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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
Tafenoquine succinate (formerly WR-238605; Krintafel), the succinate salt of tafenoquine, is an orally bioactive 8-aminoquinoline based anti-malarial drug approved for the treatment and prophylaxis of malaria.
Targets |
Anti-malarial
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ln Vivo |
When administered at the 3 mg/kg ED100 values established in WT mice, tafenoquine does not show any anti-malarial activity in CYP 2D knock-out mice. In humanized/CYP 2D6 knock-in mice, tafenoquine's anti-malarial activity is partially restored when tested at twice its ED100 (6 mg/kg)[1].
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References |
Molecular Formula |
C28H34F3N3O7
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Molecular Weight |
581.590
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Elemental Analysis |
C, 57.83; H, 5.89; F, 9.80; N, 7.23; O, 19.26
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CAS # |
106635-81-8
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Related CAS # |
Tafenoquine;106635-80-7
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Appearance |
Solid powder
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SMILES |
CC(NC1=C2N=C(OC)C=C(C)C2=C(OC3=CC=CC(C(F)(F)F)=C3)C(OC)=C1)CCCN.O=C(O)CCC(O)=O
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InChi Key |
CQBKFGJRAOXYIP-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C24H28F3N3O3.C4H6O4/c1-14-11-20(32-4)30-22-18(29-15(2)7-6-10-28)13-19(31-3)23(21(14)22)33-17-9-5-8-16(12-17)24(25,26)27;5-3(6)1-2-4(7)8/h5,8-9,11-13,15,29H,6-7,10,28H2,1-4H3;1-2H2,(H,5,6)(H,7,8)
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Chemical Name |
N4-(2,6-dimethoxy-4-methyl-5-(3-(trifluoromethyl)phenoxy)quinolin-8-yl)pentane-1,4-diamine succinate
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~125 mg/mL (~214.93 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.58 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.58 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.58 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.08 mg/mL (3.58 mM) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.7194 mL | 8.5971 mL | 17.1942 mL | |
5 mM | 0.3439 mL | 1.7194 mL | 3.4388 mL | |
10 mM | 0.1719 mL | 0.8597 mL | 1.7194 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Schematic illustrating pitfalls and protections of suppressive (yellow dose indicators) or causal (orange dose indicators) chemoprevention of non-relapsing malaria likeP. falciparum(top panel; red triangles and squares for inoculation and attack, respectively) or relapsing species likeP. vivax(bottom panel; green triangles and squares).J Travel Med.2018 Jan 1;25(1). doi: 10.1093/jtm/tay110. th> |
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Geographic distribution and prevalence ofP. vivax(A) andP. falciparum(B) in 2010,reproduced here under Creative Commons license. Hypothesized relative attack rates in the months following radical cure illustrate possible impacts of variable risks of relapse or reinfection on the estimation hypnozoitocidal efficacy oftafenoquine(TQ) fixed at a presumed ‘actual’ 95% rate compared to a chloroquine (CQ) arm without hypnozoitocidal therapy (relapse and reinfection attacks).J Travel Med.2018 Jan 1;25(1). doi: 10.1093/jtm/tay110. td> |
Antimalarial classes as guided by life cycle of the plasmodia. Evolution of the 8-aminoquinoline hypnozoitocides, including the winnowing out of irreversible severe neurotoxicity of plasmocid and related compounds distinguished by fewer than four methylene groups separating the amino groups of the alkyl chain at the defining 8-amino position. Plasmochin and others (including primaquine) having at least four methylene groups exhibited no such neurotoxicity but instead reversible toxicity at sub-lethal doses involving principally hepatic, hematological and gastrointestinal systems.J Travel Med.2018 Jan 1;25(1). doi: 10.1093/jtm/tay110. td> |