Cycloguanil Hydrochloride Property

Melting point:

210-2150C

storage temp. 

Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

solubility 

DMSO (Slightly, Sonicated), Methanol (Slightly), Water (Slightly)

form 

Solid

color 

White to Off-White

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Cycloguanil Hydrochloride Chemical Properties,Usage,Production

Description

Cycloguanil is the active metabolite of the antimalarial prodrug proguanil. Cycloguanil is formed from proguanil by the cytochrome P450 (CYP) isoforms CYP2C19 and CYP3A in human liver microsomes. It is an inhibitor of dihydrofolate reductase (DHFR; K_is = 1.5 and 0.79 nM for the P. falciparum and P. berghei enzymes, respectively). It is active against ten P. falciparum field isolates (IC₅₀s = 0.12-1,400 μg/ml). Cycloguanil reduces parasitemia in a mouse model of P. berghei infection (ED₅₀ = 2 mg/kg). It also reduces parasitemia in a rhesus monkey model of P. cynomolgi infection when administered at a dose of 0.3 mg/kg.

Chemical Properties

Crystalline Solid

Uses

Labelled antimalarial drug

Uses

Antimalarial drug.

Definition

ChEBI: Cycloguanil hydrochloride is the hydrochloride salt of cycloguanil. It is an organic molecular entity and a hydrochloride. It contains a cycloguanil.

References

[1] foote s j, galatis d, cowman a f. amino acids in the dihydrofolate reductase-thymidylate synthase gene of plasmodium falciparum involved in cycloguanil resistance differ from those involved in pyrimethamine resistance[j]. proceedings of the national academy of sciences, 1990, 87(8): 3014-3017.
[2] blakley r l. dihydrofolate reductase[j]. encyclopedia of molecular medicine, 1984.
[3] birkett d j, rees d, andersson t, et al. in vitro proguanil activation to cycloguanil by human liver microsomes is mediated by cyp3a isoforms as well as by s‐mephenytoin hydroxylase[j]. british journal of clinical pharmacology, 1994, 37(5): 413-420.