目录号 | 产品详情 | 靶点 | |
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TMIH-0028 | |||
2-(1-(methyl-d3)-1H-imidazol-4-yl)ethan-1-amine 2HCl 是 2-(1-(methyl)-1H-imidazol-4-yl)ethan-1-amine 2HCl 的氘代化合物。2-(1-(methyl)-1H-imidazol-4-yl)ethan-1-amine 2HCl 的 CAS 号为 6481-48-7。1-Methylhistamine dihydrochloride 是组胺代谢物。 | |||
T83921 | |||
IMCTA-C14是一种洗涤剂且是微生物代谢产物4-糖腺苷的衍生物。其临界胶束浓度(CMC)为0.11 mM,亲水亲油平衡(HLB)值为9.72。IMCTA-C14(0.05%和0.5%)能从OVK18卵巢癌细胞提取蛋白质,包括膜蛋白。它对几种不同菌株具有活性(MICs = 8-128 µg/ml),并对52种癌细胞系具有细胞毒性(IC50s = 2.9-29.2 µg/ml)。IMCTA-C14(50 µM)诱导OVK18细胞的自噬。 | |||
T83868 | |||
(±)13,14-EDT是一种氧脂和腎上腺酸的代谢产物,通过细胞色素P450(CYP)途径形成。在50 nM的浓度下,它能激活分离的大鼠冠状小动脉平滑肌细胞中的大导电钙激活钾通道(KCa1.1/BK),并导致分离的猪小动脉扩张(EC50 = 12 pM)。(±)13,14-EDT还能使用TP受体激动剂U-46619预收缩的分离牛冠状动脉放松。 | |||
T36489 | |||
Malformin A is a cyclopentapeptide fungal metabolite that has been found in A. niger and has diverse biological activities. It is a plant growth regulator that induces malformations in plant structure. Malformin A inhibits replication of tobacco mosaic virus (TMV) in local lesion and leaf-disc assays (IC50s = 19.7 and 45.4 μg/ml, respectively). It is cytotoxic to NCI-H460, MIA PaCa-2, MCF-7, SF-268, and WI-38 cancer cells (IC50s = 70, 50, 100, 70, and 100 nM, respectively), inhibits proliferation of PC3 and LNCaP cells (IC50s = 130 and 90 nM, respectively), and induces apoptosis and necrosis in PC3 and LNCaP cells. Malformin A also increases the accumulation of reactive oxygen species, decreases the mitochondrial membrane potential, and induces autophagy in PC3 and LNCaP cells. It is toxic to mice when administered intraperitoneally (LD50 = 3.1 mg/kg) but not orally up to doses of 50 mg/kg. | |||
T83766 | |||
Moexiprilat是一种血管紧张素转换酶(ACE; IC50 = 2.1 nM)的抑制剂,也是前药moexipril的一种活性代谢产物。通过侧链酯水解作用,在体内从moexipril转化而来。Moexiprilat (10 nM)能防止初生大鼠心脏成纤维细胞在雌激素或血管紧张素II刺激下的增殖。在以每天50 mg/kg剂量给药的去卵巢小鼠中,降低平均动脉血压,并增加心房钠尿肽水平,这是高血压的一个标志。 | |||
T35676 | |||
17β-hydroxy Exemestane is the primary active metabolite of exemestane . It is formed by metabolism of exemestane by the cytochrome P450 (CYP) isoforms CYP1A and CYP4A11. 17β-hydroxy Exemestane is an aromatase inhibitor (IC50 = 69 nM using human placental microsomes) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). It stimulates growth of AR- and ERα-positive MCF-7 (EC50 = 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1,500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7aro cells in a concentration-dependent manner. 17β-hydroxy Exemestane (20 mg/kg) inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae, in ovariectomized rats. | |||
T35751 | |||
Violacein is a bacterial metabolite originally isolated from C. violaceum that has antibacterial and antiprotozoal activities.[1] [2] It is produced by C. violaceum as a purple pigment in response to N-hexanoyl homoserine lactone , a property that has been modified to create a strain of C. violaceum used in detecting quorum-sensing molecules.[3] Violacein is active against Gram-positive bacteria, including B. subtilis and S. aureus (MICs = 0.8 and 1.6 µM, respectively). It is also active against P. falciparum, including chloroquine-susceptible and -resistant strains (IC50s = 0.85 and 0.63 µM, respectively).[2] It reduces parasitemia in a mouse model of nonlethal P. chabaudi chabaudi infection when administered at a dose of 7.5 mg/kg and increases survival in a mouse model of lethal P. chabaudi chabaudi infection. Violacein permeabilizes the cytoplasmic membrane of bacterial cells but does not affect the cell wall.[1] | |||
