MMV030084 is a PfPKG inhibitor. MMV030084 exhibits an IC₅₀ of 199 nM against liver-stage parasites in HepG2 cells. MMV030084 is highly active against synchronized schizonts, with IC₅₀ values of 109 nM for the 3D7-A10 strain and 120 nM for the multidrug-resistant Dd2-B2 strain, while showing minimal activity against ring and trophozoite stages. The compound also inhibits male gamete exflagellation with an IC₅₀ of 141 nM, though it lacks efficacy against early and late-stage gametocytes (IC₅₀ > 40 μM). Mechanistic studies identify cGMP-dependent protein kinase (PfPKG) as the primary target, with MMV030084 demonstrating an IC₅₀ of 0.4 nM in recombinant kinase assays.
MedKoo Cat#: 126360
Name: MMV030084
CAS#: 342434-07-5
Chemical Formula: C18H19ClN4O
Exact Mass: 342.1247
Molecular Weight: 342.83
Elemental Analysis: C, 63.06; H, 5.59; Cl, 10.34; N, 16.34; O, 4.67
The following data is based on the product molecular weight 342.83 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
