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DSM502

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Catalog No. T40087Cas No. 2426616-55-7

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.

DSM502

DSM502

🥰Excellent
Purity: 99.52%
Catalog No. T40087Cas No. 2426616-55-7
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 SizePriceAvailabilityQuantity
1 mg$132In Stock
2 mg$196In Stock
5 mg$328In Stock
10 mg$529In Stock
25 mg$1,080In Stock
50 mg$1,580In Stock
100 mg$2,160In Stock
1 mL x 10 mM (in DMSO)$363In Stock
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Purity:99.52%
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Product Introduction

Bioactivity
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]
Chemical Properties
Molecular Weight323.31
FormulaC16H16F3N3O
Cas No.2426616-55-7
SmilesCc1c(Cc2ccc(nc2)C(F)(F)F)c[nH]c1C(=O)NC1CC1
Relative Density.1.35 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM3.0930 mL15.4650 mL30.9301 mL154.6503 mL
5 mM0.6186 mL3.0930 mL6.1860 mL30.9301 mL
10 mM0.3093 mL1.5465 mL3.0930 mL15.4650 mL
20 mM0.1547 mL0.7733 mL1.5465 mL7.7325 mL
50 mM0.0619 mL0.3093 mL0.6186 mL3.0930 mL
100 mM0.0309 mL0.1547 mL0.3093 mL1.5465 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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