目录号 | 产品详情 | 靶点 | |
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T38764L | |||
Amylin (8-37), human acetate(135702-23-7 free base) 源自人 Amylin,对大鼠离体肠系膜阻力动脉具有直接血管舒张作用。 Amylin (8-37), human acetate,是一种小型胰腺 β 细胞激素,在没有胰岛素的情况下会形成聚集体,是 II 型糖尿病的一个关键病理特征。 | |||
T73734 | Others | ||
Acetoacetic acid是一种存在于脑脊液中的内源代谢物,主要应用于脑膜炎、妊娠、3-羟基-3-甲基戊二酰辅酶A裂解酶缺乏症、子痫前期/子痫、2型糖尿病、1型葡萄糖转运蛋白缺乏综合征及琥珀酰辅酶A:3-氧酸辅酶A转移酶缺乏症的研究中。 | |||
TN5119 | Tyrosinase Antifection | ||
Taxoquinone has strong antibacterial effect, it could be used as a promising antibacterial agent in food industry to inhibit the growth of certain important foodborne pathogens. It (100 ug/disc) displays potential anticandidal effect against Candia albica | |||
T78881 | Glucosidase | ||
α-Glucosidase-IN-36(compound 5g)作为一种α-glucosidase抑制剂,表现出有效的抑制活性,其IC50值为6.69 ± 0.18 μM,Ki值为1.65 μM,Kis值为4.54 μM。该化合物通过与α-glucosidase的活性位点结合及可能改变其二级结构来执行其抑制功能。α-Glucosidase-IN-36在2型糖尿病(T2DM)的研究中有应用潜力。 | |||
T70391 | Others | ||
ARRY-403, also known as AMG-151, is an orally available allosteric glucokinase (GK) activator developed for the treatment of type 2 diabetes mellitus (T2DM). ARRY-403 has many favorable physicochemical characteristics and ADME properties (low potential to cause drug–drug interactions (DDIs). ARRY-403 potently activates human glucokinase (GK) in vitro (EC50 = 79 nM at 5 mM glucose), with an S0.5 = 0.93 mM glucose (ARRY-403 at 5 mM) and Vmax = 134% compared to the no activator control. It possesses good in vitro drug-like properties (aqueous solubility, cell permeability, low low potential for drug-drug interactions, low predicted hepatic clearance), and selectivity against broad panels of receptors and enzymes. | |||
T78702 | Phosphatase | ||
PTP1B/AKR1B1-IN-1是一种针对PTP1B和AKR1B1的双重抑制剂,其IC50值分别为0.06 μM和4.3 μM。该化合物也能抑制TC-PTP,IC50为9 μM。在小鼠成肌细胞中,PTP1B/AKR1B1-IN-1作为胰岛素模拟剂使用,并能减少AKR1B1依赖的山梨醇积累,有助于抑制2型糖尿病的发展并控制血糖水平。 | |||
T79358 | Endogenous Metabolite | ||
PF-07247685是一种BCKDC激酶(BDK)抑制剂,具有较强的活性(EC50=2.2 nM)。该化合物能有效稳定BDK与BCKDH E2核心亚基之间的相互作用,并阻断E1亚基的磷酸化过程。BCKDH的活性受到BDK介导的磷酸化调控,从而控制支链氨基酸(BCAA)降解的关键步骤。BCAA的代谢失调与心力衰竭(HF)、2型糖尿病(T2DM)、非酒精性脂肪肝病(NAFLD)及肥胖等多种疾病相关联,尤其在心脏代谢疾病中表现明显。PF-07247685在小鼠模型中对心脏代谢终点产生改善效果,并提升了葡萄糖耐量。 | |||
T79357 | Endogenous Metabolite | ||
PF-07238025是一种BCKDC激酶(BDK)抑制剂,具有EC50值为19 nM。它通过稳定BDK和BCKDH复合体中的E2亚基相互作用,阻碍E1亚基的磷酸化过程,从而抑制了BCKDH的活性。由于BDK的磷酸化作用是控制支链氨基酸(BCAA)降解过程中的限速步骤,PF-07238025的作用与包括心力衰竭(HF)、2型糖尿病(T2DM)、非酒精性脂肪肝病(NAFLD)及肥胖在内的多种代谢性疾病的发病机制相关。研究显示PF-07238025能在小鼠体内改善心脏代谢指标并提升葡萄糖耐量。 | |||
T83906 | |||
Tirzepatide 是一种glucagon-like peptide 1 receptor (GLP-1R) 和 G protein-coupled receptor 119 (GPR119)的激动剂。它在表达人类GLP-1R或GPR119的HEK293细胞中诱导cAMP的产生(EC50s分别为6.54和1.01 nM)。Tirzepatide(100 nM)在表达人类GLP-1R或GPR119的HEK293细胞中诱导受体内化。在体内,Tirzepatide(每天10 nmol/kg)降低高脂饮食诱导的肥胖小鼠模型的体重、食物摄入量、血浆leptin、三酸甘油酯和free fatty acids (FFAs)水平、肝脏三酸甘油酯和血糖水平。它通过每三天给药50 nmol/kg的剂量,阻止A. alternata诱导的A. alternata挑战小鼠的支气管肺泡灌洗液(BALF)中嗜酸性粒细胞和淋巴细胞数量的增加。Tirzepatide(每三天50 nmol/kg)抑制由毒蕈碱受体激动剂methacholine (acetyl-β-methylcholine)导致的在糖尿病诱导的哮喘小鼠模型中的支气管收缩。含Tirzepatide的制剂已用于治疗2型糖尿病。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-00395 | Insulin Protein, Human, Recombinant | Human | P. pastoris (Yeast) | ||
INS (Insulin) is a Protein Coding gene. This gene encodes insulin, a peptide hormone that plays a vital role in the regulation of carbohydrate and lipid metabolism. After removal of the precursor signal peptide, proinsulin is post-translationally cleaved into three peptides: the B chain and A chain peptides, which are covalently linked via two disulfide bonds to form insulin, and C-peptide. The binding of insulin to the insulin receptor (INSR) stimulates glucose uptake. Diseases associated with INS include Hyperproinsulinemia and Maturity-Onset Diabetes Of The Young, Type 10. A multitude of mutant alleles with phenotypic effects has been identified, including insulin-dependent diabetes mellitus, permanent neonatal diabetes mellitus, maturity-onset diabetes of the young type 10, and hyperproinsulinemia.Cancer ImmunotherapyImmune CheckpointImmunotherapyTargeted Therapy
