[CAS NO. 2170696-76-9]  LysRs-IN-2

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PRODUCTS SPECIFICATIONS [2170696-76-9]

Catalog
HY-126130
Brand
MCE
CAS
2170696-76-9

DESCRIPTION [2170696-76-9]

Overview

MDL-
Molecular Weight355.31
Molecular FormulaC17H16F3NO4
SMILESFC1=CC=C(OC(C(NCC2(O)CCC(F)(F)CC2)=O)=CC3=O)C3=C1

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

Summary

LysRs-IN-2 is a lysyl-tRNA synthetase (KRS) inhibitor with IC 50 s of 0.015 μM and 0.13 μM for Plasmodium falciparum lysyl-tRNA synthetase ( Pf KRS) and Cryptosporidium parvum lysyl-tRNA synthetase ( Cp KRS), respectively [1] .


IC50 & Target

IC50: 0.015 μM ( Pf KRS), 0.13 μM ( Cp KRS) [1]


In Vitro

LysRs-IN-2 is active against whole-cell bloodstream P. falciparum 3D7 (EC 50 =0.27 μM), Hs KRS (IC 50 =1.8 μM), HepG2 cells (EC 50 =49 μM), and Cryptosporidium parvum (EC 50 =2.5 µM) [1] .

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] .

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.

Appearance

Solid


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
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 1.5 mg/mL (4.22 mM); Clear solution

* All of the co-solvents are available by MCE.