目录号 | 产品详情 | 靶点 | |
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T36418 | |||
O-Desmethyl-N-deschlorobenzoyl indomethacin is a metabolite of the non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor indomethacin .1It is formed from indomethacin in isolated rabbit hepatocytes. O-Desmethyl-N-deschlorobenzoyl indomethacin (600 μM) decreases the viability of HL-60 leukemia cells when cultured with glucose oxidase.2It has also been used in the synthesis of prostaglandin D2receptor antagonists.3 1.Evans, M.A., Papazafiratou, C., Bhat, R., et al.Indomethacin metabolism in isolated neonatal and fetal rabbit hepatocytesPediatr. Res.15(11)1406-1410(1981) 2.Morgan, A.G.M., Babu, D., Michail, K., et al.An evaluation of myeloperoxidase-mediated bio-activation of NSAIDs in promyelocytic leukemia (HL-60) cells for potential cytotoxic selectivityToxicol. Lett.28048-56(2017) 3.Torisu, K., Kobayashi, K., Iwahashi, M., et al.Discovery of new chemical leads for prostaglandin D2 receptor antagonistsBioorg. Med. Chem. Lett.14(17)4557-4562(2004) | |||
T37634 | |||
Docosapentaenoic acid (DPA) is a ω-3 fatty acid found in fish oils. 17-oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid is a metabolite of lipoxygenase-mediated oxidation of DPA that is produced endogenously by aspirin-enhanced COX-2 activity. It has been shown to activate Nrf2-dependent antioxidant gene expression, to act as a PPARγ agonist (EC50 = ~200 nM), and to inhibit pro-inflammatory cytokine and nitric oxide production at biological concentration ranges (5-25 μM). | |||
TN1009 | NF-κB NO Synthase Prostaglandin Receptor | ||
Epimagnolin B 是一种双环氧木质素,分离自木兰中。它能够抑制 LPS 激活的小胶质细胞中 NO 的产生。它具有抗过敏以及抗炎作用。 | |||
T37234 | |||
EDHF (endothelium-derived hyperpolarizing factor) is an unidentified mediator released from vascular endothelial cells in response to acetylcholine and bradykinin which is distinct from the NOS- (nitric oxide) and COX-derived (prostacyclin) vasodilators. Cytochrome P450 (CYP450) metabolism of polyunsaturated fatty acids, produces epoxides such as (±)14(15)-EpETrE which are prime candidates for the actual active mediator. However, the CYP450 metabolites of eicosapentaenoic acid and docosahexaenoic acid have been little studied relative to arachidonate epoxygenase metabolites. (±)14(15)-EpETE is the ω-3 homolog of 14(15)-EpETrE, derived via epoxidation of the 14,15-double bond of EPA. The EDHF activity of (±)14(15)-EpETE has not yet been determined. | |||
T69740 | |||
AMG-315 is a Potent Endocannabinoid Ligand with Stability to Metabolizing Enzymes. AMG-315 is a chiral arachidonoyl ethanolamide (AEA) analogue or (13S,1′R)-dimethylanandamide. AMG-315 is a high affinity ligand for the CB1 receptor (Ki of 7.8 ± 1.4 nM) that behaves as a potent CB1 agonist in vitro (EC50 = 0.6 ± 0.2 nM). AMG-315 is the first potent AEA analogue with significant stability for all endocannabinoid hydrolyzing enzymes as well as the oxidative enzymes COX-2. AMG-315 will serve as a very useful endocannabinoid probe. | |||
T68738 | |||
(±)-γ-Tocopherol is a form of vitamin E with antioxidant and anti-inflammatory properties. It traps and detoxifies reactive nitrogen oxide species, including nitrogen dioxide, in cell-free assays. It also reduces the synthesis of prostaglandin E2 (PGE2) induced by LPS in RAW 264.7 macrophages and by IL-1β in A549 cells. (±)-γ-Tocopherol inhibits LPS-induced nitrite release and inducible nitric oxide synthase (iNOS) expression in RAW 264.7 cells and reduces COX-2 activity in A549 cells pretreated with IL-1β. Serum levels of (±)-γ-tocopherol are decreased in patients with cardiovascular disease. | |||
T71288 | |||
Phenylbutazone-d9 is intended for use as an internal standard for the quantification of phenylbutazone by GC- or LC-MS. Phenylbutazone is a non-steroidal anti-inflammatory drug and an inhibitor of the peroxidase activity of COX (IC50 = ~100 µM in the presence of hydrogen peroxide). It also inhibits prostaglandin I synthase (IC50 = ~25 µM in the presence of hydrogen peroxide). Phenylbutazone (2 mg/kg) reduces increases in type II collagen levels in the inflamed joints of an equine model of LPS-induced acute synovitis. Formulations containing phenylbutazone have been used in the treatment of lameness in horses. | |||
TN5248 | NOS COX Prostaglandin Receptor | ||
