| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Piperaquine targets the Plasmodium parasite, specifically the intraerythrocytic stages of the malaria parasite. The compound's mechanism involves inhibition of heme detoxification, leading to the accumulation of toxic heme within the parasite and subsequent parasite death. Piperaquine is effective against chloroquine-resistant strains of P. falciparum.
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| ln Vitro |
Piperaquine phosphate demonstrates in vitro antimalarial activity against Plasmodium falciparum. It is effective against chloroquine-resistant strains. The compound's activity is assessed in vitro using parasite growth inhibition assays, where IC50 values are determined against various P. falciparum strains.
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| ln Vivo |
In mice, piperaquine (10-90 mg/kg; single ip) reduces parasitemia at all tested doses[1]. In mice with malaria, piperaquine (90 mg/kg; single ip) shows the following characteristics: in healthy mice, the t1/2, apparent clearance, and apparent volume of distribution are 17.8 days, 33.5 mg·h/L, 1.55 L/h/kg, and 956 L/kg, respectively, whereas in infected mice, they are 16.1 days, 27.3 mg·h/L, 1.9 L/h/kg, and 1,059 L/kg[1].
Piperaquine phosphate demonstrates in vivo efficacy in the treatment of malaria. It is used in combination with dihydroartemisinin as an artemisinin-based combination therapy (ACT) for the treatment of uncomplicated malaria. The compound is effective against Plasmodium falciparum infections. |
| Enzyme Assay |
In vitro enzyme assays for piperaquine are not typically performed, as the compound's mechanism involves inhibition of heme detoxification. Antimalarial activity is assessed using parasite growth inhibition assays against P. falciparum cultures. The compound's ability to inhibit heme polymerization can be measured using in vitro heme detoxification assays.
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| Cell Assay |
In vitro cellular assays for piperaquine phosphate involve culturing P. falciparum-infected erythrocytes in the presence of varying concentrations of the compound. Antimalarial activity is assessed by measuring parasite growth inhibition using fluorescence-based or microscopy-based readouts. IC50 values are determined from dose-response curves.
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| Animal Protocol |
Animal/Disease Models: Male balb/c (Bagg ALBino) mouse: (7 to 8 weeks) are inoculated with Plasmodium berghei parasites[1]
Doses: 0, 10, 30, 90 mg/kg Route of Administration: A single ip administration Experimental Results: The median survival time was 10 days at dose of 10 mg/kg. The median survival time was 54 days at dose of 30 mg/ kg. All mice were active and alert and had stable body weights throughout the course of the study at dose of 90 mg/kg. Animal/Disease Models: Male Swiss mice (6 weeks old)[1] Doses: 90 mg/kg (pharmacokinetic/PK Analysis ) Route of Administration: A single ip administration Experimental Results: t1/2=17.8 d; AUC=33.5 mg·h/L; apparent clearance=1.55 L/h/kg; apparent volume of distribution=956 L/kg. In vivo animal experiments for piperaquine phosphate involve administering the compound to Plasmodium-infected mouse models. Efficacy is evaluated by measuring parasite burden in blood using microscopy or quantitative PCR. The compound's pharmacokinetic properties and antimalarial efficacy are assessed in these studies. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for piperaquine phosphate indicate that it has a long half-life, making it suitable for use in combination therapies. The compound is administered orally. Its absorption, distribution, metabolism, and excretion properties have been characterized in clinical studies. Piperaquine is used in artemisinin-based combination therapies.
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| Toxicity/Toxicokinetics |
Toxicological data for piperaquine phosphate are derived from clinical studies. Common adverse effects include gastrointestinal disturbances, headache, and dizziness. The compound is generally well-tolerated when used in recommended doses. Comprehensive toxicological studies have been conducted as part of its clinical development.
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| References |
[1]. Moore BR, et, al. Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model. Antimicrob Agents Chemother. 2008 Jan; 52(1): 306-11.
[2]. Davis TME, et, al. Piperaquine: a resurgent antimalarial drug. Drugs. 2005; 65(1): 75-87. |
| Additional Infomation |
Piperaquine phosphate (CAS#: 85547-56-4) has the molecular formula C29H32Cl2N6·4H3PO4 and a molecular weight of 927.54. It is an antimalarial drug belonging to the bisquinoline class. Piperaquine is used in combination with dihydroartemisinin for the treatment of malaria. It is effective against chloroquine-resistant strains of Plasmodium falciparum.
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| Molecular Formula |
C29H35CL2N6O4P
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| Molecular Weight |
633.51
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| Exact Mass |
632.183
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| CAS # |
85547-56-4
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| Related CAS # |
Piperaquine tetraphosphate tetrahydrate;915967-82-7;Piperaquine tetraphosphate;911061-10-4;Piperaquine-d6 tetraphosphate;Piperaquine;4085-31-8
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| PubChem CID |
174478
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| Appearance |
Off-white to light yellow solid powder
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| Boiling Point |
721.1ºC at 760mmHg
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| Flash Point |
389.9ºC
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| LogP |
4.501
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
42
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| Complexity |
704
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OP(=O)(O)O.ClC1C=CC2=C(N3CCN(CCCN4CCN(C5C=CN=C6C=C(C=CC=56)Cl)CC4)CC3)C=CN=C2C=1
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| InChi Key |
KATNPMSTHHZOTK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H32Cl2N6.H3O4P/c30-22-2-4-24-26(20-22)32-8-6-28(24)36-16-12-34(13-17-36)10-1-11-35-14-18-37(19-15-35)29-7-9-33-27-21-23(31)3-5-25(27)29;1-5(2,3)4/h2-9,20-21H,1,10-19H2;(H3,1,2,3,4)
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| Chemical Name |
7-chloro-4-[4-[3-[4-(7-chloroquinolin-4-yl)piperazin-1-yl]propyl]piperazin-1-yl]quinoline;phosphoric acid
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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. |
| 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) |
H2O : 17.86 mg/mL (28.19 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5785 mL | 7.8925 mL | 15.7851 mL | |
| 5 mM | 0.3157 mL | 1.5785 mL | 3.1570 mL | |
| 10 mM | 0.1579 mL | 0.7893 mL | 1.5785 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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