目录号 | 产品详情 | 靶点 | |
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T61976 | |||
DS-6930 是一种有效的和选择性的 PPARγ激动剂(EC50= 41 nM)。DS-6930 可有效降低血浆葡萄糖 (PG)水平,此外,与 Rosiglitazone 相比,具有更少的 PPARγ 相关不良反应。DS-6930 在糖尿病中具有研究价值。 | |||
T69671 | |||
SR-1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR). It is an inverse agonist of RORγ and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPAR) but does not activate it. SR-1903 inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1). It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1. SR-1903 reduces the severity of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity. | |||
T16739 | Leukotriene Receptor PPAR | ||
RG-12525(NID 525) 是一种可口服且具有选择性和竞争性的白三烯 D (LTD)拮抗剂,对 LTC4,LTD4 和 LTE4 诱导的豚鼠薄壁带收缩有抑制作用,IC50 值分别为 2.6 nM,2.5 nM 和 7 nM。RG-12525 对 CYP3A4 有抑制作用, Ki 值为 0.5 µM。RG-12525 是一种新型高效的 PPAR-γ 激动剂(IC50 值约为 60 nM),具有物种特异性,可用于研究哮喘。 | |||
T37829 | |||
The peroxisome proliferator-activated receptors (PPARs) are lipid-activated transcription factors often used as drug targets for the treatment of metabolic disorders. CAY10573 is a PPAR agonist that displays potent binding at PPARα, γ, and δ with IC50 values of 113, 50, and 223 nM, respectively. It potently transactivates PPARα, γ, and δ with EC50 values of 8, 70, and 500 nM, respectively. CAY10573 demonstrates stronger binding and functional activity for PPARγ than the antidiabetic compound rosiglitazone (IC50 = 92 nM; EC50 = 220 nM). | |||
T35813 | |||
Peroxisome proliferator-activated receptors (PPARs) α, δ, γ are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism. Pharmacologies of PPARδ receptor agonists, though relatively obscure, have recently been reported to elevate high-density lipoprotein (HDL) cholesterol and lower plasma triglyceride (TG) levels in obese insulin resistant rhesus monkeys. CAY10592 is a full PPARδ agonist (EC50 = 30 nM) in a fatty acid oxidation assay of rat L6 muscle cells with desirable oral pharmacokinetic properties. In a transactivation assay using human PPAR receptors, CAY10592 acts as a selective partial PPARδ agonist (EC50 = 53 nM) with no effect on PPARα or PPARγ activity up to 30 μM. Chronic treatment of high fat fed ApoB100/CETP-transgenic mice with CAY10592 at a dose of 20 mg/kg increases HDL levels, decreases LDL and TG levels, and improves insulin sensitivity. |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-02575 | PPAR gamma/PPARG Protein, Human, Recombinant (His & GST) | Human | Baculovirus-Insect Cells | ||
Peroxisome proliferator-activated receptor gamma (PPARG), a nuclear hormone receptor, plays a critical role in the lipid and glucose homeostasis, adipocyte differentiation, as well as intracellular insulin-signaling events. The peroxisome proliferator-activated receptor gamma (PPARgamma) regulates osteoblast and osteoclast differentiation, and is the molecular target of thiazolidinediones (TZDs), insulin sensitizers that enhance glucose utilization and adipocyte differentiation. Peroxisome proliferator-activated receptor gamma (PPARG) is a transcription factor involved in atherosclerosis and related diseases. Peroxisome proliferator-activated receptor gamma (PPARG) plays an important role in the pathogenesis and maintenance of essential hypertension (EH).The functional single nucleotide polymorphisms in peroxisome proliferator-activated receptor gamma (PPARG) gene were predicted to be correlated with the susceptibility of colorectal cancer (CRC).
