目录号 | 产品详情 | 靶点 | |
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T76565 | |||
PDC31 (THG113.31; ILGHXDYK) 是FPProstaglandin Receptor 的变构和非竞争性抑制剂。PDC31是基于D-氨基酸的寡肽,用作平滑肌收缩剂。PDC31 在体内降低子宫收缩的强度和持续时间,可用于早产和原发性痛经 (PD) 的研究。PDC31 还增强人子宫肌层细胞中 Ca2+依赖性大电导 K+通道。 | |||
T35708 | |||
N-acetyl-5-Aminosalicylic acid is a metabolite of the anti-inflammatory agent 5-aminosalicylic acid and its prodrug form, sulfasalazine . It is formed in the liver, intestinal lumen, and colonic epithelial cells via N-acetyltransferases. It reduces IFN-γ binding to colonic epithelial cells by 24% when used at a concentration of 10 mM. N-acetyl-5-Aminosalicylic acid (100 μM) scavenges 2,2-diphenyl-1-picrylhydrazyl radicals in a cell-free assay and inhibits base hydroxylation in DNA stimulated by hydroxy radicals. Unlike sulfasalazine, N-acetyl-5-aminosalicylic acid does not inhibit 15-hydroxy prostaglandin dehydrogenase (PGDH). Urinary levels of N-acetyl-5-aminosalicylic acid have been used as a marker of 5-ASA adherence in patients with inflammatory bowel disease. | |||
T38208 | |||
Heneicosapentaenoic Acid (HPA) is a 21:5 ω-3 fatty acid present in trace amounts in the green alga B. pennata and in fish oils. Its chemical composition is similar to eicosapentaenoic acid (EPA) except elongated with one carbon on the carboxyl end, placing the first double bond in the δ6 position. HPA can be used to study the significance of the position of the double bonds in ω-3 fatty acids. It incorporates into phospholipids and into triacylglycerol in vivo with the same efficiency as EPA and docosahexaenoic acid and exhibits strong inhibition of arachidonic acid synthesis from linoleic acid. HPA is a poor substrate for prostaglandin H synthase (PGHS) (cyclooxygenase) and for 5-lipoxygenase but retains the ability to rapidly inactivate PGHS. | |||
T38306 | |||
Prostaglandin D2 is synthesized by hematopoietic-type PGD-synthase (H-PGDS) in mast cells and is released in large quantities during allergic and asthmatic anaphylaxis. PGD2 is also produced in the brain by lipocalin-PGD-synthase also known as β-trace. In the brain, PGD2 produces normal physiological sleep and lowering of body temperature. Further pharmacological actions include inhibition of platelet aggregation and relaxation of vascular smooth muscle. tetranor-PGDM is a major metabolite of PGD2 that is detectable in human and mouse urine. The levels of tetranor-PGDM and 2,3-dinor-11β-PGF2α , a related PGD2 metabolite, in human urine were found to be 1.5 ± 0.3 and 0.6 ± ng/mg creatinine, respectively. tetranor-PGDM was detected in murine urine at a level of 8.1 ± 1.3 ng/mg creatinine. | |||
T70097 | |||
Acefylline piperazine is a stimulant drug of the xanthine chemical class. It acts as an adenosine receptor antagonist. Acephylline piperazine is a theophylline derivative with a direct bronchodilator action. It has the advantages over theophylline in being far less toxic and producing minimal gastric irritation. It is indicated for the treatment of asthma, emphysema, acute and chronic bronchitis associated with bronchospasm.Acefylline relaxes smooth muscles, relieves bronchospasm & has a stimulant effect on respiration. It stimulates the myocardium & central nervous system, decreases peripheral resistance & venous pressure & causes diuresis. The mechanism of action is still not clear, inhibition of phosphodiesterase with a resulting increase in intracellular cyclic AMP does occur, but not apparently at concentrations normally used for clinical effect. Other proposed mechanisms of action include adenosine receptor antagonism, prostaglandin antagonism & effects on intracellular...... | |||
T36176 | |||
