LysRs-IN-2

Name: LysRs-IN-2
Brand: MedChemExpress
SKU: HY-126130
Rating: 4.5 (1 reviews)

Cat. No.: HY-126130 Purity: 99.92%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

LysRs-IN-2 Chemical Structure

CAS No. : 2170696-76-9

Size	Price	Stock	Quantity
5 mg	USD 410	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 650	In-stock	Estimated Time of Arrival: December 31
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100 mg		Get quote

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Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE LysRs-IN-2

•bioRxiv. 2023 Dec 7.

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Description

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].

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

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].

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

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

Appearance

Solid

Color

White to off-white

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.5 mg/mL (4.22 mM); Clear solution

This protocol yields a clear solution of ≥ 1.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (15.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.5 mg/mL (4.22 mM); Clear solution

This protocol yields a clear solution of ≥ 1.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (15.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.92%

Select Batch:

Data Sheet (273 KB) SDS (252 KB)

COA (245 KB) LCMS (266 KB)

Handling Instructions (2659 KB)

References

[1]. Baragaña B, et al. Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis. Proc Natl Acad Sci U S A. 2019 Apr 2;116(14):7015-7020. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.8144 mL	14.0722 mL	28.1444 mL	70.3611 mL
	5 mM	0.5629 mL	2.8144 mL	5.6289 mL	14.0722 mL
	10 mM	0.2814 mL	1.4072 mL	2.8144 mL	7.0361 mL
	15 mM	0.1876 mL	0.9381 mL	1.8763 mL	4.6907 mL
	20 mM	0.1407 mL	0.7036 mL	1.4072 mL	3.5181 mL
	25 mM	0.1126 mL	0.5629 mL	1.1258 mL	2.8144 mL
	30 mM	0.0938 mL	0.4691 mL	0.9381 mL	2.3454 mL
	40 mM	0.0704 mL	0.3518 mL	0.7036 mL	1.7590 mL
	50 mM	0.0563 mL	0.2814 mL	0.5629 mL	1.4072 mL
	60 mM	0.0469 mL	0.2345 mL	0.4691 mL	1.1727 mL
	80 mM	0.0352 mL	0.1759 mL	0.3518 mL	0.8795 mL
	100 mM	0.0281 mL	0.1407 mL	0.2814 mL	0.7036 mL

LysRs-IN-2 Related Classifications

Infection

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LysRs-IN-22170696-76-9Aminoacyl-tRNA SynthetasetRNA Synthetase, aaRSInhibitorinhibitorinhibit

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LysRs-IN-2

Customer Review

LysRs-IN-2 Related Antibodies

1 Publications Citing Use of MCE LysRs-IN-2

Featured Recommendations

•Related Screening Libraries:

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•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

LysRs-IN-2 Related Antibodies

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Complete Stock Solution Preparation Table

LysRs-IN-2 Related Classifications

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