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TMPY-06837 | PPAR alpha/PPARA Protein, Mouse, Recombinant (His) | Mouse | E. coli | ||
Peroxisome proliferators include hypolipidemic drugs, herbicides, leukotriene antagonists, and plasticizers; this term arises because they induce an increase in the size and number of peroxisomes. Peroxisomes are subcellular organelles found in plants and animals that contain enzymes for respiration and for cholesterol and lipid metabolism. The action of peroxisome proliferators is thought to be mediated via specific receptors, called PPARs, which belong to the steroid hormone receptor superfamily. PPARs affect the expression of target genes involved in cell proliferation, cell differentiation and in immune and inflammation responses. Three closely related subtypes (alpha, beta/delta, and gamma) have been identified. This gene encodes the subtype PPAR-alpha, which is a nuclear transcription factor. Multiple alternatively spliced transcript variants have been described for this gene, although the full-length nature of only two has been determined.Cancer ImmunotherapyImmune CheckpointImmunotherapyTargeted Therapy
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TMPY-06830 | PPAR alpha/PPARA Protein, Human, Recombinant (His) | Human | E. coli | ||
Peroxisome proliferators include hypolipidemic drugs, herbicides, leukotriene antagonists, and plasticizers; this term arises because they induce an increase in the size and number of peroxisomes. Peroxisomes are subcellular organelles found in plants and animals that contain enzymes for respiration and for cholesterol and lipid metabolism. The action of peroxisome proliferators is thought to be mediated via specific receptors, called PPARs, which belong to the steroid hormone receptor superfamily. PPARs affect the expression of target genes involved in cell proliferation, cell differentiation and in immune and inflammation responses. Three closely related subtypes (alpha, beta/delta, and gamma) have been identified. This gene encodes the subtype PPAR-alpha, which is a nuclear transcription factor. Multiple alternatively spliced transcript variants have been described for this gene, although the full-length nature of only two has been determined.Cancer ImmunotherapyImmune CheckpointImmunotherapyTargeted Therapy
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TMPH-02827 | PPAR gamma Protein, Mouse, Recombinant (His) | Mouse | E. coli | ||
Nuclear receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, the nuclear receptor binds to DNA specific PPAR response elements (PPRE) and modulates the transcription of its target genes, such as acyl-CoA oxidase. It therefore controls the peroxisomal beta-oxidation pathway of fatty acids. Key regulator of adipocyte differentiation and glucose homeostasis. ARF6 acts as a key regulator of the tissue-specific adipocyte P2 (aP2) enhancer. Acts as a critical regulator of gut homeostasis by suppressing NF-kappa-B-mediated proinflammatory responses. Plays a role in the regulation of cardiovascular circadian rhythms by regulating the transcription of ARNTL/BMAL1 in the blood vessels.
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TMPH-03711 | PPAR gamma Protein, Xenopus laevis, Recombinant (His) | Xenopus laevis | E. coli | ||
Receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, the receptor binds to a promoter element in the gene for acyl-CoA oxidase and activates its transcription. It therefore controls the peroxisomal beta-oxidation pathway of fatty acids. Key regulator of adipocyte differentiation and glucose homeostasis. May play a role in the regulation of circadian rhythm.
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TMPH-02855 | PML Protein, Mouse, Recombinant (His & Myc) | Mouse | E. coli | ||
Functions via its association with PML-nuclear bodies (PML-NBs) in a wide range of important cellular processes, including tumor suppression, transcriptional regulation, apoptosis, senescence, DNA damage response, and viral defense mechanisms. Acts as the scaffold of PML-NBs allowing other proteins to shuttle in and out, a process which is regulated by SUMO-mediated modifications and interactions. Positively regulates p53/TP53 by acting at different levels (by promoting its acetylation and phosphorylation and by inhibiting its MDM2-dependent degradation). Regulates phosphorylation of ITPR3 and plays a role in the regulation of calcium homeostasis at the endoplasmic reticulum. Regulates RB1 phosphorylation and activity. Acts as both a negative regulator of PPARGC1A acetylation and a potent activator of PPAR signaling and fatty acid oxidation. Regulates translation of HIF1A by sequestering MTOR, and thereby plays a role in neoangiogenesis and tumor vascularization. Regulates PER2 nuclear localization and circadian function. Cytoplasmic PML is involved in the regulation of the TGF-beta signaling pathway. Required for normal development of the brain cortex during embryogenesis. Plays a role in granulopoiesis or monopoiesis of myeloid progenitor cells. May play a role regulating stem and progenitor cell fate in tissues as diverse as blood, brain and breast. Shows antiviral activity towards lymphocytic choriomeningitis virus (LCMV) and the vesicular stomatitis virus (VSV).
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