AMK is an active metabolite of the neurohormone melatonin .1,2,3,4It is formed from melatoninviathe metabolic intermediate AFMK that is then deformylated by catalase or formamidase.5,6AMK scavenges singlet oxygenin vitrowhen used at a concentration of 200 μM.1It inhibits the epinephrine- and arachidonic acid-induced production of prostaglandin E2and PGD2in ovine seminal vesicle microsomes in a concentration- and time-dependent manner, as well as LPS-induced increases in COX-2 levels in RAW 264.7 macrophages when used at a concentration of 500 μM.2,3AMK (20 mg/kg) decreases MPTP-induced increases in lipid peroxidation in the cytosol and mitochondria from substantia nigra and striatum in a mouse model of MPTP-induced Parkinson’s disease.4 1.Schaefer, M., and Hardeland, R.The melatonin metabolite N1-acetyl-5-methoxykynuramine is a potent singlet oxygen scavengerJ. Pineal Res.46(1)49-52(2009) 2.Kelly, R.W., Amato, F., and Seamark, R.F.N-acetyl-5-methoxy kynurenamine, a brain metabolite of melatonin, is a potent inhibitor of prostaglandin biosynthesisBiochem. Biophys. Res. Commun.121(1)372-379(1984) 3.Mayo, J.C., Sainz, R.M., Tan, D.-X., et al.Anti-inflammatory actions of melatonin and its metabolites, N1-acetyl-N2-formyl-5-methoxykynuramine (AFMK) and N1-acetyl-5-methoxykynuramine (AMK), in macrophagesJ. Neuroimmunol.165(1-2)139-149(2005) 4.Tapias, V., Escames, G., López, L.C., et al.Melatonin and its brain metabolite N1-acetyl-5-methoxykynuramine prevent mitochondrial nitric oxide synthase induction in parkinsonian miceJ. Neurosci. Res.87(13)3002-3010(2009) 5.Tan, D.-X., Manchester, L.C., Reiter, R.J., et al.Melatonin directly scavenges hydrogen peroxide: A potentially new metabolic pathway of melatonin biotransformationFree Radic. Biol. Med.29(11)1177-1185(2000) 6.Hirata, F., Hayaishi, O., Tokuyama, T., et al.In vitro and in vivo formation of two new metabolites of melatoninJ. Biol. Chem.249(4)1311-1313(1974) | |||
T37213 | |||
Latanoprost is an F-series prostaglandin analog which has been approved for use as an ocular hypotensive drug. 5-trans Latanoprost is an isomer of latanoprost wherein the double bond between carbons 5 and 6 has been changed from cis (Z) to trans (E). The trans isomer of latanoprost occurs as an impurity of between 2-5% in most commercial preparations of the bulk drug product. The present compound was prepared primarily as an analytical standard for detection and quantitation of this impurity. From what can be inferred from the study of other trans isomers of F-type prostaglandins, 5-trans latanoprost's biological activity is likely to be similar to that of the cis isomer. However, there are no specific published reports on the biological activity, and on the intraocular hypotensive activity in particular, of 5-trans latanoprost. | |||
T71212 | |||
Lornoxicam-d4 is intended for use as an internal standard for the quantification of lornoxicam by GC- or LC-MS. Lornoxicam is a COX inhibitor and non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory and analgesic properties. It inhibits production of thromboxane B2 from arachidonic acid in HEL human erythroleukemic cells, which endogenously express COX-1, as well as inhibits LPS-induced formation of prostaglandin F1α from arachidonic acid in Mono-Mac-6 cells, which endogenously express COX-2. Lornoxicam reduces LPS-induced production of nitric oxide and IL-6 in cell-based assays with IC50 values of 65 and 54 µM, respectively. It reduces carrageenan-induced paw edema in rats when administered intravenously at doses ranging from 0.1 to 9 mg/kg. Formulations containing lornoxicam have been used in the management of postoperative pain. | |||
T82805 | |||
(R)-Butaprost (free acid) 是PGE2的一个结构类似物,特异性地对EP2受体亚型有选择性。该化合物用于药理学研究,以确定不同人类及动物组织和细胞中EP受体的分布。去除甲酯基团并恢复C-1自然羧酸后,增强了(R)-butaprost与前列腺素受体的结合亲和力,通常情况下,游离酸形式的亲和力是相应酯形式的10到100倍。尽管(R)-butaprost作为C-16的较低活性差向异构体,其药理作用未经充分研究,但在1986年Gardiner的论文中提到的TR 4979即布他前列素,结构中的差向异构体错误表达为16(R),实际为16(S),该错误直至1990年代后期才被美国和日本的研究纠正。 | |||
T37628 | |||
Ibuprofen impurity 1 is an Ibuprofen impurity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively[1]. [1]. Noreen Y, et al. Development of a radiochemical cyclooxygenase-1 and -2 in vitro assay for identification of natural products as inhibitors of prostaglandin biosynthesis. J Nat Prod. 1998 Jan;61(1):2-7. |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-03120 | Prostaglandin D2 Synthase Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
Prostaglandin D2 Synthase Protein, Human, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 20.1 kDa and the accession number is P41222.
