BRL 6231
BRL 6231 Basic information
- Product Name:
- BRL 6231
- Synonyms:
-
- BRL 6231
- 1-[3-[(2,4,5-Trichlorophenyl)oxy]propoxy]-1,6-dihydro-6,6-dimethyl-1,3,5-triazine-2,4-diamine
- 5-[3-(2,4,5-Trichlorophenoxy)propoxy]-6,6-dimethyl-5,6-dihydro-1,3,5-triazine-2,4-diamine
- WR-99210
- 1,6-Dihydro-6,6-dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]-1,3,5-triazine-2,4-diamine
- 6,6-dimethyl-1-(3-(2,4,5-trichlorophenoxy)propoxy)-1,6-dihydro-1,3,5-triazine-2,4-diamine
- Antifolate,Inhibitor,Bacterial,WR 99210,inhibit,WR99210,WR-99210
- 1,3,5-Triazine-2,4-diamine, 1,6-dihydro-6,6-dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]-
- CAS:
- 47326-86-3
- MF:
- C14H18Cl3N5O2
- MW:
- 394.68
- Mol File:
- 47326-86-3.mol
BRL 6231 Chemical Properties
- Boiling point:
- 519.7±60.0 °C(Predicted)
- Density
- 1.52±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMSO: soluble0.2mg/mL, clear (warmed)
- pka
- 8.48±0.40(Predicted)
- form
- powder
- color
- white to off-white
BRL 6231 Usage And Synthesis
Uses
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.html" class="link-product" target="_blank">Pyrimethamine (HY-18062)-resistant P. falciparum strains) as well as T. gondii[1][2][3].
Biochem/physiol Actions
WR99210 is a potent inhibitor of Plasmodium falciparum dihydrofolate reductase (DHFR), which is a major malarial drug target. It has subnanomolar potency for the wild type, double mutant and quadruple mutant dihydrofolate reductases.
in vivo
WR99210 (1.25 mg/kg; i.p.; single daily for 5 days) is highly effective against T. gondii tachyzoites in a mouse model[1].
| Animal Model: | Male mice (T. gondii-infected)[1]. |
| Dosage: | 1.25 mg/kg |
| Administration: | Intraperitoneal injection; single daily for 5 days. |
| Result: | Exhibited intraperitoneal parasite numbers were 2 logs less in mice on the day 5. |
References
[1] Mui EJ, et al. Triazine Inhibits Toxoplasma gondii tachyzoites in vitro and in vivo. Antimicrob Agents Chemother. 2005 Aug;49(8):3463-7. DOI:10.1128/AAC.49.8.3463-3467.2005
[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. DOI:10.1073/pnas.182295999
[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. DOI:10.1128/AAC.00308-09
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