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Terbinafine HCl.
有效的非竞争性角鲨烯环氧酶抑制剂,Terbinafine hydrochloride (TDT 067 hydrochloride) 是治疗真菌感染的抗真菌药物。它是来自念珠菌属的角鲨烯环氧化酶有效的非竞争性抑制剂, Ki值为30 nM。
目录号: PC14948 纯度: ≥98%
CAS No. :78628-80-5
商品编号 规格 价格 会员价 是否有货 数量
PC14948-100mg 100mg ¥490.00 请登录
PC14948-200mg 200mg ¥833.00 请登录
PC14948-10mM (in 1mL DMSO) 10mM (in 1mL DMSO) ¥784.00 请登录
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中文名称
Terbinafine HCl.
中文别名
盐酸特比萘芬;(E)-N-(6,6-二甲基-2-庚烯-4-炔基)-N-甲基-1-萘甲胺盐酸盐;特比萘芬盐酸盐;特比萘芬;特比萘酚;盐酸特比萘酚;特拉萘芬盐酸盐;反-N-(6,6-二甲基-2-庚烯-4-炔基)-N-甲基-1-萘基甲胺盐酸盐;(E)-N-(6,6-二甲基-2-庚烯-4-炔;二氨甲基环己基甲烷;反-N-(6,6-二甲基-2-庚-4-炔基)-N-甲基-1-萘基甲胺盐酸盐;甲氧苄啶;萘甲胺盐酸盐;特比萘芬 盐酸特比萘芬;特比萘芬系统适应性 EP标准品;特比萘芬盐酸盐 标准品;特比萘芬盐酸盐及其杂质标准品;盐酸特比奈芬;盐酸特比奈酚;盐酸特比萘fen;盐酸特比萘芬 EP标准品;盐酸特比萘芬 USP标准品;盐酸特比萘芬TERBINAFINE HYDROCHLORIDE;盐酸特比萘芬TERBINAFINE HYDROCHLORIDE78628;盐酸特比萘酚 标准品;(E)-N-(6,6-二甲基庚-2- 烯-4-炔基)-N-甲基-1-萘甲胺盐酸盐;特比奈酚;特比萘芬,盐酸D5;特比萘芬,盐酸D7;特比萘酚盐酸盐;植物组织果糖含量测试盒;trans-N-(6,6-Dimethyl-2-hepten-4-ylyl)-N-methyl-1-naphthylmethylamine 盐酸盐;(E)-N,6,6-三甲基-N-(萘-1-基甲基)庚-2-烯-4-炔-1-胺盐酸盐;盐酸特比萘芬,医药级,纯度:>99%;(E)-N-(6,6-二甲基庚-2-烯-4-炔基)-N-甲基-1-萘甲胺盐酸盐
英文名称
Terbinafine HCl
英文别名
TERBINAFINE HYDROCHLORIDE;(e)-n-(6,6-dimethyl-2-hepten-4-ynyl)-n-methyl-1-naphthalenemethanamine monohydrochloride;(E)-N-(6,6-DIMETHYL-2-HEPTEN-4-YNYL)-N-METHYL-1-NAPHTHYLMETHYLAMINE HYDROCHLORIDE;LAMISIL;N-[(2E)-6,6-DIMETHYL-2-HEPTEN-4-YNYL]-N-METHYL-1-NAPHTHALENEMETHANAMINE;n,6,6-trimethyl-n-(naphthalen-1-ylmethyl)hept-2-en-4-yn-1-amine hydrochloride;TERBINAFINE HCL;TRANS-N-(6,6-DIMETHYL-2-HEPTEN-4-YNYL)-N-METHYL-1-NAPHTHYLMETHYLAMINE HYDROCHLORIDE;(e)-n-(6,6-dimethyl-2-hepten-4-ynyl)-n-methyl-1-naphthalenemethylaminehydroc;lamosil;n-(6,6-dimethyl-2-hepten-4-ynyl)-n-methyl-1-naphthalenemethanamin(e)-1-naphthalenemethanaminmon;n-(6,6-dimethyl-2-hepten-4-ynyl)-n-methyl-1-naphthalenemethanamin(e)-1-naphthalenemethanaminmonohydrochloride;TerbutalineSulfateBase;Lamisil, N-[(2E)-6,6-Dimethyl-2-hepten-4-ynyl]-N-methyl-1-naphthalenemethanamine;1-Naphthalenemethanamine, N-(2E)-6,6-dimethyl-2-hepten-4-ynyl-N-methyl-, hydrochloride;TERNBINAFINEHCL;({[(2E)-6,6-Dimethylhept-2-en-4-yn-1-yl](methyl)amino}methyl)naphthalene hydrochloride;Trebinafine hydrochloride;1-(3,5-Dihydroxyphenyl)-2-(tert-butylamino)ethanol;Terbutaline;N,6,6-Trimethyl-N-(1-naphthylmethyl)hept-2-en-4-yn-1-amine hydrochloride;TERBINAFINE;Terbinafine (hydrochloride);Terbinafine Hydrochl;terbinafine hydrochloride;Terbinafine Hydrochioride;trans-N-(6,6-Dimethyl-2-hepten-4-ylyl)-N-methyl-1-naphthylmethylamine hydrochloride;(E)-N,6,6-Trimethyl-N-(naphthalen-1-ylmethyl)hept-2-en-4-yn-1-amine Hydrochloride;[ "" ];Lamisil Krem;Lamisil AT;Terbinafinum [Latin];Terbinafina [Spanish];MycoVa;Terbinafinum;Terbinafina;Zabel;CPD000469152;012C11ZU6G;(E)-N-(6,6-Dimethyl-2-hepten-4-ynyl)-N-methyl-1-naphthalenemethylamine hydrochloride;C21H26ClN;Terbinafine h
Cas No.
78628-80-5
分子式
C21H26ClN
分子量
327.89
包装储存

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Terbinafine hydrochloride (TDT 067 hydrochloride) is an orally active and potent antifungal agent. Terbinafine hydrochloride is a potent non-competitive inhibitor of squalene epoxidase from Candida, with a Ki of 30 nM. Terbinafine hydrochloride also shows antibacterial activity against certain Gram-positive and Gram-negative bacteria.

性状

Solid

IC50 & Target[1][2]

Ki: 30 nM (squalene epoxidase)

体外研究(In Vitro)

Terbinafine has a primary fungicidal action 体外研究 against most fungal pathogens, including dermatophytes, and dimorphic and filamentous fungi. Terbinafine specifically inhibits fungal ergosterol biosynthesis at the point of squalene epoxidation. The treated fungal cells rapidly accumulate tlic intermediate squalene and become deficient in the end-product of the pathway, ergosterol.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Terbinafine is not only active after topical application but is very effective in experimental dermatophytoses following oral administration. In fungi infected guinea-pigs, the skin temperature dropps dramatically after the fourth treatment of terbinafine.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial
参考文献
溶解度数据
体外研究: 

DMSO : 60 mg/mL (182.99 mM; Need ultrasonic)

H2O : 1 mg/mL (3.05 mM; ultrasonic and warming and heat to 60°C)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0498 mL 15.2490 mL 30.4980 mL
5 mM 0.6100 mL 3.0498 mL 6.0996 mL
10 mM 0.3050 mL 1.5249 mL 3.0498 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    建议依照次序添加每种溶剂: 0.5% CMC-Na/saline water

    Solubility: 13.75 mg/mL (41.93 mM); Suspended solution; Need ultrasonic

  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.62 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.62 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 3.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.62 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.62 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.62 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.62 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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