| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
The primary target of WR99210 hydrochloride is dihydrofolate reductase (DHFR), an enzyme in the folate pathway that is essential for parasite survival. The compound inhibits P. falciparum DHFR (pfDHFR) with subnanomolar potency (IC₅₀ < 0.075 nM). WR99210 hydrochloride is effective against wild-type, double mutant, and quadruple mutant DHFR enzymes.
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| ln Vitro |
In vitro studies have demonstrated that WR99210 hydrochloride is a potent inhibitor of pfDHFR. The compound shows IC₅₀ < 0.075 nM against DHFR. WR99210 hydrochloride has good antiparasitic activity and is effective against P. falciparum and P. vivax strains as well as Toxoplasma gondii. These potent in vitro activities make it a valuable research tool.
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| ln Vivo |
In vivo studies have confirmed the antimalarial activity of WR99210 hydrochloride. The compound is orally active. WR99210 hydrochloride was developed as an antimalarial drug candidate. It is widely used to select Plasmodium transfectants. The compound's in vivo efficacy has been demonstrated in animal models.
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| Enzyme Assay |
For DHFR inhibition assays, recombinant DHFR enzyme is incubated with a substrate in the presence of WR99210 hydrochloride. Enzyme activity is measured spectrophotometrically, and IC₅₀ values are calculated. For anti-parasitic activity screening, P. falciparum parasites are cultured and treated with serial dilutions of the compound. Parasite growth inhibition is assessed.
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| Cell Assay |
For in vitro cell-based studies, P. falciparum parasites are cultured in human erythrocytes and treated with serial dilutions of WR99210 hydrochloride. Parasite growth is assessed by measuring [³H]-hypoxanthine incorporation or by fluorescence-based methods. Cytotoxicity against mammalian cells is assessed in parallel.
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| Animal Protocol |
In vivo animal studies for WR99210 hydrochloride have been conducted in mouse models of malaria. Mice infected with P. falciparum are treated with the compound via oral administration. Parasitemia is monitored, and efficacy endpoints include reduction in parasitemia and survival.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of WR99210 hydrochloride have been characterized. The compound is orally active. It has low toxicity. Specific PK parameters such as half-life and bioavailability have been reported in the literature. WR99210 hydrochloride is used to select Plasmodium transfectants.
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| Toxicity/Toxicokinetics |
Toxicological data for WR99210 hydrochloride are available from preclinical studies. The compound has low toxicity. Standard toxicology studies have been conducted. The compound's safety profile supports its use in research applications.
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| References |
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| Additional Infomation |
WR99210 hydrochloride is a research compound for antimalarial drug discovery. It is a potent inhibitor of pfDHFR with subnanomolar potency. The compound was originally developed as an antimalarial drug candidate. It is widely used to select Plasmodium transfectants. No clinical trials have been reported for this compound. WR99210 hydrochloride serves as a valuable research tool for studying DHFR inhibition and antimalarial drug resistance.
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| Molecular Formula |
C14H18N5O2CL3
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|---|---|
| Molecular Weight |
431.14
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| Exact Mass |
431.026
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| CAS # |
30711-93-4
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| Related CAS # |
WR99210;47326-86-3
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| PubChem CID |
121749
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
25
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| Complexity |
503
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VOTSDCGUYAGUNS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H18Cl3N5O2.ClH/c1-14(2)21-12(18)20-13(19)22(14)24-5-3-4-23-11-7-9(16)8(15)6-10(11)17;/h6-7H,3-5H2,1-2H3,(H4,18,19,20,21);1H
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| Chemical Name |
6,6-dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]-1,3,5-triazine-2,4-diamine;hydrochloride
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3194 mL | 11.5972 mL | 23.1943 mL | |
| 5 mM | 0.4639 mL | 2.3194 mL | 4.6389 mL | |
| 10 mM | 0.2319 mL | 1.1597 mL | 2.3194 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.
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