目录号 | 产品详情 | 靶点 | |
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T38269 | |||
Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM. Purfalcamine has antimalarial activity and causes malaria parasites developmental arrest at the schizont stage[1][2]. Purfalcamine has low activity against Toxoplasma gondii calcium-dependent protein kinase 3 (TgCDPK3)[1]. Purfalcamine (225, 450 nM) has no effect on the parasitemia in the first 32 hours. After about 40 hours, parasite level remains stable and then begins dropping[1]. Purfalcamine inhibits proliferation with EC50s of 171-259 nM for P. falciparum strains (3D7, Dd2, FCB, HB3 and W2), which indicates effectiveness against drug-resistant parasites[1]. Given that the EC50 value for P. falciparum (3D7) is 230 nM, Purfalcamine shows a therapeutic window ranging from 23-fold to 36-fold (EC50s for CHO=12.33 μM, HEp2=7.235 μM, HeLa=7.029 μM and Huh7=5.476 μM)[1]. Purfalcamine (10 mg/kg; oral gavage; BID; for 6 days) demonstrates a delay in the onset of parasitemia in treated mice[1]. Purfalcamine (20 mg/kg; orally gavage) exhibits a Cmax of 2.6 μM with a half-life of 3.1 hours[1]. Animal Model: Male BALB/c mice, 7 weeks of age with the malaria parasite[1] [1]. Nobutaka Kato, et al. Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility. Nat Chem Biol. 2008 Jun;4(6):347-56. [2]. Rajshekhar Y Gaji, et al. Expression of the essential Kinase PfCDPK1 from Plasmodium falciparum in Toxoplasma gondii facilitates the discovery of novel antimalarial drugs. Antimicrob Agents Chemother. 2014 May;58(5):2598-607. | |||
T78184 | |||
MMV009085是一种针对恶性疟原虫己糖转运体PfHT1的特异性抑制剂,具有潜在的抗疟效果。它同时抑制人葡萄糖转运蛋白,强效抑制葡萄糖吸收(IC50:2.6 μM)及恶性疟原虫3D7株的生长(EC50:1.23±0.04 μM)。 | |||
T63635 | |||
Quinate 是抗心律失常剂,是有效的、选择性的、口服具有活力的细胞色素 P450db (cytochrome P450db) 抑制剂,是一种有效的 K+通道 (K+channel) 阻断剂 (IC50: 19.9 μM)。Quinate 也能够用于研究疟疾。 | |||
T72547 | |||
Plm IV inhibitor-2 是一种有效的Plm IV 抑制剂,对Plm IV、II 和 I 的IC50分别为24 nM、70 nM 和 0.3 μM。适用于研究Plasmodium 寄生虫引起的疟疾。 | |||
T64286 | |||
Quinidine polygalacturonate 是一种有效的、选择性的、口服具有活力的细胞色素 P450db (cytochrome P450db) 抑制剂,也是一种有效的 K+通道 (K+channel) 阻断剂,其 IC50值为 19.9 μM,也能够诱导凋亡。Quinidine polygalacturonate 是一种抗心律失常剂,也能够用于研究疟疾。 | |||
T60893 | |||
Ep vinyl quinidine (3-Epiquinine) 是Quinidine 的一种乙烯基立体异构体。Quinidine 可用于研究疟疾,也是一种抗心律失常剂。Quinidine 是口服有效的、选择性细胞色素 P450db 抑制剂,以及钾通道的有效阻断剂,IC50值为 19.9 μM。 | |||
T79633 | Parasite | ||
Antileishmanial agent-22 (compound 15b)是一种抗寄生虫和抗菌化合物,展示了对抗利什曼病、疟疾和结核病的活性。该化合物通过抗叶酸途径抑制利什曼原虫(IC50=0.408 μM)。在100 μM浓度时,Antileishmanial agent-22对叶酸和亚叶酸的抑制率分别达到88%和94%。在体内,以48.4 μM/kg/day剂量对伯氏疟原虫展示96.67%的抑制效果;在体外,其IC50值为0.038 μM。Antileishmanial agent-22还能抑制结核分枝杆菌,MIC值为28.44 μM。 | |||
T74247 | |||
TPE-MI(Tetraphenylethene maleimide)在与马来酰亚胺与硫醇反应前不具荧光性。在与游离的半胱氨酸硫醇标记时,其荧光被激活,后者多在球形蛋白质的核心,仅在展开时显露。TPE-MI适用于测量细胞中未折叠蛋白质的负荷,并能在亨廷顿病诱导的多能干细胞模型中监测蛋白质平衡失衡,以及在形成可见聚合体之前,监测转染突变亨廷顿外显子1的细胞的状况。此外,TPE-MI用于检测双氢青蒿素处理后疟疾寄生虫的蛋白质损伤。应暗处储存。 | |||
T36649 | |||
AN3661, a potent antimalarial lead compound, targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue subunit 3 (PfCPSF3). AN3661 inhibits Plasmodium falciparum laboratory-adapted strains, Ugandan field isolates, and murine P. berghei and P. falciparum infections[1]. AN3661 is active at nanomolar (IC50=20-56 nM) concentrations against P. falciparum laboratory strains known to be sensitive (3D7) or resistant (W2, Dd2, K1, HB3, FCR3 and TM90C2B), and AN3661 is similarly active in ex vivo studies of fresh Ugandan field isolates (mean ex vivo IC50=64 nM). AN3661 shows minimal cytotoxicity against mammalian cell lines, with the CC50 60.5 μM against Jurkat cells, and all other CC50 values greater than the highest concentrations tested (25 μM or above)[1].AN3661 inhibits the stability of P. falciparum transcripts[1]. AN3661 (50-200 mg.kg; p.o.; daily for 4 days) inhibits murine P. berghei infections with ED90 (4 days) 0.34 mg/kg[1].AN3661 is administered orally for 4 days, beginning on the third day of infection, the ED90 4 days after initiation of treatment is 0.57 mg/kg[1]. Animal Model: P. berghei-infected mice (malaria model)[1] [1]. Sonoiki E, et al. A potent antimalarial benzoxaborole targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue. Nat Commun. 2017;8:14574. Published 2017 Mar 6. |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-04180 | PfLDH Protein, P. falciparum, Recombinant (His) | P. falciparum | E. coli | ||
