LysRs-IN-2|cas:2170696-76-9|西域试剂

LysRs-IN-2,99.92%

产品编号：Bellancom-126130| CAS NO：2170696-76-9| 分子式：C₁₇H₁₆F₃NO₄| 分子量：355.31

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货号	价格	库存与货期
Bellancom-126130	￥1400.00	杭州北京（现货）
Bellancom-126130	￥4100.00	杭州北京（现货）
Bellancom-126130	￥6500.00	杭州北京（现货）

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LysRs-IN-2

产品介绍

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。

生物活性

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.

体外研究

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).

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

体内研究

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).

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

Animal Model:	Murine P. falciparum NODscidIL2Rγnull (SCID) model
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)
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.

体内研究

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

Animal Model:	Murine P. falciparum NODscidIL2Rγnull (SCID) model
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)
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 60 mg/mL (168.87 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	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，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: ≥ 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: ≥ 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。