1β,6α-Dihydroxyeudesm-4(15)-ene (Voleneol,DE) can attenuate the lipopolysaccharide (LPS)-induced inflammation in BV2 microglial cells, it also can dose-dependently suppress the protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenas | |||
T37182 | |||
The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes. AX 048 is a potent group IVA cPLA2 inhibitor that demonstrates 50% inhibition of the enzyme at a mole fraction (XI(50)) of 0.022. Pretreatment with AX 048 (ED50 = 1.2 mg/kg) dose-dependently reduces thermal hyperalgesia evoked by carrageenan injection of rat hind paw. At concentrations as high as 30 μM, AX 048 does not inhibit COX activity or interfere with central cannabinoid receptor signaling. | |||
T36152 | |||
14S(15R)-EET is an oxylipin and a cytochrome P450 metabolite of arachidonic acid .114S(15R)-EET binds to isolated guinea pig monocytes with a Kivalue of 612.5 nM in a competitive binding assay using [3H]14(15)-EET.2It induces dilation of precontracted isolated canine epicardial arterioles (EC50= 4 pM) and denuded porcine subepicardial arterioles (EC50= 3 pM).3Unlike 14R(15S)-EET, 14S(15R)-EET does not inhibit COX in enzyme assays or isolated platelets.4 1.Daikh, B.E., Lasker, J.M., Raucy, J.L., et al.Regio- and stereoselective epoxidation of arachidonic acid by human cytochromes P450 2C8 and 2C91J. Pharmacol. Exp. Ther.271(3)1427-1433(1994) 2.Wong, P.Y.-K., Lai, P.-S., and Falck, J.R.Mechanism and signal transduction of 14 (R), 15 (S)-epoxyeicosatrienoic acid (14,15-EET) binding in guinea pig monocytesProstaglandins Other Lipid Mediat.62(4)321-333(2000) 3.Zhang, Y., Oltman, C.L., Lu, T., et al.EET homologs potently dilate coronary microvessels and activate BKCa channelsAm. J. Physiol. Heart Circ. Physiol.280(6)H2430-H2440(2001) 4.Fitzpatrick, F.A., Ennis, M.D., Baze, M.E., et al.Inhibition of cyclooxygenase activity and platelet aggregation by epoxyeicosatrienoic acidsJ. Biol. Chem.261(2)15334-15338(1986) |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-01736 | COX-2 Protein, Human, Recombinant (His) | Human | Baculovirus Insect Cells | ||
PTGS2, also known as COX-2, is s component of Prostaglandin-endoperoxide synthase (PTGS). PTGS, also known as cyclooxygenase, is the key enzyme in prostaglandin biosynthesis, and acts both as a dioxygenase and as a peroxidase. There are two isozymes of PTGS: a constitutive PTGS1 and an inducible PTGS2, which differ in their regulation of expression and tissue distribution. PTGS2 is overexpressed in many cancers. The overexpression of PTGS2 along with increased angiogenesis and GLUT-1 expression is significantly associated with gallbladder carcinomas. Furthermore the product of COX-2, PGH2 is converted by prostaglandin E2 synthase into PGE2, which in turn can stimulate cancer progression. Consequently inhibiting COX-2 may have benefit in the prevention and treatment of these types of cancer. PTGS2 is regulated by specific stimulatory events, suggesting that it is responsible for the prostanoid biosynthesis involved in inflammation and mitogenesis. It mediates the formation of prostaglandins from arachidonate and may have a role as a major mediator of inflammation and/or a role for prostanoid signaling in activity-dependent plasticity.Cancer ImmunotherapyImmune CheckpointImmunotherapyTargeted Therapy
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TMPH-01179 | COX4I1 Protein, Human, Recombinant (His & SUMO) | Human | E. coli | ||
COX4I1 Protein, Human, Recombinant (His & SUMO) is expressed in E. coli.
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TMPH-01180 | COX5A Protein, Human, Recombinant (GST) | Human | E. coli | ||
COX5A Protein, Human, Recombinant (GST) is expressed in E. coli.
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TMPY-03511 | COX5B Protein, Human, Recombinant (His) | Human | E. coli | ||
Cytochrome C oxidase (COX) is the terminal enzyme of the mitochondrial respiratory chain. It is a multi-subunit enzyme complex that couples the transfer of electrons from cytochrome c to molecular oxygen and contributes to a proton electrochemical gradient across the inner mitochondrial membrane. The complex consists of 13 mitochondrial- and nuclear-encoded subunits. The mitochondrially-encoded subunits perform the electron transfer and proton pumping activities. The functions of the nuclear-encoded subunits are unknown but they may play a role in the regulation and assembly of the complex. This gene encodes the nuclear-encoded subunit Vb of the human mitochondrial respiratory chain enzyme.
