Kerydin;他伐硼罗

AN-2690 is a broad-spectrum antifungal agent used to treat onychomycosis.

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实验方案

技术信息

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].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00680095	Onychomycosis	Phase 1	Completed	-	United States, Virginia ... more >> The Education and Research Foundation, Inc. Lynchburg, Virginia, United States, 24501 Collapse <<
NCT00679965	Distal, Subungual Onychomycosi... more >>s Collapse <<	Phase 2	Completed	-	Mexico ... more >> Unidad de Investigación en Salud (UIS) Chihuahua, Mexico Hospital "Dr. Angel Leaño" Guadalajara, Mexico Instituto Dermatologico Jalisciense Guadalajara, Mexico Centro Dermatologico Pascua Mexico City, Mexico CIF-BIOTEC Medica Sur. Mexico City, Mexico IMIC Mexico City, Mexico Hospital Universitario Dr. José Eleuterio González Monterrey, Mexico MIRC / OCA Hospital Monterrey, Mexico ISSEMYM Toluca, Mexico Collapse <<
NCT01278394	Onychomycosis	Phase 2	Completed	-	Mexico ... more >> Instituto Dermatologico Jalisciense Guadalajara, Mexico IMIC Mexico City, Mexico Collapse <<

更多
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 6.5819 mL
- 32.9097 mL
- 65.8194 mL
- 5 mM
- 1.3164 mL
- 6.5819 mL
- 13.1639 mL
- 10 mM
- 0.6582 mL
- 3.2910 mL
- 6.5819 mL

技术信息

CAS号

174671-46-6

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C7H6BFO2

运输

蓝冰

分子量

151.93

别名

AN-2690;Kerydin;他伐硼罗

溶解度

DMSO	28.0 mg/mL (184.3 mM)
Water	Insoluble
Ethanol	29.0 mg/mL (190.9 mM)

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT00680095	Onychomycosis	Phase 1	Completed	-	United States, Virginia ... more >> The Education and Research Foundation, Inc. Lynchburg, Virginia, United States, 24501 Collapse <<
NCT00679965	Distal, Subungual Onychomycosi... more >>s Collapse <<	Phase 2	Completed	-	Mexico ... more >> Unidad de Investigación en Salud (UIS) Chihuahua, Mexico Hospital "Dr. Angel Leaño" Guadalajara, Mexico Instituto Dermatologico Jalisciense Guadalajara, Mexico Centro Dermatologico Pascua Mexico City, Mexico CIF-BIOTEC Medica Sur. Mexico City, Mexico IMIC Mexico City, Mexico Hospital Universitario Dr. José Eleuterio González Monterrey, Mexico MIRC / OCA Hospital Monterrey, Mexico ISSEMYM Toluca, Mexico Collapse <<
NCT01278394	Onychomycosis	Phase 2	Completed	-	Mexico ... more >> Instituto Dermatologico Jalisciense Guadalajara, Mexico IMIC Mexico City, Mexico Collapse <<
NCT00679523	Onychomycosis	Phase 2	Completed	-	Mexico ... more >> Unidad de Investigación en Salud (UIS) Chihuahua, Mexico Hospital "Dr. Angel Leaño" Guadalajara, Mexico Instituto Dermatologico Jalisciense Guadalajara, Mexico Centro Dermatologico Pascua Mexico City, Mexico CIF-BIOTEC Medica Sur. Mexico City, Mexico IMIC Mexico City, Mexico Hospital Universitario Dr. José Eleuterio González Monterrey, Mexico MIRC / OCA Hospital Monterrey, Mexico ISSEMYM Toluca, Mexico Collapse <<
NCT01278394	-	-	Completed	-	-
NCT03405818	-	-	Completed	-	-
NCT00680160	Onychomycosis	Phase 2	Completed	-	United States, Texas ... more >> J&S Studies Bryan, Texas, United States, 77802 Collapse <<
NCT00680134	Onychomycosis	Phase 2	Completed	-	United States, Alabama ... more >> University of Alabama at Birmingham Birmingham, Alabama, United States, 35233 United States, California University of California, San Francisco San Francisco, California, United States, 94143-0517 United States, New Mexico Academic Dermatology Associates Albuquerque, New Mexico, United States, 87106 United States, New York Columbia University Medical Center New York, New York, United States, 10032 United States, Texas DermResearch, Inc. Austin, Texas, United States, 78759 J&S Studies Bryan, Texas, United States, 77802 Endeavor Clinical Trials, PA & San Antonio Podiatry Associates, PC San Antonio, Texas, United States, 78229 Collapse <<
NCT00679601	Onychomycosis	Phase 2	Completed	-	United States, Texas ... more >> J&S Studies Bryan, Texas, United States, 77802 Collapse <<
NCT00679770	Distal, Subungual Onychomycosi... more >>s Collapse <<	Phase 2	Completed	-	United States, New Mexico ... more >> Academic Dermatology Associates Albuquerque, New Mexico, United States, 87106 United States, Texas DermResearch, Inc. Austin, Texas, United States, 78759 J&S Studies Bryan, Texas, United States, 77802 Endeavor Clinical Trials, PA & San Antonio Podiatry Associates, PC San Antonio, Texas, United States, 78229 Collapse <<
NCT01270971	Onychomycosis of Toenails	Phase 3	Completed	-	-
NCT01302119	Onychomycosis of Toenails	Phase 3	Completed	-	-
NCT03405818	Onychomycosis ... more >> Tinea Unguium Collapse <<	Phase 4	Completed	-	United States, California ... more >> Madera Family Medical Group Madera, California, United States, 93637 Stanford University School of Medicine Palo Alto, California, United States, 94304 United States, District of Columbia MedStar Health Research Institute - MedStar Georgetown University Hospital Washington, District of Columbia, United States, 20016 United States, Florida Doctors Research Network South Miami, Florida, United States, 33143 United States, New York University Hospital, SUNY Downstate Medical Center Brooklyn, New York, United States, 11203 Skin Specialty Dermatology New York, New York, United States, 10155 United States, Oregon Cyn3rgy Research Gresham, Oregon, United States, 97030 Oregon Dermatology & Research Center Portland, Oregon, United States, 97210 United States, Texas West Houston Clinical Research Services LLC Houston, Texas, United States, 77055 Texas Dermatology and Laser Specialists San Antonio, Texas, United States, 78218 United States, Utah Jordan Valley Dermatology Center West Jordan, Utah, United States, 84088 United States, Virginia PI Coor Clinical Research, LLC Burke, Virginia, United States, 22015 Collapse <<
NCT01270971	-	-	Completed	-	-
NCT01302119	-	-	Completed	-	-

Tavaborole/他伐硼罗 Catalog No. CSN13870

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