Plasmodium falciparum lactate dehydrogenase (PfLDH) is a key enzyme for energy generation of malarial parasites and is considered to be a potential antimalarial target. The ability of PfLDH- or PfIDEh-based immuno-PCR assays to detect <1 parasite/microL suggests that improvements of bound antibody sensor technology may greatly increase the sensitivity of malaria rapid diagnostic tests. The PfLDH test could be used to detect failures and, therefore, to assess anti-malarial efficacy.
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TMPY-01445 | CD36 Protein, Mouse, Recombinant (His) | Mouse | HEK293 | ||
The cluster of differentiation (CD) system is commonly used as cell markers in Immunophenotyping. Different kinds of cells in the immune system can be identified through the surface CD molecules associating with the immune function of the cell. There are more than 320 CD unique clusters and subclusters have been identified. Some of the CD molecules serve as receptors or ligands important to the cell through initiating a signal cascade which then alter the behavior of the cell. Some CD proteins do not take part in cell signal process but have other functions such as cell adhesion. Cluster of differentiation 36 (CD36), also known as FAT, SCARB3, GP88, glycoprotein IV (gpIV) and glycoprotein IIIb (gpIIIb), is a member of the CD system as well as the class B scavenger receptor family of cell surface proteins. CD36 can be found on the surface of many cell types in vertebrate animals and it consists of 472 amino acids and is extensively glycosylated. It is an integral membrane protein primarily serving as receptors for thrombospondin and collagen and by the erythrocytes infected with the human malaria parasite. The role of CD36 as a cell surface receptor has been extended to that of a signal transduction molecule.
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TMPY-01282 | CD36 Protein, Human, Recombinant (His) | Human | HEK293 | ||
The cluster of differentiation (CD) system is commonly used as cell markers in Immunophenotyping. Different kinds of cells in the immune system can be identified through the surface CD molecules associating with the immune function of the cell. There are more than 320 CD unique clusters and subclusters have been identified. Some of the CD molecules serve as receptors or ligands important to the cell through initiating a signal cascade which then alter the behavior of the cell. Some CD proteins do not take part in cell signal process but have other functions such as cell adhesion. Cluster of differentiation 36 (CD36), also known as FAT, SCARB3, GP88, glycoprotein IV (gpIV) and glycoprotein IIIb (gpIIIb), is a member of the CD system as well as the class B scavenger receptor family of cell surface proteins. CD36 can be found on the surface of many cell types in vertebrate animals and it consists of 472 amino acids and is extensively glycosylated. It is an integral membrane protein primarily serving as receptors for thrombospondin and collagen and by the erythrocytes infected with the human malaria parasite. The role of CD36 as a cell surface receptor has been extended to that of a signal transduction molecule.
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TMPY-04765 | PKLR Protein, Human, Recombinant (His) | Human | E. coli | ||
Pyruvate kinase (PKLR) is a critical erythrocyte enzyme that is required for glycolysis and production of ATP. Pyruvate kinase deficiency (PKD) is the most frequent red blood cell enzyme abnormality of the glycolytic pathway and the most common cause of hereditary nonspherocytic hemolytic anemia. Over 250 PKLR-gene mutations have been described, including missense/nonsense, splicing and regulatory mutations, small insertions, small and gross deletions, causing PKD and hemolytic anemia of variable severity. PKLR expression was increased in liver metastases as well as in primary colorectal tumors of patients with metastatic disease. PKLR protein variants may affect the frequency, and the intensity of malaria episodes induced by different Plasmodium parasites in humans living in areas of endemic malaria.
