目录号 | 产品详情 | 靶点 | |
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T75733 | |||
Saralasin ([Sar1,Ala8] Angiotensin II) TFA,血管紧张素 II (angiotensin II) 的八肽衍生物,作为竞争性血管紧张素 II 受体 (angiotensin II receptor) 拮抗剂,其Ki值达0.32 nM(涵盖74%的结合位点),显示出部分激动剂特性。适应于肾血管性高血压、肾素依赖性(血管紧张素原性)高血压的研究。 | |||
T60348 | |||
N1,N11-Diethylnorspermine (DENSPM) 是一种有效的抗癌剂。N1,N11-Diethylnorspermine 是一种精胺类似物,可激活多胺分解代谢。N1,N11-Diethylnorspermine 诱导细胞色素 c 从线粒体中释放,导致 caspase 3的激活。N1,N11-Diethylnorspermine 通过诱导亚精胺/精胺 N1- 乙酰转移酶 (SSAT) 结合产生过氧化氢杀灭多形胶质母细胞瘤 (GBM) 细胞。 | |||
T81115 | |||
sPLA2-IIA Inhibitor 是 FLSYK 的环状五肽类似物,具有环2-Nal-Leu-Ser-2-Nal-Arg (c2) 结构,能够特异性结合 hGIIA(人类 IIA 磷脂酶 A2),有效抑制其酯键水解活性。该化合物作为酯酶超家族的一员,主要作用于甘油磷脂 sn-2 位置的酯键,从而阻断游离脂肪酸和花生四烯酸等物质的释放。 | |||
T38008 | |||
KBC-007 is a synthetic branched chain-containing analog of α-galactosylceramide (α-GalCer). It induces IL-4 and IFN-γ secretion by mouse splenocytes when used at a concentration of 0.5 ng/ml and IL-2 secretion by DN32.D3 NKT hybridoma cells co-cultured with CD1d-transfected RBL cells pre-loaded with KBC-007 at a concentration of 8 ng/ml. KBC-007 (1 μg per animal) increases levels of IL-4, but not IFN-γ, to a similar degree as α-GalCer in mouse serum. KBC-007 (0.5 μg per animal) increases the survival rate of mice immunized with the inactivated influenza A virus A/PR/8/34 in a model of influenza infection. | |||
T37669 | |||
The A1, A2A, A2B, and A3 adenosine receptors (ARs) are ubiquitous G protein-coupled receptors. The four AR subtypes have been implicated in several areas of therapeutic interest such as stroke and other ischemic conditions, as well as inflammation, neurodegenerative diseases, diabetes, and sleep regulation. A3 AR antagonists are of interest as therapeutic agents in glaucoma agents and inflammation. CAY10498 is a potent and selective A3 AR antagonist exhibiting a Ki of 37 nM with 60 and 200-fold selectivity over A1 and A2A adenosine receptors, respectively. CAY10498 is also a structural analog of reversine, a dedifferentiation agent of embryonic progenitor cells. However, no dedifferentiation effects or any connection between A3 AR antagonism and dedifferentiation have been demonstrated. | |||
T38118 | |||
Zanamivir-13C,15N2is intended for use as an internal standard for the quantification of zanamivir by GC- or LC-MS. Zanamivir is a sialic acid analog that inhibits neuraminidase release of newly replicated influenza virus particles.1It has been shown to selectively inhibit the growth of influenza A and B viruses in plaque reduction assays with IC50values ranging from 5 to 14 nM and to directly inhibit influenza A and B virus neuraminidases with IC50values ranging from 0.6 to 7.9 nMin vitro. Intranasal zanamivir administration at 0.4 mg/kg twice daily reduces mortality and viral titers in lung homogenates of mice infected with influenza. 1.Elliott, M.Zanamivir: From drug design to the clinicPhilos. Trans. R. Soc. Lond. B Biol Sci.356(1416)1885-1893(2001) | |||
T60666 | |||
Antibacterial agent 105 (Compound 17) 是一种喹诺酮类的 Phenanthrolinic 类似物。Antibacterial agent 105 对结核分枝杆菌表现出抗菌活性,MIC90值为2.64 μM。此外,Antibacterial agent 105 对不同种类的菌种都表现出抗菌活性,对M. smegmatis,M. aurum,M. marinum,BCG,E. aerogenes 和S. aureus 的 MIC90值分别为 11.18, 11.18,0.70,1.40,44.70 和 22.35 μM。 | |||
T37030 | |||
The phosphatidylinositol (PtdIns) phosphates represent a small percentage of total membrane phospholipids. However, they play a critical role in the generation and transmission of cellular signals. PtdIns-(4)-P1 (1,2-dioctanoyl) is a synthetic analog of natural phosphatidylinositol (PtdIns) featuring C8:0 fatty acids at the sn-1 and sn-2 positions. The compound contains the same inositol and diacylglycerol (DAG) stereochemistry as the natural compound. PtdIns-(4)-P1 can be phosphorylated to di- (PtdIns-P2; PIP2) and triphosphates (PtdIns-P3; PIP3). Hydrolysis of PtdIns-(4,5)-P2 by phosphoinositide (PI)-specific phospholipase C generates inositol triphosphate (IP3) and DAG which are key second messengers in an intricate biochemical signal transduction cascade. | |||
