| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
The primary biological target of GNF179 metabolite is not fully characterized, but it is believed to share the mechanism of action of the parent drug. GNF179 is an 8,8-dimethyl IP analog that targets the parasite's phosphatidylinositol 4-kinase (PI4K) or a related enzyme involved in phospholipid metabolism. This disrupts intracellular signaling and membrane trafficking, leading to parasite death. The metabolite may retain some antimalarial activity, but its primary role is as an analytical marker of drug metabolism.
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| ln Vitro |
In vitro, GNF179 metabolite is used as an analytical standard rather than for biological activity testing. The parent drug GNF179 exhibits potent activity against P. falciparum with an IC50 of 4.8 nM against the multidrug-resistant W2 strain. The metabolite may have reduced or altered antimalarial activity compared to the parent drug, but detailed potency data for the metabolite are not typically reported.
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| ln Vivo |
In vivo, GNF179 metabolite is measured in plasma and tissues during pharmacokinetic studies of GNF179. The parent drug reduces Plasmodium berghei parasitemia levels by 99.7% with a single 100 mg/kg oral dose in mice and prolongs survival by an average of 19 days. GNF179 also protects against infectious P. berghei sporozoite challenge at a single oral dose of 15 mg/kg. The metabolite is monitored to assess drug clearance and exposure.
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| Enzyme Assay |
For non-cellular analytical assays, GNF179 metabolite is quantified by LC-MS/MS. Biological samples (plasma, liver, brain) are extracted by protein precipitation or liquid-liquid extraction, and the metabolite is separated on a C18 column using a gradient of water and acetonitrile containing formic acid. Detection is performed by multiple reaction monitoring (MRM) in positive ion mode.
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| Cell Assay |
For cell-based assays, GNF179 metabolite could be tested for antimalarial activity against P. falciparum-infected red blood cells. Parasite growth is assessed by measuring [3H]-hypoxanthine incorporation or by Giemsa-stained thin blood smears. IC50 values are determined from dose-response curves. Cytotoxicity against mammalian cell lines is assessed by MTT assay.
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| Animal Protocol |
For in vivo experiments, GNF179 is administered orally to mice infected with P. berghei, and the metabolite is measured in plasma and tissues by LC-MS/MS. Pharmacokinetic parameters (Cmax, AUC, t1/2) of the metabolite are calculated. The efficacy of GNF179 is assessed by measuring parasitemia levels and survival time.
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| References |
| Molecular Formula |
C14H16N3F
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|---|---|
| Molecular Weight |
245.29534
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| Exact Mass |
245.133
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| CAS # |
1310455-86-7
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| Related CAS # |
GNF179;1261114-01-5
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| PubChem CID |
57521783
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| Appearance |
White to off-white solid
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| LogP |
2.856
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
18
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| Complexity |
299
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1(C2=NC(C3=CC=C(F)C=C3)=CN2CCN1)C
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0766 mL | 20.3832 mL | 40.7664 mL | |
| 5 mM | 0.8153 mL | 4.0766 mL | 8.1533 mL | |
| 10 mM | 0.4077 mL | 2.0383 mL | 4.0766 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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