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106635-81-8

106635-81-8 structure
106635-81-8 structure
  • Name: Tafenoquine (Succinate)
  • Chemical Name: butanedioic acid,4-N-[2,6-dimethoxy-4-methyl-5-[3-(trifluoromethyl)phenoxy]quinolin-8-yl]pentane-1,4-diamine
  • CAS Number: 106635-81-8
  • Molecular Formula: C28H34F3N3O7
  • Molecular Weight: 581.58100
  • Catalog: Signaling Pathways Anti-infection Parasite
  • Create Date: 2017-02-08 23:30:55
  • Modify Date: 2024-01-22 18:06:17
  • Tafenoquine Succinate (WR 238605 Succinate) is an 8-aminoquinoline. Tafenoquine is an anti-malarial prophylactic agent[1].
Name butanedioic acid,4-N-[2,6-dimethoxy-4-methyl-5-[3-(trifluoromethyl)phenoxy]quinolin-8-yl]pentane-1,4-diamine
Synonyms Tafenoquine succinate
UNII-DL5J0B8VSS
Tafenoquine Succinate
tafenoquine maleate
Etaquine
Tafenoquine (Succinate)
Description Tafenoquine Succinate (WR 238605 Succinate) is an 8-aminoquinoline. Tafenoquine is an anti-malarial prophylactic agent[1].
Related Catalog
Target

Anti-malarial[1]

In Vivo Tafenoquine exhibits no anti-malarial activity in CYP 2D knock-out mice when dosed at their ED100 values (3 mg/kg) established in WT mice. Tafenoquine anti-malarial activity is partially restored in humanized/CYP 2D6 knock-in mice when tested at two times its ED100 (6 mg/kg)[1].
References

[1]. Marcsisin SR, et al. Tafenoquine and NPC-1161B require CYP 2D metabolism for anti-malarial activity: implications for the 8-aminoquinoline class of anti-malarial compounds. Malar J. 2014 Jan 3;13:2.
Density 1.237g/cm3
Boiling Point 565.6ºC at 760mmHg
Molecular Formula C28H34F3N3O7
Molecular Weight 581.58100
Flash Point 295.9ºC
Exact Mass 581.23500
PSA 153.23000
LogP 6.61990
Storage condition 2-8℃

CHEMICAL IDENTIFICATION

RTECS NUMBER :
SA0242400
CAS REGISTRY NUMBER :
106635-81-8
LAST UPDATED :
199107
DATA ITEMS CITED :
2
MOLECULAR FORMULA :
C24-H28-F3-N3-O3.C4-H6-O4
MOLECULAR WEIGHT :
581.65

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
416 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 32,1728,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
71 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 32,1728,1989
RIDADR NONH for all modes of transport

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