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TMPY-05069 | Prostaglandin D2 Synthase Protein, Rat, Recombinant (His) | Rat | HEK293 Cells | ||
Prostaglandin D2 Synthase Protein, Rat, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 20.3 kDa and the accession number is A6JT70.
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TMPY-04624 | Prostaglandin D2 Synthase Protein, Mouse, Recombinant (His) | Mouse | HEK293 Cells | ||
Prostaglandin D2 Synthase Protein, Mouse, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 19.9 kDa and the accession number is O09114-1.
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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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TMPY-03876 | PTGFRN Protein, Cynomolgus, Recombinant (His) | Cynomolgus | HEK293 Cells | ||
EWI-F, also known as PTGFRN, is inversely related to the loss of CD9. Its expression correlates with the metastatic status of hLT. EWI-F inhibits the binding of prostaglandin F2-alpha (PGF2-alpha) to its specific FP receptor, by decreasing the receptor number rather than the affinity constant. EWI-F expression positively correlates with the metastatic status of hLT, and that the upregulation of EWI-F expression could be one of the mechanisms underlying the loss of CD9 in solid tumours.
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TMPJ-00690 | PGDS Protein, Human, Recombinant | Human | E. coli | ||
Hematopoietic Prostaglandin D Synthase (HPGDS) belongs to the GST superfamily and Sigma family. HPGDS contains one GST C-terminal domain and one GST N-terminal domain. HPGDS is highly expressed in adipose tissue, macrophages, and placenta, and it exists in the form of homodimer in living body. HPGDS is a cytosolic enzyme that isomerizes PGH(2). HPGDS is a bifunctional enzyme that catalyzes both the conversion of PGH2 to PGD2 and also shows low glutathione-peroxidase activity towards cumenehydroperoxide.
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TMPY-04077 | HPGDS/PGD2 Protein, Human, Recombinant (His) | Human | E. coli | ||
HPGDS/PGD2 Protein, Human, Recombinant (His) is expressed in E. coli expression system with His tag. The predicted molecular weight is 24.2 kDa and the accession number is O60760.
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TMPH-01039 | CBR1 Protein, Human, Recombinant (E. coli, His) | Human | E. coli | ||
CBR1 Protein, Human, Recombinant (E. coli, His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecular weight is 34.2?kDa and the accession number is P16152.
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TMPJ-00348 | CD316 Protein, Human, Recombinant (hFc) | Human | HEK293 Cells | ||
Immunoglobulin Superfamily Member 8 (IGSF8) is a single-pass membrane protein. IGSF8 contains four Ig-like C2 type domains. The Ig-like C2-type domains 3 and 4 are required for interactions with CD81. IGSF8 may regulate proliferation and differentiation of keratinocytes. IGSF8 may participate in the regulation of neurite outgrowth and maintenance of the neural network in the adult brain. It also may play a role on integrin-dependent morphology and motility functions.
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TMPH-01040 | CBR1 Protein, Human, Recombinant (His) | Human | P. pastoris (Yeast) | ||
CBR1 Protein, Human, Recombinant (His) is expressed in yeast with N-6xHis tag. The predicted molecular weight is 32.2 kDa and the accession number is P16152.