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TMPY-02895 | IgG3 Protein, Human, Recombinant | Human | HEK293 | ||
IGHG3 (Immunoglobulin Heavy Constant Gamma 3 (G3m Marker), also known as IgG3) is a Protein Coding gene. Ig gamma-3 chain C region is a protein that in humans is encoded by the IGHG3 gene. Immunoglobulins, also known as antibodies, are membrane-bound or secreted glycoproteins produced by B lymphocytes. In the recognition phase of humoral immunity, the membrane-bound immunoglobulins serve as receptors which, upon binding of a specific antigen, trigger the clonal expansion and differentiation of B lymphocytes into immunoglobulins-secreting plasma cells. Murine immunoglobulin G (IgG) plays an important role in mediating protective immune responses to malaria. Diseases associated with IGHG3 include Heavy Chain Disease and Gamma Heavy Chain Disease. Among its related pathways are IL4-mediated signaling events and the Creation of C4 and C2 activators.
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TMPY-03399 | KLHL2 Protein, Human, Recombinant (GST) | Human | E. coli | ||
KLHL2 (Kelch Like Family Member 2) is a Protein Coding gene. 3 alternatively spliced human isoforms have been reported. KLHL2 contains 1 BTB (POZ) domain and 6 Kelch repeats. It is widely expressed in the brain, esophagus, and other tissues. KLHL2 gene has been proposed to participate in intracellular protein transportation. KLHL2 is expected to have molecular functions such as transporter activity, actin-binding, and protein binding. KLHL2 localizes in various compartments such as actin cytoskeleton, cytoplasm, membrane, and nucleus. It may also play a role in organizing the actin cytoskeleton of the brain cells. Diseases associated with KLHL2 include Mixed Malaria and Inclusion Body Myopathy With Early-Onset Paget Disease Of Bone With Or Without Frontotemporal Dementia 2.
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TMPY-02696 | IgG3 Protein, Mouse, Recombinant | Mouse | HEK293 | ||
IGHG3 (Immunoglobulin Heavy Constant Gamma 3 (G3m Marker), also known as IgG3) is a Protein Coding gene. Ig gamma-3 chain C region is a protein that in humans is encoded by the IGHG3 gene. Immunoglobulins, also known as antibodies, are membrane-bound or secreted glycoproteins produced by B lymphocytes. In the recognition phase of humoral immunity, the membrane-bound immunoglobulins serve as receptors which, upon binding of a specific antigen, trigger the clonal expansion and differentiation of B lymphocytes into immunoglobulins-secreting plasma cells. Murine immunoglobulin G (IgG) plays an important role in mediating protective immune responses to malaria. Diseases associated with IGHG3 include Heavy Chain Disease and Gamma Heavy Chain Disease. Among its related pathways are IL4-mediated signaling events and the Creation of C4 and C2 activators.
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TMPY-03985 | Adenosine Deaminase Protein, Human, Recombinant (His) | Human | Baculovirus-Insect Cells | ||
Adenosine Desaminase (ADA) deficiency, is a purine metabolic disorder that cause severe combined immunodeficiency (SCID) due to the accumulation of toxic metabolites that primarily affects development, differentiation and function of T and B lymphocytes. Adenosine deaminase is a polymorphic enzyme that has an important role in immune functions and in the regulation of intracellular and extracellular concentrations of adenosine and adenosine receptor activity. ADA activity might be considered as a useful diagnostic tool among the other markers in these diseases. Genetic variability of ADA activity may have, therefore, an important role in resistance to malaria. Adenosine Deaminase (ADA) deficiency is an autosomal recessive variant of severe combined immunodeficiency (SCID) caused by systemic accumulation of ADA substrates.
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TMPY-03479 | CD36 Protein, Rhesus, Recombinant (hFc) | Rhesus | HEK293 | ||
The cluster of differentiation (CD) system is commonly used as cell markers in Immunophenotyping. Different kinds of cells in the immune system can be identified through the surface CD molecules associating with the immune function of the cell. There are more than 320 CD unique clusters and subclusters have been identified. Some of the CD molecules serve as receptors or ligands important to the cell through initiating a signal cascade which then alter the behavior of the cell. Some CD proteins do not take part in cell signal process but have other functions such as cell adhesion. Cluster of differentiation 36 (CD36), also known as FAT, SCARB3, GP88, glycoprotein IV (gpIV) and glycoprotein IIIb (gpIIIb), is a member of the CD system as well as the class B scavenger receptor family of cell surface proteins. CD36 can be found on the surface of many cell types in vertebrate animals and it consists of 472 amino acids and is extensively glycosylated. It is an integral membrane protein primarily serving as receptors for thrombospondin and collagen and by the erythrocytes infected with the human malaria parasite. The role of CD36 as a cell surface receptor has been extended to that of a signal transduction molecule.
