| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Targets |
Plasmodium Toxoplasma
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| ln Vitro |
Purfalcamine exhibits minimal efficacy against the calcium-dependent protein kinase 3 (TgCDPK3) of Toxoplasma gondii [1]. For the first 32 hours, purfalcamine (225, 450 nM) has no effect on the parasitemia. The parasite level stays constant for almost 40 hours before starting to decline[1]. For P. falciparum strains (3D7, Dd2, FCB, HB3, and W2), purfalcamine inhibits proliferation with EC50s of 171-259 nM, indicating efficacy against drug-resistant parasites[1]. Purfalcamine exhibits a therapeutic window extending from 23-fold to 36-fold (EC50s for CHO=12.33 μM, HEp2=7.235 μM, HeLa=7.029 μM, and Huh7=5.476 μM), because the EC50 value for P. falciparum (3D7) is 230 nM[1].
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| ln Vivo |
In treated mice, purfalcamine (10 mg/kg; oral gavage; BID; for 6 days) shows a delay in the development of parasitemia[1]. The half-life of purfalcamine (20 mg/kg; oral gavage) is 3.1 hours, and its Cmax is 2.6 μM[1].
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| Animal Protocol |
Animal/Disease Models: Male balb/c (Bagg ALBino) mouse:, 7 weeks of age with the malaria parasite[1]
Doses: 10 mg /kg Route of Administration: po (oral gavage); BID; for 6 days Experimental Results: Demonstrated a delay in the onset of parasitemia in treated mice when compared with control mice. Animal/Disease Models: Five- to sixweeks old male balb/c (Bagg ALBino) mouse: (22- 25 g)[1] Doses: 20 mg/kg (pharmacokinetic/PK Analysis) Route of Administration: Orally gavage Experimental Results: demonstrated a maximum plasma exposure (Cmax) of 2.6 μM with a half-life of 3.1 hrs (hours). |
| References |
[1]. Nobutaka Kato, et al. Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility. Nat Chem Biol. 2008 Jun;4(6):347-56.
[2]. Rajshekhar Y Gaji, et al. Expression of the essential Kinase PfCDPK1 from Plasmodium falciparum in Toxoplasma gondii facilitates the discovery of novel antimalarial drugs. Antimicrob Agents Chemother. 2014 May;58(5):2598-607. |
| Molecular Formula |
C29H33FN8O
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|---|---|
| Molecular Weight |
528.62
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| CAS # |
1038620-68-6
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
FC1=CC=CC(=C1)N1C=NC2C(NC3C=CC(=CC=3)C(N3CCCCC3)=O)=NC(=NC1=2)NC1CCC(CC1)N
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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 |
| 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 : 12.5 mg/mL (23.65 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.36 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 12.5 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: ≥ 1.25 mg/mL (2.36 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 12.5 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: ≥ 1.25 mg/mL (2.36 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8917 mL | 9.4586 mL | 18.9172 mL | |
| 5 mM | 0.3783 mL | 1.8917 mL | 3.7834 mL | |
| 10 mM | 0.1892 mL | 0.9459 mL | 1.8917 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.
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