WR99210
Based on 6 publication(s) in Google Scholar
WR99210 is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor (IC50<0.075 nM). WR99210 shows good antiparasitic activity and is effective against P. falciparum and P. falciparum strains (including Pyrimethamine< (HY-18062)-resistant P. falciparum strains) as well as T. gondii.
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- Pureza: 99.10%
- No. CAS: 47326-86-3
- Fòrmula: C14H18Cl3N5O2
- Peso molecular:394.68
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years
* The compound is unstable in solutions, freshly prepared is recommended.
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) WR99210
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Actividad biológica
IC50: <0.075 nM (DHFR)[3].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Vero | IC50 |
>1 μM
Compound: WR99210
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Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
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[PMID: 32294614] |
| Vero | IC50 |
>10 μM
Compound: WR99210
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Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 72 hrs by SRB assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 72 hrs by SRB assay
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[PMID: 34624822] |
WR99210 (0-100 nM; 92 h) is highly effective against T. gondii tachyzoites in tissue culture[1].
WR99210 (0-100 nM; 92 h) shows low cytotoxicity to human foreskin fibroblasts[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human foreskin fibroblasts (T. gondii-infected)
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Concentration:0-100 nM
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Incubation Time:92 h
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Result:Showed marked inhibition of T. gondii, with an IC50 value of approximately 50 nM.
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Cell Line:Human foreskin fibroblasts
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Concentration:0-100 nM
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Incubation Time:92 h
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Result:Lacked of toxicity for fibroblasts.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male mice (T. gondii-infected)[1].
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Dosage:1.25 mg/kg
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Administration:Intraperitoneal injection; single daily for 5 days.
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Result:Exhibited intraperitoneal parasite numbers were 2 logs less in mice on the day 5.
Chemical Information
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No. CAS 47326-86-3
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Appearance Solid
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Peso molecular 394.68
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Fòrmula C14H18Cl3N5O2
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Color White to off-white
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SMILES
CC1(N=C(N=C(N1OCCCOC2=C(C=C(C(Cl)=C2)Cl)Cl)N)N)C
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Synonyms
BRL 6231 free base
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years * The compound is unstable in solutions, freshly prepared is recommended.
Publications (6)
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Journal Impact Factor
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Most Recent
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PLoS Biol
Mechanistic basis for multidrug resistance and collateral drug sensitivity conferred to the malaria parasite by polymorphisms in PfMDR1 and PfCRT. [Abstract]2022 May; 20(5): e3001616. PMID: 35507548 -
Antimicrob Agents Chemother
Synergistic activity of RSL3 and Pyrimethamine to inhibit the proliferation of Plasmodium falciparum. [Abstract]2025 Aug 18:e0047125. PMID: 40823867 -
Microbiol Spectr
Plasmodium falciparum GAP40 Plays an Essential Role in Merozoite Invasion and Gametocytogenesis. [Abstract]2023 Jun 15;11(3):e0143423. PMID: 37249423 -
bioRxiv
Duplication of superoxide dismutase and a mutation in aquaglyceroporin mediates the sensitivity of Plasmodium falciparum to cryptosporin, a natural product derived from Acaromyces ingoldii. [Abstract]2026 Jun 10:2026.06.08.730986. PMID: 42327216 -
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Solvente y solubilidad
DMSO : 5 mg/mL (12.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Mui EJ, et al. Triazine Inhibits Toxoplasma gondii tachyzoites in vitro and in vivo. Antimicrob Agents Chemother. 2005 Aug;49(8):3463-7. [Content Brief]
[2]. Hastings MD, et al. Pyrimethamine and WR99210 exert opposing selection on dihydrofolatereductase from Plasmodium vivax. Proc Natl Acad Sci U S A. 2002 Oct 1;99(20):13137-41. [Content Brief]
[3]. Kiara SM, et al. In vitro activity of antifolate and polymorphism in dihydrofolate reductase of Plasmodium falciparum isolates from the Kenyan coast: emergence of parasites with Ile-164-Leu mutation. Antimicrob Agents Chemother. 2009 Sep;53(9):3793-8. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5337 mL | 12.6685 mL | 25.3370 mL | 63.3425 mL |
| 5 mM | 0.5067 mL | 2.5337 mL | 5.0674 mL | 12.6685 mL | |
| 10 mM | 0.2534 mL | 1.2668 mL | 2.5337 mL | 6.3342 mL |
WR99210 Related Classifications
HY-116387 Related Classifications
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