T37488 | |||
Protectin D1 (also known as neuroprotectin D1 when produced in neuronal tissues) is a DHA-derived dihydroxy fatty acid that exhibits potent protective and anti-inflammatory activities. 10(S),17(S)-DiHDHA is a DHA metabolite, also referred to as protectin DX (PDX). It is produced by an apparent double lipoxygenase (LO)-mediated reaction in murine peritonitis exudates, in suspensions of human leukocytes, or by soybean 15-LO incubated with DHA. It differs from protectin D1 with respect to the stereochemistry of the C-10 hydroxyl and the double bond configuration at the 13 and 15 positions. 10(S),17(S)-DiHDHA blocks neutrophil infiltration in murine peritonitis by 20-25% at a dose of 1 ng/mouse. It also inhibits platelet activation by both impairing thromboxane (TX) synthesis and TX receptor activation. | |||
T37215 | |||
5α,6β-Dihydroxycholestanol is an oxysterol metabolite of cholesterol formed from conversion of cholesterol epoxides by 5,6-epoxysterol hydrolase. It inhibits NMDA-mediated calcium influx in HEK293 cells expressing NR1/NR2B NMDA receptors in a concentration-dependent manner. It also binds to voltage-gated sodium (Nav) channels and decreases action potentials in hippocampal neurons in vitro when used at a concentration of 10 uM. It increases survival of spinal cord motoneurons, cortical neurons, and cerebellar granule neurons in vitro when used at concentrations ranging from 5 to 15 uM. 5α,6β-Dihydroxycholestanol is neuroprotective in a rat model of cerebral ischemia when administered at a dose of 12 mg/kg and increases latency to seizure onset and reduces severity of seizures induced by pentylenetetrazole in rats. 5α,6β-Dihydroxycholestanol has been used as a replacement for cholesterol in the study of cholesterol binding proteins. | |||
T37305 | |||
The lipoxins are trihydroxy fatty acids containing a 7,9,11,13-conjugated tetraene. Lipoxin A4 (LXA4) was first described as a metabolite of 15-HpETE and/or 15-HETE when added in vitro to isolated human leukocytes. The material obtained in this manner consists of at least four distinct isomers: 5(S), 6(S); 5(S), 6(R); and the 11-trans and 11-cis isomers of each of these. 6(S)-LXA4 is one of the original four metabolites first identified by Serhan, Nicolaou, and Samuelsson. It was considered to be an artifact by these authors because it lacked the potency of the 5(S),6(R) isomer with respect to contraction of isolated guinea pig lung parenchymal strips. It has not been possible to isolate natural" LXA4 from humans or other mammals in amounts sufficient for determination of absolute stereochemistry. Most authors refer to LXA4 as the 5(S) |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPH-00844 | HSD11B2 Protein, Human, Recombinant (His) | Human | P. pastoris (Yeast) | ||
Catalyzes the conversion of cortisol to the inactive metabolite cortisone. Modulates intracellular glucocorticoid levels, thus protecting the nonselective mineralocorticoid receptor from occupation by glucocorticoids. HSD11B2 Protein, Human, Recombinant (His) is expressed in yeast with N-6xHis tag. The predicted molecular weight is 46.1 kDa and the accession number is P80365.
