piperaquine phosphate

Names

[ Name ]:
piperaquine phosphate

[Synonym ]:
Quinoline, 4,4'-(1,3-propanediyldi-4,1-piperazinediyl)bis[7-chloro-
4,4'-(propane-1,3-diyldipiperazine-4,1-diyl)bis(7-chloroquinoline)
Piperaquine tetraphosphate tetrahydrate
7-Chloro-4-[4-[3-[4-(7-chloroquinolin-4-yl)piperazin-1-yl]propyl]piperazin-1-yl]quinoline
Piperaquine
piperaquinoline
PIRERAQUINE PHOSPHATE
4,4'-(1,3-Propanediyldi-4,1-piperazinediyl)bis(7-chloroquinoline)

Biological Activity

[Description]:

Piperaquine is a bisquinoline antimalarial agent. Piperaquine can be used in antimalarial research in combination with Artemisinin[1][2].

[Related Catalog]:

Research Areas >> Infection

[In Vivo]

Piperaquine (10-90 mg/kg; a single i.p.) decreases parasitemia at all of the doses tested in mice[1]. Piperaquine (90 mg/kg; a single i.p.) exhibits the t1/2, apparent clearance, and apparent volume of distribution 17.8 days, 33.5 mg•h/L, 1.55 L/h/kg, and 956 L/kg, respectively, in healthy mice and 16.1 days, 27.3 mg•h/L, 1.9 L/h/kg, and 1,059 L/kg in malaria-infected mice[1].

[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.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
721.1±60.0 °C at 760 mmHg

[ Melting Point ]:
198-200°C (lit.)

[ Molecular Formula ]:
C₂₉H₃₂Cl₂N₆

[ Molecular Weight ]:
535.511

[ Flash Point ]:
389.9±32.9 °C

[ Exact Mass ]:
534.206543

[ PSA ]:
38.74000

[ LogP ]:
5.15

[ Vapour Pressure ]:
0.0±2.3 mmHg at 25°C

[ Index of Refraction ]:
1.664

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VC3280000

CHEMICAL NAME :: Quinoline, 4,4'-(trimethylenedi-4,1-piperazinediyl)bis(7-chloro-

CAS REGISTRY NUMBER :: 4085-31-8

BEILSTEIN REFERENCE NO. :: 0905079

LAST UPDATED :: 199612

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C29-H32-Cl2-N6

MOLECULAR WEIGHT :: 535.57

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1098 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: CYLPDN Zhongguo Yaoli Xuebao. Acta Pharmacologica Sinica. Chinese Journal of Pharmacology. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1980- Volume(issue)/page/year: 7,273,1986

Safety Information

[ Hazard Codes ]:
Xi

[ HS Code ]:
2942000000

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2933990090

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%