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Piperaquine (Synonyms: Piperaquinoline)

Catalog No.GC13875

used in combination with artimesinin for inhibition of HIV-1 replication

Products are for research use only. Not for human use. We do not sell to patients.

Piperaquine Chemical Structure

Cas No.: 4085-31-8

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10mg
$75.00
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25mg
$173.00
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50mg
$321.00
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100mg
$570.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

IC50: 9.8 to 217.3 nM for P. falciparum isolates

Piperaquine, an antimalarial drug, is first synthesised in the 1960s and extensively used as prophylaxis and treatment during the next 20 years.

In vitro: In 280 P. falciparum isolates, the IC50 for piperaquine ranged from 9.8 nM to 217.3 nM and a significant but low correlation was observed between the IC50 values for piperaquine and chloroquine. However, the coefficient of determination indicated that only 2.1% of the variation in the response to piperaquine was explained by the variation in the response to chloroquine. Moreover, the mean value for piperaquine was 74.0 nM in the Pfcrt K76 wild-type group and 87.7 nM in the 76T mutant group and such difference was not significant [1].

In vivo: Male SD rats were orally administered piperaquine or as a short-term i.v. infusion. Results showed that piperaquine disposition was best described by a 3-compartment model with a rapid initial distribution phase after i.v. administration. The PK of piperaquine was characterized by a low clearance, a large volume of distribution and a long terminal half-life [2].

Clinical trial: The safety and efficacy of a combination of dihydroartemisinin (DHA) and piperaquine was assessed in patients with uncomplicated falciparum malaria. Mean total DHA and piperaquine doses were 9.1 and 73.9 mg/kg, respectively, for children and 6.6 and 52.9 mg/kg for adults. Results showed that excluding the results for 1 child who died, there was a 96.9% 28-day cure rate. Side effects were reported by 22 patients but did not necessitate premature cessation of therapy [3].

References:
[1] Pascual A et al.  In vitro piperaquine susceptibility is not associated with the Plasmodium falciparum chloroquine resistance transporter gene. Malar J. 2013 Nov 25;12:431.
[2] Tarning J, Lindegardh N, Sandberg S, Day NJ, White NJ, Ashton M.  Pharmacokinetics and metabolism of the antimalarial piperaquine after intravenous and oral single doses to the rat. J Pharm Sci. 2008 Aug;97(8):3400-10.
[3] Denis MB, Davis TM, Hewitt S, Incardona S, Nimol K, Fandeur T, Poravuth Y, Lim C, Socheat D.  Efficacy and safety of dihydroartemisinin-piperaquine (Artekin) in Cambodian children and adults with uncomplicated falciparum malaria. Clin Infect Dis. 2002 Dec 15;35(12):1469-76.

Chemical Properties

Cas No. 4085-31-8 SDF
Synonyms Piperaquinoline
Chemical Name 4,4'-(1,3-propanediyldi-4,1-piperazinediyl)bis[7-chloro-quinoline
Canonical SMILES ClC1=CC2=C(C=C1)C(N3CCN(CC3)CCCN4CCN(CC4)C5=C6C=CC(Cl)=CC6=NC=C5)=CC=N2
Formula C29H32Cl2N6 M.Wt 535.5
Solubility ≤0.2mg/ml in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.8674 mL 9.3371 mL 18.6741 mL
5 mM 0.3735 mL 1.8674 mL 3.7348 mL
10 mM 0.1867 mL 0.9337 mL 1.8674 mL
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Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 12 reference(s) in Google Scholar.)

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