GNF179
Based on 1 Customer Validation
GNF179 is an optimized 8,8-dimethyl imidazolopiperazine analog that exhibits antimalarial potency (IC50 of 4.8 nM against the multidrug resistant strain W2). GNF179 is orally active.
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- Pureté: 99.78%
- CAS No.: 1261114-01-5
- Formule: C22H23ClFN5O
- Masse moléculaire:427.90
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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Plasmodium |
GNF179 does not rapidly inhibit parasite protein biosynthesis nor is it likely to target parasite cytochrome bc1, which has been validated as a hepatic stage target for Atovaquone (HY-13832). GNF179 may act against sporozoites instead of hepatic stages[1].
GNF179 (5-100 nM; 48 h) shows high inhibition of gametocyte sexual life cycle progression in the mosquito as it abolished oocyst formation at 5 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Naïve Balb/C mice infected with P. berghei[1]
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Dosage:15 mg/kg
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Administration:Oral, single dose
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Result:Protected against an infectious P. berghei sporozoite.
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Animal Model:Naïve Balb/C mice[1]
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Dosage:3 or 20 mg/kg
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Administration:IV or PO (Pharmacokinetic Analysis)
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Result:Pharmacokinetics of GNF179 in naïve Balb/C mice.
Dose AUC(0-∞)
(hrs*µM)AUC/dose t1/2
(hrs)MRT
(hrs)CL
(ml/min/kg)Vss
(L/kg)C0 or Cmax
(µM)F (%) 3 mg/kg i.v. 8.88 3.0 8.9 9.0 22 11.8 6.1 nd 20 mg/kg p.o. 20.70 1.0 8.4 nd nd nd 1.2 58
AUC, Area Under the Curve; T1/2, half life; CL, clearance; VSS, steady-state volume of distribution; C0, initial concentration; Cmax maximum concentration; F, fraction of dose absorbed; hrs, hours; nd, not determined.
Chemical Information
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CAS No. 1261114-01-5
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Appearance Solid
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Masse moléculaire 427.90
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Formule C22H23ClFN5O
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Color Light yellow to yellow
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SMILES
CC1(C)C2=NC(C3=CC=C(F)C=C3)=C(NC4=CC=C(Cl)C=C4)N2CCN1C(CN)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
DMSO : 100 mg/mL (233.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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
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.
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
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 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Meister S, et al. Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery. Science. 2011 Dec 9;334(6061):1372-7. [Content Brief]
[2]. Ouologuem DT, et al. A Novel Ex Vivo Drug Assay for Assessing the Transmission-Blocking Activity of Compounds on Field-Isolated Plasmodium falciparum Gametocytes. Antimicrob Agents Chemother. 2022 Nov 2:e0100122. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3370 mL | 11.6850 mL | 23.3699 mL | 58.4249 mL |
| 5 mM | 0.4674 mL | 2.3370 mL | 4.6740 mL | 11.6850 mL | |
| 10 mM | 0.2337 mL | 1.1685 mL | 2.3370 mL | 5.8425 mL | |
| 15 mM | 0.1558 mL | 0.7790 mL | 1.5580 mL | 3.8950 mL | |
| 20 mM | 0.1168 mL | 0.5842 mL | 1.1685 mL | 2.9212 mL | |
| 25 mM | 0.0935 mL | 0.4674 mL | 0.9348 mL | 2.3370 mL | |
| 30 mM | 0.0779 mL | 0.3895 mL | 0.7790 mL | 1.9475 mL | |
| 40 mM | 0.0584 mL | 0.2921 mL | 0.5842 mL | 1.4606 mL | |
| 50 mM | 0.0467 mL | 0.2337 mL | 0.4674 mL | 1.1685 mL | |
| 60 mM | 0.0389 mL | 0.1947 mL | 0.3895 mL | 0.9737 mL | |
| 80 mM | 0.0292 mL | 0.1461 mL | 0.2921 mL | 0.7303 mL | |
| 100 mM | 0.0234 mL | 0.1168 mL | 0.2337 mL | 0.5842 mL |
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