Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Targets |
IC50: 95 nM (P. falciparum DHODH), 52 nM (P. vivax DHODH)[1]
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ln Vitro |
DSM705 hydrochloride exhibits inhibitory activity with no inhibition of the human enzyme against P. falciparum DHODH (PfDHODH, IC50=95 nM), P. vivax DHODH (PvDHODH, IC50=52 nM), and Pf3D7 cells (EC50=12 nM)[1].
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ln Vivo |
At a dose of 50 mg/kg, DSM705 (3-200 mg/kg; po twice a day for 6 days) hydrochloride offers the highest rate of parasite killing and completely suppresses parasitemia by days 7-8[1]. Among Swiss outbred mice, DSM705 (2.6 and 24 mg/kg; a single po) hydrochloride shows high oral bioavailability (74%, 70%), apparent t1/2 (3.4, 4.5 h), and Cmax (2.6, 20 μM)[1]. Mice treated with DSM705 (2.3 mg/kg; one IV) hydrochloride show plasma clearance (CL=2.8 mL/min/kg) and Vss (1.3 L/kg)[1].
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Animal Protocol |
Animal/Disease Models: SCID (severe combined immunodeficient) mouse were inoculated with parasites[1]
Doses: 3, 10, 20, 50, 100, 200 mg/kg Route of Administration: Po twice a day for 6 days Experimental Results: Killed parasite in a dose dependent manner and fully suppressed parasitemia by days 7-8. Animal/Disease Models: Swiss Outbred Mice[ 1] Doses: 2.6 and 24 mg/kg for po; 2.3 mg/kg for iv (pharmacokinetic/PK Analysis) Route of Administration: A single po and iv Experimental Results: Po: F=74/70%, t1/2=3.4/4.5 h, Cmax=2.6/20 μM. Iv: CL=2.8 mL/min/kg, Vss=1.3 L/kg. |
References |
[1]. Palmer MJ, et, al. Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series. J Med Chem. 2021 May 13;64(9):6085-6136.
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Molecular Formula |
C19H20CLF3N6O
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Molecular Weight |
440.85
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Related CAS # |
DSM705;2653225-38-6
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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: Please store this product in a sealed and protected environment, 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) |
DMSO :~100 mg/mL (~226.83 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.67 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.67 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2683 mL | 11.3417 mL | 22.6835 mL | |
5 mM | 0.4537 mL | 2.2683 mL | 4.5367 mL | |
10 mM | 0.2268 mL | 1.1342 mL | 2.2683 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.