NP213 TFA

NP213 TFA; 纯度: 96.22%

NP213 TFA 是一种快速、新颖、的合成抗菌肽 (AMP),具有抗真菌 (anti-fungal) 活性。NP213 TFA 以真菌胞质膜为靶点,通过对膜的扰动和破坏发挥作用。NP213 对甲真菌感染有效且耐受性好。

NP213 TFAamp;;

NP213 TFA Chemical Structure

规格 价格 是否有货 数量
10;mM;*;1 mL in DMSO ¥5710 In-stock
5 mg ¥2700 In-stock
10 mg ¥4300 In-stock
25 mg ¥7600 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

NP213 TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Infection Compound Library
  • Antifungal Compound Library
  • Peptide Library

生物活性

NP213 TFA is a rapidly acting, novel, first-in-class synthetic antimicrobial peptide (AMP), has anti-fungal activities. NP213 TFA targets the fungal cytoplasmic membrane and plays it role via membrane perturbation and disruption. NP213 TFA is effective and well-tolerated in resolving nail fungal infections[1][2].

IC50 Target

IC50: fungal[1]

体外研究
(In Vitro)

NP213 (500-1000 μg/mL; 18 hours) increases the number of PI-stained T. rubrum NCPF0118 cells in samples. This results suggests that NP213 is fungicidal and the mechanisms of action involved membrane permeabilization[1].
NP213 is against T. rubrum NCPF0118, shows different MIC values against T. rubrum NCPF0118, and the MICs varies depending on the source of the keratin. The MIC values are 16-32 mg/L, 125 mg/L, and 250 mg/L for NP213 in 1640 media containing human nail Keratin, human skin Keratin and Lamb’s wool Keratin, respectively[1].NP213 TFA (2-3 hours; 0-8 μg/ml) has great activity against clinically relevant yeast, including candida spp, Cryptococcus spp and Trichosporon spp. For all 122 yeast isolates, with the median MIC100 values of 1-2 µg/ml[3].

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

Cell Cytotoxicity Assay[3]

Cell Line: Clinically relevant yeast isolates
Concentration: 0 μg/ml; 0.125 μg/ml; 0.25 μg/ml; 0.5 μg/ml; 1 μg/ml; 2 μg/ml; 4 μg/ml; 8 μg/ml
Incubation Time: 2 h, 2.5 h, 4 h
Result: Decreased isolates growth as a dose-dependent manner.

体内研究
(In Vivo)

NP213 TFA (25 mg/kg) is well tolerated in mice. In Murine models of acute disseminated candidiasis, NP213 is tolerated and efficacious and exhibits a half-life of approximately 4.5 h[3].

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

分子量

1207.32

Formula

C44H85F3N28O9

Sequence

Cyclo-Arg-Arg-Arg-Arg-Arg-Arg-Arg

Sequence Shortening

Cyclo-RRRRRRR

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Protect from light, stored under nitrogen

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (protect from light, stored under nitrogen)

溶解性数据
In Vitro:;

H2O : 100 mg/mL (82.83 mM; Need ultrasonic)

DMSO : 100 mg/mL (82.83 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.8283 mL 4.1414 mL 8.2828 mL
5 mM 0.1657 mL 0.8283 mL 1.6566 mL
10 mM 0.0828 mL 0.4141 mL 0.8283 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,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 (protect from light, stored under nitrogen)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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.

    请依序添加每种溶剂:;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.5 mg/mL (2.07 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.07 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 ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂:;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (2.07 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.07 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
  • 3.

    请依序添加每种溶剂:;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.5 mg/mL (2.07 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.07 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。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
  • [1]. Mercer DK,et al. Improved Methods for Assessing Therapeutic Potential of Antifungal Agents against Dermatophytes and Their Application in the Development of NP213, a Novel Onychomycosis Therapy Candidate.Antimicrob Agents Chemother. 2019 Apr 25;63(5). pii: e02117-18.

    [2]. Neelabh, et al. Sequential and Structural Aspects of Antifungal Peptides from Animals, Bacteria and Fungi Based on Bioinformatics Tools.Probiotics Antimicrob Proteins. 2016 Jun;8(2):85-101.

    [3]. Novamycin®/NP339 Technology Summary