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Merck
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SML2375

Sigma-Aldrich

KDU691

≥98% (HPLC)

同義詞:

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

經驗公式(希爾表示法):
C22H18ClN5O2
CAS號碼:
分子量::
419.86
MDL號碼:
分類程式碼代碼:
12352200

化驗

≥98% (HPLC)

形狀

powder

顏色

white to brown

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

2-8°C

SMILES 字串

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

生化/生理作用

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.

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


分析證明 (COA)

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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
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
Pamela A Magistrado et al.
ACS infectious diseases, 2(11), 816-826 (2016-12-10)
MMV007564 is a novel antimalarial benzimidazolyl piperidine chemotype identified in cellular screens. To identify the genetic determinant of MMV007564 resistance, parasites were cultured in the presence of the compound to generate resistant lines. Whole genome sequencing revealed distinct mutations in
Nil Gural et al.
Cell host & microbe, 23(3), 395-406 (2018-02-27)
The unique relapsing nature of Plasmodium vivax infection is a major barrier to malaria eradication. Upon infection, dormant liver-stage forms, hypnozoites, linger for weeks to months and then relapse to cause recurrent blood-stage infection. Very little is known about hypnozoite
L Dembele et al.
Scientific reports, 7(1), 2325-2325 (2017-05-26)
Malaria control and elimination are threatened by the emergence and spread of resistance to artemisinin-based combination therapies (ACTs). Experimental evidence suggests that when an artemisinin (ART)-sensitive (K13 wild-type) Plasmodium falciparum strain is exposed to ART derivatives such as dihydroartemisinin (DHA)

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