1. Metabolic Enzyme/Protease
  2. Aminoacyl-tRNA Synthetase
  3. LysRs-IN-2

LysRs-IN-2 

目录号: HY-126130 纯度: 98.69%
产品使用指南

LysRs-IN-2 是一种赖氨酸 tRNA 合成酶 (KRS) 抑制剂,其对恶性疟原虫 KRS (PfKRS) 和小隐孢子虫 KRS (CpKRS) 的 IC50 值分别为 0.015 μM、0.13 μM。

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LysRs-IN-2 Chemical Structure

LysRs-IN-2 Chemical Structure

CAS No. : 2170696-76-9

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Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥7660 In-stock
1 mg ¥5500 In-stock
5 mg ¥9800 In-stock
10 mg ¥15000 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Description

LysRs-IN-2 is a lysyl-tRNA synthetase (KRS) inhibitor with IC50s of 0.015 μM and 0.13 μM for Plasmodium falciparum lysyl-tRNA synthetase (PfKRS) and Cryptosporidium parvum lysyl-tRNA synthetase (CpKRS), respectively[1].

IC50 & Target

IC50: 0.015 μM (PfKRS), 0.13 μM (CpKRS)[1]

In Vitro

LysRs-IN-2 is active against whole-cell bloodstream P. falciparum 3D7 (EC50=0.27 μM), HsKRS (IC50=1.8 μM), HepG2 cells (EC50=49 μM), and Cryptosporidium parvum (EC50=2.5 µM)[1].

In Vivo

LysRs-IN-2 (1.5 mg/kg; orally once a day for 4 days) reduces parasitemia by 90% in the murine P. falciparum SCID model. LysRs-IN-2 (20 mg/kg; orally once a day for 7 days) reduces parasite shedding in NOD SCID gamma mice and INF-γ-knockout mice (Cryptosporidium mouse models)[1].

Animal Model: Murine P. falciparum NODscidIL2Rγnull (SCID) model[1]
Dosage: 1.5 mg/kg
Administration: Orally once a day for 4 days
Result: Reduced parasitemia by 90% in the malaria SCID mouse model.
Animal Model: NOD SCID gamma and INF-γ–knockout mouse models (Cryptosporidium mouse models)[1]
Dosage: 20 mg/kg
Administration: Orally once a day for 7 days
Result: Reduced parasite shedding below detection level, and this reduction was sustained for 3 wk after treatment had stopped in INF-γ-knockout mice. Dosed orally at a concentration of 20 mg/kg once a day for 7 days showed 96% reduction of parasite shedding comparable to paromomycin in NOD SCID gamma mice.
Molecular Weight

355.31

Formula

C₁₇H₁₆F₃NO₄

CAS No.

2170696-76-9

SMILES

FC1=CC=C(OC(C(NCC2(O)CCC(F)(F)CC2)=O)=CC3=O)C3=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 60 mg/mL (168.87 mM)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8144 mL 14.0722 mL 28.1444 mL
5 mM 0.5629 mL 2.8144 mL 5.6289 mL
10 mM 0.2814 mL 1.4072 mL 2.8144 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 (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: ≥ 2.08 mg/mL (5.85 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.85 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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,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: ≥ 1.5 mg/mL (4.22 mM); Clear solution

    此方案可获得 ≥ 1.5 mg/mL (4.22 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 15.0 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,再用生理盐水定溶至 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: ≥ 1.5 mg/mL (4.22 mM); Clear solution

    此方案可获得 ≥ 1.5 mg/mL (4.22 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 15.0 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。
References

Purity: 98.69%

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Keywords:

LysRs-IN-2Aminoacyl-tRNA SynthetasetRNA Synthetase, aaRSInhibitorinhibitorinhibit

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产品名称:
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目录号:
HY-126130
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