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Merck
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SML2375

Sigma-Aldrich

KDU691

≥98% (HPLC)

Synonyme(s) :

KDU 691, N-(4-Chlorophenyl)-N-methyl-3-[4-(methylcarbamoyl)phenyl]imidazo[1,2-a]pyrazine-6-carboxamide, N-(4-Chlorophenyl)-N-methyl-3-[4-[(methylamino)carbonyl]phenyl]imidazo[1,2-a]pyrazine-6-carboxamide

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About This Item

Formule empirique (notation de Hill):
C22H18ClN5O2
Numéro CAS:
1513879-19-0
Poids moléculaire :
419.86
Numéro MDL:
MFCD28963927
Code UNSPSC :
12352200

Pureté

≥98% (HPLC)

Forme

powder

Couleur

white to brown

Solubilité

DMSO: 2 mg/mL, clear

Température de stockage

2-8°C

Chaîne SMILES 

O=C(N(C1=CC=C(Cl)C=C1)C)C(N=C2)=CN3C2=NC=C3C4=CC=C(C(NC)=O)C=C4

Actions biochimiques/physiologiques

KDU691 is an orally active imidazopyrazine class antiparasitic that inhibits Plasmodium & Cryptosporidium phosphatidylinositol-4-OH kinase, PI(4)K, in an ATP-competitive, highly potent and selective manner (IC50/[ATP] = 1.5 nM/10 μM/P. vivax & 17 nM/3 μM/C. parvum PI(4)K) with little or no activity against human PI3Kα/β/γ/δ, PI4KIIIβ, VPS34, and 36 human protein kinases. KDU691 is effective against human pathogens P. falciparum, P. vivax, C. parvum and C. hominis, as well as simian parasite P. cynomolgi. KDU691 blocks Plasmodium development in all life-cycle stages and displays in vivo efficacy in murine models of malaria and cryptosporidiosis.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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Pamela Orjuela-Sanchez et al.
ACS infectious diseases, 4(4), 531-540 (2018-03-16)
To develop new drugs and vaccines for malaria elimination, it will be necessary to discover biological interventions, including small molecules that act against Plasmodium vivax exoerythrocytic forms. However, a robust in vitro culture system for P. vivax is still lacking. Thus
Michelle Yi-Xiu Lim et al.
Nature microbiology, 16166-16166 (2016-09-20)
A molecular understanding of drug resistance mechanisms enables surveillance of the effectiveness of new antimicrobial therapies during development and deployment in the field. We used conventional drug resistance selection as well as a regime of limiting dilution at early stages
Ujjini H Manjunatha et al.
Nature, 546(7658), 376-380 (2017-06-01)
Diarrhoeal disease is responsible for 8.6% of global child mortality. Recent epidemiological studies found the protozoan parasite Cryptosporidium to be a leading cause of paediatric diarrhoea, with particularly grave impact on infants and immunocompromised individuals. There is neither a vaccine
Anne-Marie Zeeman et al.
Antimicrobial agents and chemotherapy, 60(5), 2858-2863 (2016-03-02)
Two Plasmodium PI4 kinase (PI4K) inhibitors, KDU691 and LMV599, were selected for in vivo testing as causal prophylactic and radical-cure agents for Plasmodium cynomolgi sporozoite-infected rhesus macaques, based on their in vitro activity against liver stages. Animals were infected with
Laurent Dembele et al.
Antimicrobial agents and chemotherapy, 62(5) (2018-03-14)
Artemisinin (ART) resistance has spread through Southeast Asia, posing a serious threat to the control and elimination of malaria. ART resistance has been associated with mutations in the Plasmodium falciparum kelch-13 (Pfk13) propeller domain. Phenotypically, ART resistance is defined as
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