| Identification | Back Directory | [Name]
TAFENOQUINE SUCCINATE | [CAS]
106635-81-8 | [Synonyms]
WR-238605
SB-252263
Krintafel
SB 252263AX
Wr238605 succinate
Tafenoquine Succinate
N-[2,6-Dimethoxy-4-methyl-5-[3-(trifluoromethyl)phenoxy]quinolin-8-yl]pentane-1,4-diamine
8-[(4-Amino-1-methylbutyl)amino]-2,6-dimethoxy-4-methyl-5-[3-(trifluoromethyl)phenoxy]quinoline succinate
TAFENOQUINE SUCCINATE; WR-238605, WR 238605, WR238605, SB-252263-AAB; SB252263-AAB; SB 252263-AAB; KRINTAFEL;
Butanedioic acid, compd. with N(sup 4)-(2,6-dimethoxy-4-methyl-5-(3-(trifluoromethyl)phenoxy)-8-quinolinyl)-1,4-pentanediamine (1:1) | [Molecular Formula]
C28H34F3N3O7 | [MDL Number]
MFCD00892249 | [MOL File]
106635-81-8.mol | [Molecular Weight]
581.581 |
| Chemical Properties | Back Directory | [Melting point ]
146-149° | [storage temp. ]
2-8°C | [solubility ]
DMSO: soluble5mg/mL (clear solution) | [form ]
powder | [color ]
white to beige | [InChIKey]
CQBKFGJRAOXYIP-UHFFFAOYSA-N | [SMILES]
OC(=O)CCC(O)=O.COc1cc(C)c2c(Oc3cccc(c3)C(F)(F)F)c(OC)cc(NC(C)CCCN)c2n1 |
| Hazard Information | Back Directory | [Uses]
Tafenoquine succinate is a new 8-aminoquinoline with an improved therapeutic index and safety profile as compared to primaquine (P733500).Tafenoquine has the potential to become a widely used drug in the preven tion and treatment of malaria infection and could replace some currently used drugs as resistant strains of Plasmodium species increase.
| [Biochem/physiol Actions]
Tafenoquine is an antimalarial primaquine analog being investigated to treat and prevent Plasmodium vivax infections. It can eliminate both blood and liver stages of Plasmodium vivax. Tafenoquine has also been tested as a therapy for leishmaniasis. | [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]. | [IC 50]
Plasmodium |
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| Company Name: |
Sigma-Aldrich
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| Tel: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
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