1,3-dihydro-1-hydroxy-2,1-Benzoxaborole-7-propanoic acid

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

  H315：Verursacht Hautreizungen.

  H319：Verursacht schwere Augenreizung.

  H335：Kann die Atemwege reizen.

• Sicherheit

  P261：Einatmen von Staub vermeiden.

  P305+P351+P338：BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach Möglichkeit entfernen. Weiter spülen.

1,3-dihydro-1-hydroxy-2,1-Benzoxaborole-7-propanoic acid Chemische Eigenschaften,Einsatz,Produktion Methoden

• Biologische Aktivität

  AN3661, a potent antimalarial lead compound, targets Plasmodium falciparum cleavage and polyadenylate-specific factor homolog subunit 3 (PfCPSF3). It inhibits infection of laboratory-adapted strains of Plasmodium falciparum (mean IC50=32 nM), Ugandan field isolates (mean IC50=64 nM) and mice P. berghei and P. falciparum.

• in vitro

  AN3661 is active at nanomolar (IC ₅₀ =20-56 nM) concentrations against P. falciparum laboratory strains known to be sensitive (3D7) or resistant (W2, Dd2, K1, HB3, FCR3 and TM90C2B), and AN3661 is similarly active in ex vivo studies of fresh Ugandan field isolates (mean ex vivo IC ₅₀ =64 nM). AN3661 shows minimal cytotoxicity against mammalian cell lines, with the CC ₅₀ 60.5 μM against Jurkat cells, and all other CC ₅₀ values greater than the highest concentrations tested (25 μM or above).
  AN3661 inhibits the stability of P. falciparum transcripts.

• in vivo

  AN3661 (50-200 mg.kg; po; daily for 4 days) inhibits murine P. berghei infections with ED ₉₀ (4 days) 0.34 mg/kg.
  AN3661 is administered orally for 4 days, beginning on the third day of infection, the ED ₉₀ 4 days after initiation of treatment is 0.57 mg/kg.

  < td class="col1 fwb"> Animal Model:

  P. berghei -infected mice (malaria model)
  Dosage:	50, 100, 200 mg/kg
  Administration:	Orally; daily for 4 days
  Result:	Rapidly controlled parasitemias, with an ED 90 of 0.34 mg/kg. Daily dosages of 50 mg/kg and 100 mg/kg extended survival, and mice treated with 200 mg/kg per day demonstrated long-term cures.

1,3-dihydro-1-hydroxy-2,1-Benzoxaborole-7-propanoic acid Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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