Halofantrine hydrochloride

Modify Date: 2024-01-03 15:54:37

Halofantrine hydrochloride Structure
Halofantrine hydrochloride structure
Common Name Halofantrine hydrochloride
CAS Number 36167-63-2 Molecular Weight 536.885
Density 1.244g/cm3 Boiling Point 596.2ºC at 760mmHg
Molecular Formula C26H31Cl3F3NO Melting Point N/A
MSDS Chinese USA Flash Point 314.4ºC

 Use of Halofantrine hydrochloride


Halofantrine hydrochloride (SKF-102886) is a blocker of delayed rectifier potassium current via the inhibition of human-ether-a-go-go-related gene (HERG) channel and a potent antimalarial compound[1][2].

 Names

Name Halofantrine Hydrochloride
Synonym More Synonyms

 Halofantrine hydrochloride Biological Activity

Description Halofantrine hydrochloride (SKF-102886) is a blocker of delayed rectifier potassium current via the inhibition of human-ether-a-go-go-related gene (HERG) channel and a potent antimalarial compound[1][2].
Related Catalog
Target

Malaria[1].HERG channel[2].

References

[1]. Krishna S, et al. Pharmacokinetics, efficacy and toxicity of parenteral halofantrine in uncomplicated malaria. Br J Clin Pharmacol. 1993 Dec;36(6):585-91.

[2]. Tie, H., et al., Inhibition of HERG potassium channels by the antimalarial agent halofantrine. Br. J. Pharmacol. 130, 1967-1975, (2000) Traebert.

 Chemical & Physical Properties

Density 1.244g/cm3
Boiling Point 596.2ºC at 760mmHg
Molecular Formula C26H31Cl3F3NO
Molecular Weight 536.885
Flash Point 314.4ºC
Exact Mass 535.142334
PSA 23.47000
LogP 9.44630
Storage condition 2-8°C

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
SF7790000
CHEMICAL NAME :
9-Phenanthrenemethanol, 1,3-dichloro-alpha-(2-(dibutylamino)ethyl)-6-(trifluo romethyl)-, hydrochloride
CAS REGISTRY NUMBER :
36167-63-2
LAST UPDATED :
199503
DATA ITEMS CITED :
8
MOLECULAR FORMULA :
C26-H30-Cl2-F3-N-O.Cl-H
MOLECULAR WEIGHT :
536.93
WISWESSER LINE NOTATION :
L B666J DG FG IYQ2N4&4 MXFFF &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
7143 ug/kg
TOXIC EFFECTS :
Liver - liver function tests impaired Kidney, Ureter, Bladder - urine volume decreased Kidney, Ureter, Bladder - hematuria
REFERENCE :
LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 340,909,1992
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
18 mg/kg/D
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting Gastrointestinal - other changes
REFERENCE :
DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 5,547,1980
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
72 mg/kg/3D-I
TOXIC EFFECTS :
Cardiac - cardiomyopathy including infarction
REFERENCE :
LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 341,1054,1993
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
7143 ug/kg
TOXIC EFFECTS :
Liver - jaundice, other or unclassified Kidney, Ureter, Bladder - urine volume decreased Blood - other hemolysis with or without anemia
REFERENCE :
LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 340,909,1992
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
3400 mg/kg
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
ACTRAQ Acta Tropica. (Schwabe & Co., Steintorstr. 13, CH-4010 Basel, Switzerland) V.1- 1944- Volume(issue)/page/year: 37,232,1980
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
2050 mg/kg
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
ACTRAQ Acta Tropica. (Schwabe & Co., Steintorstr. 13, CH-4010 Basel, Switzerland) V.1- 1944- Volume(issue)/page/year: 37,232,1980 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
240 mg/kg
SEX/DURATION :
female 6 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetal death
REFERENCE :
TOXID9 Toxicologist. (Soc. of Toxicology, Inc., 475 Wolf Ledge Parkway, Akron, OH 44311) V.1- 1981- Volume(issue)/page/year: 4,85,1984
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
120 mg/kg
SEX/DURATION :
female 6 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
REFERENCE :
TOXID9 Toxicologist. (Soc. of Toxicology, Inc., 475 Wolf Ledge Parkway, Akron, OH 44311) V.1- 1981- Volume(issue)/page/year: 4,85,1984

 Safety Information

Hazard Statements H413
Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
RIDADR NONH for all modes of transport
RTECS SF7790000

 Articles27

More Articles
Effect of serum lipoproteins on stereoselective halofantrine metabolism by rat hepatocytes.

Chirality 24(7) , 558-65, (2012)

Experimental hyperlipidemia has shown to decrease cytochrome P450 3A4 and 2C11 expression and to increase liver concentrations and the plasma protein binding of halofantrine (HF) enantiomers. The pres...

Discordant temporal evolution of Pfcrt and Pfmdr1 genotypes and Plasmodium falciparum in vitro drug susceptibility to 4-aminoquinolines after drug policy change in French Guiana.

Antimicrob. Agents Chemother. 56(3) , 1382-9, (2012)

Analysis of the evolution of drug target genes under changing drug policy is needed to assist monitoring of Plasmodium falciparum drug resistance in the field. Here we genotype Pfcrt and Pfdmr1 of 700...

Using resin to generate a non-invasive intestinal bile-depleted rat model was unsuccessful.

Eur. J. Pharm. Sci. 47(2) , 347-51, (2012)

The purpose of this study was to evaluate if a rat model, based upon co-administration of the anion-exchanging resin, cholestyramine, could replace surgery when evaluating the importance of bile on dr...

 Synonyms

9-phenanthrenemethanol, 1,3-dichloro-α-[2-(dibutylamino)ethyl]-6-(trifluoromethyl)-, hydrochloride
UNII:2B7ENL644K
3-(Dibutylamino)-1-[1,3-dichlor-6-(trifluormethyl)phenanthren-9-yl]propan-1-olhydrochlorid
MFCD00879136
3-(Dibutylamino)-1-[1,3-dichloro-6-(trifluoromethyl)-9-phenanthryl]propan-1-ol hydrochloride (1:1)
3-(dibutylamino)-1-[1,3-dichloro-6-(trifluoromethyl)phenanthren-9-yl]propan-1-ol hydrochloride
EINECS 252-895-4
3-(dibutylamino)-1-[1,3-dichloro-6-(trifluoromethyl)phenanthren-9-yl]propan-1-ol hydrochloride (1:1)
3-(Dibutylamino)-1-[1,3-dichloro-6-(trifluoromethyl)-9-phenanthryl]-1-propanol hydrochloride (1:1)
9-Phenanthrenemethanol, 1,3-dichloro-α-[2-(dibutylamino)ethyl]-6-(trifluoromethyl)-, hydrochloride (1:1)
Halofantrine hydrochloride
3-(dibutylamino)-1-[1,3-dichloro-6-(trifluorométhyl)phénanthrén-9-yl]propan-1-ol chlorhydrate
UNII:H77DL0Y630
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