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TMPH-02683 | GSTP1 Protein, Mouse, Recombinant (His & SUMO) | Mouse | E. coli | ||
Conjugation of reduced glutathione to a wide number of exogenous and endogenous hydrophobic electrophiles. Involved in the formation of glutathione conjugates of both prostaglandin A2 (PGA2) and prostaglandin J2 (PGJ2). Participates in the formation of novel hepoxilin regioisomers. Regulates negatively CDK5 activity via p25/p35 translocation to prevent neurodegeneration.
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TMPH-01398 | GSTP1 Protein, Human, Recombinant (E. coli, His) | Human | E. coli | ||
Conjugation of reduced glutathione to a wide number of exogenous and endogenous hydrophobic electrophiles. Involved in the formation of glutathione conjugates of both prostaglandin A2 (PGA2) and prostaglandin J2 (PGJ2). Participates in the formation of novel hepoxilin regioisomers. Regulates negatively CDK5 activity via p25/p35 translocation to prevent neurodegeneration. GSTP1 Protein, Human, Recombinant (E. coli, His) is expressed in E. coli expression system with N-10xHis tag. The predicted molecular weight is 28.2 kDa and the accession number is P09211.
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TMPH-01399 | GSTP1 Protein, Human, Recombinant (His) | Human | P. pastoris (Yeast) | ||
Conjugation of reduced glutathione to a wide number of exogenous and endogenous hydrophobic electrophiles. Involved in the formation of glutathione conjugates of both prostaglandin A2 (PGA2) and prostaglandin J2 (PGJ2). Participates in the formation of novel hepoxilin regioisomers. Regulates negatively CDK5 activity via p25/p35 translocation to prevent neurodegeneration. GSTP1 Protein, Human, Recombinant (His) is expressed in yeast with N-6xHis tag. The predicted molecular weight is 25.2 kDa and the accession number is P09211.
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TMPH-02438 | IL-1 alpha/IL1A Protein, Rhesus macaque, Recombinant (His & SUMO) | Rhesus | E. coli | ||
Produced by activated macrophages, IL-1 stimulates thymocyte proliferation by inducing IL-2 release, B-cell maturation and proliferation, and fibroblast growth factor activity. IL-1 proteins are involved in the inflammatory response, being identified as endogenous pyrogens, and are reported to stimulate the release of prostaglandin and collagenase from synovial cells. IL-1 alpha/IL1A Protein, Rhesus macaque, Recombinant (His & SUMO) is expressed in E. coli expression system with N-6xHis-SUMO tag. The predicted molecular weight is 34.1 kDa and the accession number is P48089.
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TMPJ-01010 | PLA2G16 Protein, Human, Recombinant (His) | Human | E. coli | ||
Group XVI Phospholipase A1/A2 (PLA2G16) belongs to the H-rev 107 family. PLA2G16 is expressed in a number of human tumors including ovarian carcinomas, lung carcinomas. PLA2G16 is involved in the regulation of differentiation and survival. PLA2G16 regulates adipocyte lipolysis and release of fatty acids through a G-protein coupled pathway involving prostaglandin and EP3. It has also been reported to play a crucial role in the development of obesity in mouse models.
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TMPJ-01392 | IL-1 beta/IL-1F2 Protein, Cavia porcellus, Recombinant (His) | Cavia porcellus | E. coli | ||
Interleukin-1 beta (IL1B) belongs to the IL-1 family. Interleukin 1 (IL-1) is a family of polypeptide cytokines consisting of two agonists, IL-1 alpha (IL-1F1) and IL-1 beta (IL-1F2) encoded by two distinct genes and perform identical biological functions. IL-1 stimulates thymocyte proliferation by inducing IL-2 release, B-cell maturation and proliferation, and fibroblast growth factor activity. IL-1 proteins are involved in the inflammatory response. It is identified as endogenous pyrogens, and is reported to stimulate the release of prostaglandin and collagenase from synovial cells.
