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GNF179, an optimized 8,8-dimethyl IP analog, exhibits potency (4.8 nM against the multidrug-resistant strain W2), in vitro metabolic stability, and in vivo oral bioavailability.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $135 | In Stock | |
5 mg | $289 | In Stock | |
10 mg | $478 | In Stock | |
25 mg | $789 | In Stock | |
50 mg | $1,080 | In Stock | |
100 mg | $1,480 | In Stock | |
1 mL x 10 mM (in DMSO) | $318 | In Stock |
Description | GNF179, an optimized 8,8-dimethyl IP analog, exhibits potency (4.8 nM against the multidrug-resistant strain W2), in vitro metabolic stability, and in vivo oral bioavailability. |
In vitro | 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. 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. 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). |
Molecular Weight | 427.9 |
Formula | C22H23ClFN5O |
Cas No. | 1261114-01-5 |
Smiles | CC1(C)N(CCn2c(Nc3ccc(Cl)cc3)c(nc12)-c1ccc(F)cc1)C(=O)CN |
Relative Density. | 1.36 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 120 mg/mL (280.44 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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