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DSM502 DSM502 is a dihydroorotic acid dehydrogenase (DHODH) inhibitor with antimalarial activity that inhibits Plasmodium DHODH and can be used as a lead for antimalarial compounds.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $132 | In Stock | |
2 mg | $196 | In Stock | |
5 mg | $328 | In Stock | |
10 mg | $529 | In Stock | |
25 mg | $1,080 | In Stock | |
50 mg | $1,580 | In Stock | |
100 mg | $2,160 | In Stock | |
1 mL x 10 mM (in DMSO) | $363 | In Stock |
Description | DSM502 DSM502 is a dihydroorotic acid dehydrogenase (DHODH) inhibitor with antimalarial activity that inhibits Plasmodium DHODH and can be used as a lead for antimalarial compounds. |
Targets&IC50 | DHODH (P. vivax):16 nM (IC50), DHODH (P. falciparum):20 nM (IC50) |
In vitro | DSM502 has inhibitory activity against Plasmodium falciparum DHODH (Pf DHODH, IC 50 =20 nM), Plasmodium vivax DHODH (Pv DHODH, IC 50 =14 nM) and Pf 3D7 cells (EC 50 =14 nM), but has no inhibitory effect on the human enzyme [1]. |
In vivo | DSM502 (10 and 50 mg/kg; oral, once daily for 4 days) resulted in 97% parasite clearance in the confirmatory SCID study and 85% clearance in the GSK study; DSM502 (18.3 and 50 mg/kg; single oral dose) exhibited high oral bioavailability (>100%, >100%), apparent t 1/2 (2.6, 3.6 h) and C max (8.4, 42.3 μM) in mice; and DSM502 (2.8 mg/kg; single intravenous injection) exhibited apparent t 1/2 (2.8 h), plasma clearance (26.1 mL/min/kg) and V ss (1.2 L/kg) in mice. [1] |
Molecular Weight | 323.31 |
Formula | C16H16F3N3O |
Cas No. | 2426616-55-7 |
Smiles | Cc1c(Cc2ccc(nc2)C(F)(F)F)c[nH]c1C(=O)NC1CC1 |
Relative Density. | 1.35 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 150 mg/mL (463.95 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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