Halofantrine Hydrochloride

• CAT Number: R046742
• CAS Number: 36167-63-2
• Molecular Formula: C26H31Cl3F3NO
• Molecular Weight: 536.885
• Purity: ≥95%
• Synonyms: 1,3-Dichloro-α-[2-(dibutylamino)ethyl]-6-(trifluoromethyl)-9-phenanthrenemethanol;?(+/-)-Halofantrine Hydrochloride; Halfan Hydrochloride; SKF 102886; WR 171669
• Storage: -20°C
• IUPAC Name: 3-(dibutylamino)-1-[1,3-dichloro-6-(trifluoromethyl)phenanthren-9-yl]propan-1-ol;hydrochloride
• InChI: InChI=1S/C26H30Cl2F3NO.ClH/c1-3-5-10-32(11-6-4-2)12-9-25(33)23-16-22-21(14-18(27)15-24(22)28)20-13-17(26(29,30)31)7-8-19(20)23;/h7-8,13-16,25,33H,3-6,9-12H2,1-2H3;1H
• InChIKey: WANGFTDWOFGECH-UHFFFAOYSA-N
• SMILES: CCCCN(CCCC)CCC(C1=C2C=CC(=CC2=C3C=C(C=C(C3=C1)Cl)Cl)C(F)(F)F)O.Cl

Halofantrine hydrochloride is a blocker of delayed rectifier potassium current via the inhibition of hERG channel. It is an inhibitor of the hERG channel.

Reference

1:Partitioning of halofantrine hydrochloride between water, micellar solutions, and soybean oil: Effects on its apparent ionization constant. Taillardat-Bertschinger A, Perry CS, Galland A, Prankerd RJ, Charman WN.J Pharm Sci. 2003 Nov;92(11):2217-28. PMID: 14603507 2:Effects of halofantrine hydrochloride (halfan) on the histology of the ovary of mature female Wistar rats. Adjene JO, Agoreyo FO.Afr J Reprod Health. 2003 Apr;7(1):113-20. PMID: 12816318 3:A physicochemical basis for the extensive intestinal lymphatic transport of a poorly lipid soluble antimalarial, halofantrine hydrochloride, after postprandial administration to dogs. Khoo SM, Prankerd RJ, Edwards GA, Porter CJ, Charman WN.J Pharm Sci. 2002 Mar;91(3):647-59. PMID: 11920750 4:X-ray crystal structure of the antimalarial agent (-)-halofantrine hydrochloride supports stereospecificity for cardiotoxicity. Karle JM.Antimicrob Agents Chemother. 1997 Apr;41(4):791-4. PMID: 9087491 Free PMC Article5:In vivo sensitivity of Plasmodium falciparum to halofantrine hydrochloride in Burkina Faso. Del Nero L, Lamizana L, Nebie I, Sare S, Bougouma L, Pietra V.Am J Trop Med Hyg. 1994 Jan;50(1):102-6. PMID: 8304564 6:A new micronized formulation of halofantrine hydrochloride in the treatment of acute Plasmodium falciparum malaria. Gillespie SH, Msaki EP, Ramsay A, Ngowi FI, Fox R.Trans R Soc Trop Med Hyg. 1993 Jul-Aug;87(4):467-9. PMID: 8249083 7:Halofantrine hydrochloride–efficacy and safety in children with acute malaria. Khan MA, Rehman GN, Qazi SA.J Pak Med Assoc. 1991 Jan;41(1):8-10. PMID: 1900550 Free Article8:[Halofantrine hydrochloride in the treatment of Plasmodium falciparum malaria in a region of resistance. Analysis of 54 pediatric cases]. Mashako MN, Kingway MP, Kayembe N.Ann Soc Belg Med Trop. 1990 Mar;70(1):25-32. French. PMID: 2196007 9:Structure of the antimalarial halofantrine hydrochloride. Karle JM, Karle IL.Acta Crystallogr C. 1989 Aug 15;45 ( Pt 8):1248-50. PMID: 2604946 10:Clinical trials with halofantrine hydrochloride in Malawi. Wirima J, Khoromana C, Molyneux ME, Gilles HM.Lancet. 1988 Jul 30;2(8605):250-2. PMID: 2899238