T37342 | |||
Quorum sensing is a regulatory system used by bacteria for controlling gene expression in response to increasing cell density. Controlling bacterial infections by quenching their quorum sensing systems is a promising field of study. The expression of specific target genes, such as transcriptional regulators belonging to the LuxIR family of proteins, is coordinated by synthesis of diffusible acylhomoserine lactone (AHL) molecules. N-butyryl-L-Homocysteine thio-lactone is an analog of N-butyryl-L-homoserine lactone, the small diffusible signaling molecule involved in quorum sensing, thereby controlling gene expression and cellular metabolism. N-butyryl-L-Homocysteine thio-lactone induces violacein expression in C. violaceum mutants usually not able to produce AHLs. | |||
T76305 | |||
[Ala2] Endothelin-3, human 为ET-3的线性类似物,其结构中的Cys残基被Ala所替代。ET-3是由人体横纹肌肉瘤细胞系产生,且仅在此细胞系中表达的一种具有血管活性的肽。在非肌肉来源的肉瘤细胞系中不表达。该肽能够作为旁分泌因子,促进内皮细胞迁移。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPH-03036 | Cytotoxin 2 Protein, Naja atra, Recombinant (His & Myc) | Naja atra | E. coli | ||
Basic protein that binds to cell membrane and depolarizes cardiomyocytes. It also shows lytic activities, but 2-fold less important than that of CTX-A4. It binds to the integrin alpha-V/beta-3 (ITGAV/ITGB3) with a moderate affinity. It may interact with sulfatides in the cell membrane which induces pore formation and cell internalization and is responsible for cytotoxicity in cardiomyocytes. It also may target the mitochondrial membrane and induce mitochondrial swelling and fragmentation.
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TMPH-00645 | Lactose permease Protein, E. coli, Recombinant (His) | E. coli | E. coli | ||
Responsible for transport of beta-galactosides into the cell, with the concomitant import of a proton (symport system). Can transport lactose, melibiose, lactulose or the analog methyl-1-thio-beta,D-galactopyranoside (TMG), but not sucrose or fructose. The substrate specificity is directed toward the galactopyranosyl moiety of the substrate. Lactose permease Protein, E. coli, Recombinant (His) is expressed in E. coli expression system with N-10xHis tag. The predicted molecular weight is 34.4 kDa and the accession number is P02920.
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TMPJ-00871 | BAR Protein, S. hygroscopicus, Recombinant | Streptomyces hygroscopicus | E. coli | ||
Phosphinothricin N-acetyltransferase (PAT) is an enzyme that acetylates the free NH2 group of L-phosphinothricin (L-PPT) in the presence of acetyl-CoA as a co-substrate. It is highly specific for L-PPT and does not acetylate other L-amino acids or structurally similar molecules. L-PPT is a glutamate analog that can inhibit glutamine synthetase activity in plants, resulting in the accumulation of ammonia to toxic levels and impairment of photosynthesis. The introduction of a PAT gene into a plant genome can confer resistance to glufosinate herbicide during post-emergent applications.
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TMPH-03038 | Cobra venom factor Protein, Naja kaouthia, Recombinant (His & SUMO) | Naja kaouthia | E. coli | ||
Complement-activating protein in cobra venom. It is a structural and functional analog of complement component C3b, the activated form of C3. It binds factor B (CFB), which is subsequently cleaved by factor D (CFD) to form the bimolecular complex CVF/Bb. CVF/Bb is a C3/C5 convertase that cleaves both complement components C3 and C5. Structurally, it resembles the C3b degradation product C3c, which is not able to form a C3/C5 convertase. Unlike C3b/Bb, CVF/Bb is a stable complex and completely resistant to the actions of complement regulatory factors H (CFH) and I (CFI). Therefore, CVF continuously activates complement resulting in the depletion of complement activity.
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