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TMPY-03242 | CD36 Protein, Rat, Recombinant (hFc) | Rat | HEK293 | ||
The cluster of differentiation (CD) system is commonly used as cell markers in Immunophenotyping. Different kinds of cells in the immune system can be identified through the surface CD molecules associating with the immune function of the cell. There are more than 320 CD unique clusters and subclusters have been identified. Some of the CD molecules serve as receptors or ligands important to the cell through initiating a signal cascade which then alter the behavior of the cell. Some CD proteins do not take part in cell signal process but have other functions such as cell adhesion. Cluster of differentiation 36 (CD36), also known as FAT, SCARB3, GP88, glycoprotein IV (gpIV) and glycoprotein IIIb (gpIIIb), is a member of the CD system as well as the class B scavenger receptor family of cell surface proteins. CD36 can be found on the surface of many cell types in vertebrate animals and it consists of 472 amino acids and is extensively glycosylated. It is an integral membrane protein primarily serving as receptors for thrombospondin and collagen and by the erythrocytes infected with the human malaria parasite. The role of CD36 as a cell surface receptor has been extended to that of a signal transduction molecule.
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TMPY-01449 | CD36 Protein, Mouse, Recombinant (His & hFc) | Mouse | HEK293 | ||
The cluster of differentiation (CD) system is commonly used as cell markers in Immunophenotyping. Different kinds of cells in the immune system can be identified through the surface CD molecules associating with the immune function of the cell. There are more than 320 CD unique clusters and subclusters have been identified. Some of the CD molecules serve as receptors or ligands important to the cell through initiating a signal cascade which then alter the behavior of the cell. Some CD proteins do not take part in cell signal process but have other functions such as cell adhesion. Cluster of differentiation 36 (CD36), also known as FAT, SCARB3, GP88, glycoprotein IV (gpIV) and glycoprotein IIIb (gpIIIb), is a member of the CD system as well as the class B scavenger receptor family of cell surface proteins. CD36 can be found on the surface of many cell types in vertebrate animals and it consists of 472 amino acids and is extensively glycosylated. It is an integral membrane protein primarily serving as receptors for thrombospondin and collagen and by the erythrocytes infected with the human malaria parasite. The role of CD36 as a cell surface receptor has been extended to that of a signal transduction molecule.
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TMPY-03243 | CD36 Protein, Rat, Recombinant (His) | Rat | HEK293 | ||
The cluster of differentiation (CD) system is commonly used as cell markers in Immunophenotyping. Different kinds of cells in the immune system can be identified through the surface CD molecules associating with the immune function of the cell. There are more than 320 CD unique clusters and subclusters have been identified. Some of the CD molecules serve as receptors or ligands important to the cell through initiating a signal cascade which then alter the behavior of the cell. Some CD proteins do not take part in cell signal process but have other functions such as cell adhesion. Cluster of differentiation 36 (CD36), also known as FAT, SCARB3, GP88, glycoprotein IV (gpIV) and glycoprotein IIIb (gpIIIb), is a member of the CD system as well as the class B scavenger receptor family of cell surface proteins. CD36 can be found on the surface of many cell types in vertebrate animals and it consists of 472 amino acids and is extensively glycosylated. It is an integral membrane protein primarily serving as receptors for thrombospondin and collagen and by the erythrocytes infected with the human malaria parasite. The role of CD36 as a cell surface receptor has been extended to that of a signal transduction molecule.
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TMPY-06951 | CD36 Protein, Human, Recombinant (His & Avi), Biotinylated | Human | HEK293 | ||
The cluster of differentiation (CD) system is commonly used as cell markers in Immunophenotyping. Different kinds of cells in the immune system can be identified through the surface CD molecules associating with the immune function of the cell. There are more than 320 CD unique clusters and subclusters have been identified. Some of the CD molecules serve as receptors or ligands important to the cell through initiating a signal cascade which then alter the behavior of the cell. Some CD proteins do not take part in cell signal process but have other functions such as cell adhesion. Cluster of differentiation 36 (CD36), also known as FAT, SCARB3, GP88, glycoprotein IV (gpIV) and glycoprotein IIIb (gpIIIb), is a member of the CD system as well as the class B scavenger receptor family of cell surface proteins. CD36 can be found on the surface of many cell types in vertebrate animals and it consists of 472 amino acids and is extensively glycosylated. It is an integral membrane protein primarily serving as receptors for thrombospondin and collagen and by the erythrocytes infected with the human malaria parasite. The role of CD36 as a cell surface receptor has been extended to that of a signal transduction molecule.
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