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TMPJ-00071 | EPO/Erythropoietin Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
Erythropoietin (EPO) is a glycoprotein hormone that is principally known for its role in erythropoiesis, where it is responsible for stimulating proliferation and differentiation of erythroid progenitor cells. Erythropoietin is a member of the EPO/TPO family. It is a secreted, glycosylated cytokine composed of four alpha helical bundles. The differentiation of CFU-E (Colony Forming Unit-Erythroid) cells into erythrocytes can only be accomplished in the presence of EPO. Physiological levels of EPO in adult mammals are maintained primarily by the kidneys, whereas levels in fetal or neonatal mammals are maintained by the liver. EPO also can exert various non-hematopoietic activities, including vascularization and proliferation of smooth muscle, neural protection during hypoxia, and stimulation of certain B cells. Genetic variation in erythropoietin is associated with susceptbility to microvascular complications of diabetes type 2. These are pathological conditions that develop in numerous tissues and organs as a consequence of diabetes mellitus. They include diabetic retinopathy, diabetic nephropathy leading to end-stage renal disease, and diabetic neuropathy.
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TMPY-03962 | AFM Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
Afamin is an 87 kDa glycoprotein with five predicted N-glycosylation sites. Afamin's glycan abundance contributes to conformational and chemical inhomogeneity presenting great challenges for molecular structure determination. Afamin, a human plasma glycoprotein and putative transporter of hydrophobic molecules, has been shown to act as extracellular chaperone for poorly soluble, acylated Wnt proteins, forming a stable, soluble complex with functioning Wnt proteins. The 2.1-Å crystal structure of glycosylated human afamin reveals an almost exclusively hydrophobic binding cleft capable of harboring large hydrophobic moieties. Afamin plays a role in anti-apoptotic cellular processes related to oxidative stress and is associated with insulin resistance and other features of metabolic syndrome. Afamin may serve as a new early biomarker for pathological glucose metabolism during pregnancy. And first trimester screening for pre-eclampsia could be provided by a combination of afamin and placental bed vascularization. Moreover, the combination of first trimester serum afamin levels with BMI could provide a possible screening for gestational diabetes mellitus.
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TMPK-01128 | LRG1 Protein, Mouse, Recombinant (His) | Mouse | HEK293 Cells | ||
Diabetic nephropathy (DN) is an important public health concern of increasing proportions and the leading cause of end-stage renal disease (ESRD) in diabetic patients. It is one of the most common long-term microvascular complications of diabetes mellitus that is characterized by proteinuria and glomerular structural changes. LRG1 is a novel pro-angiogenic factors involved in the abnormal angiogenesis and renal fibrosis in DN. LRG1 Protein, Mouse, Recombinant (His) is expressed in HEK293 mammalian cells with C-His tag. The predicted molecular weight is 34.9 kDa and the accession number is Q91XL1.
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TMPK-00526 | LRG1 Protein, Cynomolgus, Recombinant (His) | Cynomolgus | HEK293 Cells | ||
Diabetic nephropathy (DN) is an important public health concern of increasing proportions and the leading cause of end-stage renal disease (ESRD) in diabetic patients. It is one of the most common long-term microvascular complications of diabetes mellitus that is characterized by proteinuria and glomerular structural changes. LRG1 is a novel pro-angiogenic factors involved in the abnormal angiogenesis and renal fibrosis in DN. LRG1 Protein, Cynomolgus, Recombinant (His) is expressed in HEK293 mammalian cells with C-His tag. The predicted molecular weight is 35.69 kDa and the accession number is A0A2K5VVA4.