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TMPY-03752 | COX4NB Protein, Human, Recombinant (His) | Human | E. coli | ||
COX4NB Protein, Human, Recombinant (His) is expressed in E. coli expression system with His tag. The predicted molecular weight is 25.6 kDa and the accession number is O43402.
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TMPH-02617 | COX5A Protein, Mouse, Recombinant (His & SUMO) | Mouse | E. coli | ||
Component of the cytochrome c oxidase, the last enzyme in the mitochondrial electron transport chain which drives oxidative phosphorylation. The respiratory chain contains 3 multisubunit complexes succinate dehydrogenase (complex II, CII), ubiquinol-cytochrome c oxidoreductase (cytochrome b-c1 complex, complex III, CIII) and cytochrome c oxidase (complex IV, CIV), that cooperate to transfer electrons derived from NADH and succinate to molecular oxygen, creating an electrochemical gradient over the inner membrane that drives transmembrane transport and the ATP synthase. Cytochrome c oxidase is the component of the respiratory chain that catalyzes the reduction of oxygen to water. Electrons originating from reduced cytochrome c in the intermembrane space (IMS) are transferred via the dinuclear copper A center (CU(A)) of subunit 2 and heme A of subunit 1 to the active site in subunit 1, a binuclear center (BNC) formed by heme A3 and copper B (CU(B)). The BNC reduces molecular oxygen to 2 water molecules using 4 electrons from cytochrome c in the IMS and 4 protons from the mitochondrial matrix.
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TMPY-04908 | Coxsackievirus A16 (Cox A16) (strain G-10) VP1 Protein (Fc) | CV | Baculovirus Insect Cells | ||
Coxsackievirus A16 (Cox A16) (strain G-10) VP1 Protein (Fc) is expressed in Baculovirus insect cells with Fc tag. The predicted molecular weight is 59.5 kDa and the accession number is AAA50478.1.
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TMPY-04807 | Coxsackievirus A16 (Cox A16) (strain G-10) VP4 Protein (Fc) | CV | Baculovirus Insect Cells | ||
Coxsackievirus A16 (Cox A16) (strain G-10) VP4 Protein (Fc) is expressed in Baculovirus insect cells with Fc tag. The predicted molecular weight is 32.6 kDa and the accession number is AAA50478.1.
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TMPH-03639 | COX7A1 Protein, Trachypithecus cristatu, Recombinant (hFc) | Trachypithecus cristatus | HEK293 Cells | ||
N/A. COX7A1 Protein, Trachypithecus cristatu, Recombinant (hFc) is expressed in HEK293 mammalian cells with C-hFc tag. The predicted molecular weight is 31.9 kDa and the accession number is Q9N234.
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TMPJ-00704 | SCO1 Protein, Human, Recombinant (GST) | Human | E. coli | ||
Protein SCO1 Homolog, Mitochondrial (SCO1) is a member of the SCO1/2 family. SCO1 has a homodimer structure. SCO1 is located in mitochondrion and is highly expressed in muscle, heart, and brain. It is characterized by high rates of Oxidative Phosphorylation (OxPhos). SCO1 is thought to play a important role in cellular copper homeostasis, mitochondrial redox signaling and insertion of copper into the active site of COX. The defects of SCO1 can result in Mitochondrial Complex IV Deficiency (MT-C4D). A disorder of the mitochondrial respiratory chain has heterogeneous clinical manifestations, ranging from isolated myopathy to severe multisystem disease affecting several tissues and organs.
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TMPY-03658 | ETHE1 Protein, Human, Recombinant (His) | Human | E. coli | ||
ETHE1, also known as HSCO, is a sulfur dioxygenase that localizes within the mitochondrial matrix. ETHE1 probably plays an important role in metabolic homeostasis in mitochondria. It may also function as a nuclear-cytoplasmic shuttling protein that binds transcription factor RELA/NFKB3 in the nucleus and exports it to the cytoplasm. ETHE1 can suppresses p53-induced apoptosis by preventing nuclear localization of RELA. Mutations in ETHE1 gene result in ethylmalonic encephalopathy. Ethylmalonic encephalopathy is an autosomal recessive, invariably fatal disorder characterized by early-onset encephalopathy, microangiopathy, chronic diarrhea, defective cytochrome c oxidase (COX) in muscle and brain, high concentrations of C4 and C5 acylcarnitines in blood and high excretion of ethylmalonic acid in urine.
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