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TMPY-03414 | ABHD10 Protein, Human, Recombinant (aa 53-306, His) | Human | Baculovirus Insect Cells | ||
Mycophenolic acid (MPA), the active metabolite of the immunosuppressant mycophenolate mofetil (MMF), is primarily metabolized by glucuronidation to a phenolic glucuronide (MPAG) and an acyl glucuronide (AcMPAG). It is known that AcMPAG, which may be an immunotoxic metabolite, is deglucuronidated in human liver. AcMPAG deglucuronidation activity was detected in both human liver cytosol (HLC) and microsomes (HLM). By purification from HLC with column chromatographic purification steps, the enzyme responsible for AcMPAG deglucuronidationis identified as α/β hydrolase domain containing 1 (ABHD1). Recombinant ABHD1 expressed in Sf9 cells efficiently deglucuronidated AcMPAG with a K(m) value of 1.7 ± 1.2 μM, which was similar to those in HLM, HLC, and human liver homogenates (HLH). Immunoblot analysis revealed ABHD1 protein expression in both HLC and HLM. The AcMPAG deglucuronidation by recombinant ABHD1, HLC, and HLH were potently inhibited by AgNO(3), CdCl(2), CuCl(2), PMSF, bis-p-nitrophenylphosphate, and DTNB. The CL(int) value of AcMPAG formation from MPA, which was catalyzed by human UGT2B7, in HLH was increased by 1.8-fold in the presence of PMSF. Thus, human ABHD1 would affect the formation of AcMPAG, the immunotoxic metabolite.
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TMPH-00843 | HSD11B1 Protein, Human, Recombinant (His & SUMO) | Human | E. coli | ||
Catalyzes reversibly the conversion of cortisol to the inactive metabolite cortisone. Catalyzes reversibly the conversion of 7-ketocholesterol to 7-beta-hydroxycholesterol. In intact cells, the reaction runs only in one direction, from 7-ketocholesterol to 7-beta-hydroxycholesterol. HSD11B1 Protein, Human, Recombinant (His & SUMO) is expressed in E. coli expression system with N-6xHis-SUMO tag. The predicted molecular weight is 45.5 kDa and the accession number is P28845.
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TMPY-00320 | APOA1BP Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
APOA1BP, now renamed NAXE, encodes an epimerase essential in the cellular metabolite repair for NADHX and NADPHX. The enzyme catalyzes the epimerization of NAD(P)HX, thereby avoiding the accumulation of toxic metabolites.Pathogenic biallelic mutations in NAXE in children from four families with (sub-) acute-onset ataxia, cerebellar edema, spinal myelopathy, and skin lesions.
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TMPH-02615 | CBS Protein, Mouse, Recombinant (His) | Mouse | E. coli | ||
Hydro-lyase catalyzing the first step of the transsulfuration pathway, where the hydroxyl group of L-serine is displaced by L-homocysteine in a beta-replacement reaction to form L-cystathionine, the precursor of L-cysteine. This catabolic route allows the elimination of L-methionine and the toxic metabolite L-homocysteine. Also involved in the production of hydrogen sulfide, a gasotransmitter with signaling and cytoprotective effects on neurons.
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TMPH-01597 | KYAT1 Protein, Human, Recombinant (His & SUMO) | Human | E. coli | ||
Catalyzes the irreversible transamination of the L-tryptophan metabolite L-kynurenine to form kynurenic acid (KA), an intermediate in the tryptophan catabolic pathway which is also a broad spectrum antagonist of the three ionotropic excitatory amino acid receptors among others. Also metabolizes the cysteine conjugates of certain halogenated alkenes and alkanes to form reactive metabolites. Catalyzes the beta-elimination of S-conjugates and Se-conjugates of L-(seleno)cysteine, resulting in the cleavage of the C-S or C-Se bond.
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TMPY-02420 | HEMK2 Protein, Human, Recombinant (His) | Human | E. coli | ||
N6AMT1 (N-6 Adenine-Specific DNA Methyltransferase 1) is a Protein Coding gene. 2 alternatively spliced human isoforms have been reported. This gene encodes an N(6)-adenine-specific DNA methyltransferase. It belongs to the eukaryotic/archaeal PrmC-related family. The encoded enzyme may be involved in the methylation of release factor I during translation termination. N6AMT1 has a significant role in determining susceptibility to arsenic toxicity and carcinogenicity because of its specific activity in methylating MMAIII to DMA and other unknown mechanisms. N6AMT1 methylates the toxic inorganic arsenic (iAs) metabolite, monomethylarsonous acid (MMA), to the less toxic dimethylarsinic acid (DMA). N6AMT1 polymorphisms were associated with arsenic methylation in Andean women, independent of AS3MT.
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