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  2. Parasite
  3. GNF179

GNF179 

Cat. No.: HY-15975
Handling Instructions

GNF179 is an optimized 8,8-dimethyl IP analog that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability.

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

GNF179 Chemical Structure

GNF179 Chemical Structure

CAS No. : 1261114-01-5

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Description

GNF179 is an optimized 8,8-dimethyl IP analog that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability. IC50 value: 4.8 nM [1] Target: Anti-parasitic agent GNF179 exhibits a low clearance (CL=22 ml/min/kg, ~25% of hepatic blood flow in mice), a large volume of distribution (steady-state volume of distribution, Vss=11.8 l/kg), a moderate residence time (MRT=9 hours) and suitable terminal half-life (t1/2=8.9 hours). GNF179 reduced Plasmodium berghei parasitemia levels by 99.7% with a single 100 mg/kg oral dose, and prolonged mouse survival by an average of 19 days. GNF179 was able to protect against an infectious P. berghei sporozoite challenge with a single oral dose at 15 mg/kg while NITD609 was not.

Molecular Weight

427.90

Formula

C₂₂H₂₃ClFN₅O

CAS No.

1261114-01-5

SMILES

CC1(C)C2=NC(C3=CC=C(F)C=C3)=C(NC4=CC=C(Cl)C=C4)N2CCN1C(CN)=O

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (292.12 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3370 mL 11.6850 mL 23.3699 mL
5 mM 0.4674 mL 2.3370 mL 4.6740 mL
10 mM 0.2337 mL 1.1685 mL 2.3370 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 (4.86 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.86 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (4.86 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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GNF179
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