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TMPJ-01199 | BTN2A1 Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
Butyrophilin 2A1 (BTN2A1) is an approximately widely expressed and variably glycosylated type I transmembrane glycoprotein. Mature human Butyrophilin 2A1 consisits of a 220 amino acid (aa) extracellular domain with two immunoglobulin-like domains, a 21 aa transmembrane segment, and a 258 aa cytoplasmic domain. Alternative splicing generates additional isoforms of human Butyrophilin 2A1 that lack the first Ig like domain or transmembrane segment as well as isoforms with substitutions and deletions in the cytoplasmic region. BTN2A1 is widely expressed including on colonic epithelial cells, on immune cells, and in milk fat globules. It binds to the C-type lectin DCSIGN on monocytederived dendritic cells, and this interaction can be blocked by soluble gp130 from HIV. The polymorphism of BTN2A1 has been associated with metabolic syndrome, type II diabetes mellitus, chronic kidney disease, and hypertension.
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TMPJ-00014 | Resistin Protein, Human, Recombinant (His) | Human | E. coli | ||
Resistin known as adipose tissue-specific secretory factor (ADSF) or C/EBP-epsilon-regulated myeloid-specific secreted cysteine-rich protein (XCP1) that seems to suppress insulin ability to stimulate glucose uptake into adipose cells. The length of the resistin pre-peptide in human is 108 amino acid residues and in the mouse and rat it is 114 aa; the molecular weight is ~12.5 kDa. Resistin is a cytokine whose physiologic role has been the subject of much controversy regarding its involvement with obesity and type II diabetes mellitus (T2DM). Resistin has been shown to cause "high levels of 'bad' cholesterol (low-density lipoprotein or LDL), increasing the risk of heart disease, resistin increases the production of LDL in human liver cells and also degrades LDL receptors in the liver. Potentially links obesity to diabetes.
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TMPY-04394 | Glucokinase Protein, Human, Recombinant | Human | E. coli | ||
Glucokinase belongs to the bacterial glucokinase family. Hexokinases phosphorylate glucose to produce glucose-6-phosphate, the first step in most glucose metabolism pathways. Alternative splicing of this gene results in three tissue-specific forms of glucokinase, one found in pancreatic islet beta cells and two found in liver. The protein localizes to the outer membrane of mitochondria. In contrast to other forms of hexokinase, this enzyme is not inhibited by its product glucose-6-phosphate but remains active while glucose is abundant. Mutations in this gene have been associated with non-insulin dependent diabetes mellitus (NIDDM), maturity onset diabetes of the young, type 2 (MODY2) and persistent hyperinsulinemic hypoglycemia of infancy (PHHI). It can Catalyzes the initial step in utilization of glucose by the beta-cell and liver at physiological glucose concentration. Glucokinase has a high Km for glucose, and so it is effective only when glucose is abundant. The role of GCK is to provide G6P for the synthesis of glycogen. Pancreatic glucokinase plays an important role in modulating insulin secretion. Hepatic glucokinase helps to facilitate the uptake and conversion of glucose by acting as an insulin-sensitive determinant of hepatic glucose usage. It has a pivotal role as glucose sensor of the pancreatic beta-cells. Glucokinase explains the capacity, hexose specificity, affinities, sigmoidicity, and anomeric preference of pancreatic islet glycolysis, and because stimulation of glucose metabolism is a prerequisite of glucose stimulation of insulin release, glucokinase also explains many characteristics of this beta-cell function. Glucokinase of the beta-cell is induced or activated by glucose in contrast to liver glucokinase, which is regulated by insulin. Tissue-specific regulation corresponds with observations that liver and pancreatic beta-cell glucokinase are structurally distinct. Glucokinase could play a glucose-sensor role in hepatocytes as well, and certain forms of diabetes mellitus might be due to glucokinase deficiencies in pancreatic beta-cells, hepatocytes, or both.
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TMPY-04122 | ATOX1 Protein, Human, Recombinant (His) | Human | E. coli | ||
ATOX1 is a cytoplasmic copper chaperone that interacts with the copper-binding domain of the membrane copper transporters ATP7A and ATP7B. ATOX1 has also been suggested to have a potential anti-oxidant activity. As the trace element copper is essential, but extremely toxic in high concentrations, intracellular copper concentrations are tightly controlled. Once in the cell, copper is distributed by metallochaperones, including the small cytoplasmic protein ATOX1. ATOX1 plays an important role in the transfer of copper to the copper export P-type ATPases ATP7A and ATP7B to facilitate copper excretion. There is a novel function for Atox1 as a transcription factor (TF) regulating Ccnd1 was proposed. Antioxidant 1 (ATOX1) functions as an antioxidant against hydrogen peroxide and superoxide, and therefore may play a significant role in many human diseases, including diabetes mellitus (DM). The transduced Tat-ATOX1 protein protects pancreatic beta-cells by inhibiting STZ-induced cellular toxicity in vitro and in vivo. Thus Tat-ATOX1 protein has potential applications as a therapeutic agent for oxidative stress-induced diseases including DM.
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