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TMPJ-00962 | AKR1C3 Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
AKR1C3, is an enzyme which belongs to the aldo/keto reductase family. It is expressed in many tissues including adrenal gland, brain, kidney, liver, lung, mammary gland, placenta, small intestine, colon, spleen, prostate and testis. AKR1C3 catalyzes the conversion of aldehydes and ketones to alcohols. It catalyzes the reduction of prostaglandin (PG) D2, PGH2 and phenanthrenequinone (PQ) and the oxidation of 9-alpha,11-beta-PGF2 to PGD2,which functions as a bi-directional 3-alpha-, 17-beta- and 20-alpha HSD. It can interconvert active androgens, estrogens and progestins with their cognate inactive metabolites.
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TMPY-02945 | Prokineticin 1/EG-VEGF Protein, Human, Recombinant (His) | Human | Baculovirus Insect Cells | ||
EG-VEGF, also known as prokineticin-1, is a member of the AVIT (prokineticin) family. Prokineticins are secreted proteins that can promote angiogenesis and induce strong gastrointestinal smooth muscle contraction. EG-VEGF can be detected in the steroidogenic glands, ovary, testis, adrenal and placenta. EG-VEGF has little or no effect on a variety of other endothelial and non-endothelial cell types. It induces proliferation, migration and fenestration (the formation of membrane discontinuities) in capillary endothelial cells derived from endocrine glands. It directly influences neuroblastoma progression by promoting the proliferation and migration of neuroblastoma cells. EG-VEGF may play a role in placentation. It may also function in normal and pathological testis angiogenesis. It positively regulates PTGS2 expression and prostaglandin synthesis.
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TMPH-02690 | PLA2G10 Protein, Mouse, Recombinant (His & Myc) | Mouse | E. coli | ||
Secretory calcium-dependent phospholipase A2 that primarily targets extracellular phospholipids. Hydrolyzes the ester bond of the fatty acyl group attached at sn-2 position of phospholipids with preference for phosphatidylcholines and phosphatidylglycerols over phosphatidylethanolamines. Preferentially releases sn-2 omega-6 and omega-3 polyunsaturated fatty acyl (PUFA) chains over saturated fatty acyls. Contributes to phospholipid remodeling of very low-density lipoprotein (VLDL), low-density lipoprotein (LDL) and high-density lipoprotein (HDL) particles. Hydrolyzes LDL phospholipids releasing unsaturated fatty acids that regulate macrophage differentiation toward foam cells. Efficiently hydrolyzes and inactivates PAF, a potent lipid mediator present in oxidized LDL. May act in an autocrine and paracrine manner. Secreted by lung epithelium, targets membrane phospholipids of infiltrating eosinophils, releasing arachidonate and boosting eicosanoid and cysteinyl leukotriene synthesis involved in airway inflammatory response. Secreted by gut epithelium, hydrolyzes dietary and biliary phosphatidylcholines in the gastrointestinal lumen, thereby regulating adipogenesis and body weight. Plays a stem cell regulator role in colon epithelium. Within intracellular compartment, mediates Paneth-like cell differentiation and its stem cell supporting functions by inhibiting Wnt signaling pathway in intestinal stem cell (ISC). Secreted in the intestinal lumen upon inflammation, acts in an autocrine way and promotes prostaglandin E2 synthesis that stimulates the Wnt signaling pathway in ISCs and tissue regeneration. May participate in hair follicle morphogenesis by regulating phosphatidylethanolamines metabolism at the outermost epithelial layer and facilitating melanin synthesis. By generating lysophosphatidylcholines (LPCs) at sperm acrosome controls sperm cell capacitation, acrosome reaction and overall fertility. May promote neurite outgrowth in neuron fibers involved in nociception. Contributes to lipid remodeling of cellular membranes and generation of lipid mediators involved in pathogen clearance. Cleaves sn-2 fatty acyl chains of phosphatidylglycerols and phosphatidylethanolamines, which are major components of membrane phospholipids in bacteria. Displays bactericidal activity against Gram-positive bacteria by directly hydrolyzing phospholipids of the bacterial membrane. In pulmonary epithelium, may contribute to host defense response against adenoviral infection. Prevents adenovirus entry into host cells by hydrolyzing host cell plasma membrane, releasing C16:0 LPCs that inhibit virus-mediated membrane fusion and viral infection. Likely prevents adenoviral entry into the endosomes of host cells. May play a role in maturation and activation of innate immune cells including macrophages, group 2 innate lymphoid cells and mast cells.
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