SML2375
KDU691
≥98% (HPLC)
别名:
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
登录 查看组织和合同定价。
选择尺寸
关于此项目
经验公式（希尔记法）:
C22H18ClN5O2
化学文摘社编号:
分子量:
419.86
UNSPSC Code:
12352200
MDL number:
NACRES:
NA.21
InChI
1S/C22H18ClN5O2/c1-24-21(29)15-5-3-14(4-6-15)19-11-26-20-12-25-18(13-28(19)20)22(30)27(2)17-9-7-16(23)8-10-17/h3-13H,1-2H3,(H,24,29)
InChI key
TYMFFISSODJRDV-UHFFFAOYSA-N
SMILES string
O=C(N(C1=CC=C(Cl)C=C1)C)C(N=C2)=CN3C2=NC=C3C4=CC=C(C(NC)=O)C=C4
assay
≥98% (HPLC)
form
powder
color
white to brown
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
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.
Orally active antiparasitic (antimalarial & anti-cryptosporidial), Plasmodium & Cryptosporidium phosphatidylinositol-4-OH kinase, PI(4)K, inhibitor.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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
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)
Koen J Dechering et al.
Scientific reports, 7(1), 17680-17680 (2017-12-17)
Eradication of malaria requires a novel type of drug that blocks transmission from the human to the mosquito host, but selection of such a drug is hampered by a lack of translational models. Experimental mosquito infections yield infection intensities that
Case W McNamara et al.
Nature, 504(7479), 248-253 (2013-11-29)
Achieving the goal of malaria elimination will depend on targeting Plasmodium pathways essential across all life stages. Here we identify a lipid kinase, phosphatidylinositol-4-OH kinase (PI(4)K), as the target of imidazopyrazines, a new antimalarial compound class that inhibits the intracellular
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
我们的科学家团队拥有各种研究领域经验，包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.
联系客户支持