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Search Results for " glucose tolerance "

33

抑制剂 & 化合物

8

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T2014	CCG-1423 CCG1423	LRRK2; Rho; Ras	Autophagy; Cell Cycle/Checkpoint; GPCR/G Protein; MAPK
	CCG-1423 是一种选择性 RhoA 通路抑制剂，可抑制 SRF 介导的转录，能抑制细胞的转移前列腺癌PC-3细胞侵袭模型。
T11765	KPLH1130	Dehydrogenase; PDK	Metabolism; PI3K/Akt/mTOR signaling
	KPLH1130，一种选择性丙酮酸脱氢酶激酶(PDK)抑制剂，在高脂饮食(HFD)喂养的小鼠中提高了糖耐量。KPLH1130 抑制巨噬细胞极化并减轻了炎症反应。
T3312	AM-2394 AM2394	Glucokinase	Metabolism
	AM-2394 是新型的 glucokinase 激活剂 (GKA)。它能够激活葡萄糖激酶 (GK)，EC50=60 nM。
T62238	AMPK activator 4	AMPK	Chromatin/Epigenetic; PI3K/Akt/mTOR signaling
	AMPK activator 4 是一种有效且具有选择性的AMPK激活剂，不抑制线粒体复合物 I。AMPK activator 4 选择性地激活肌肉组织中的 AMPK且剂量依赖性地改善正常小鼠的糖耐量，显著降低 db/db 糖尿病小鼠的空腹血糖水平和改善胰岛素抵抗。AMPK activator 4 具有降血糖作用。
T21979	P32/98 (hemifumarate)
	P32/98 hemifumarate 为二肽基肽酶 IV (DPP4) 抑制剂，可在Zucker糖尿病大鼠模型中改善葡萄糖耐量、提高胰岛素敏感性及增强β细胞反应性，具有预防2型糖尿病的潜力。
T30169	ASP-8497 UNII-GC7THT248G,ASP8497,ASP 8497
	ASP8497 is a potent, long-acting DPP-IV inhibitor that improves glucose tolerance by elevating GLP-1 levels in a glucose-dependent insulin-stimulating manner. The compound is used as a therapeutic agent for impaired glucose tolerance and type 2 diabetes.
T38771	P32/98 P32/98
	P32/98 is a potent inhibitor of dipeptidyl peptidase IV . P32/98 improves glucose tolerance, insulin sensitivity and β-cell responsiveness in preclinical studies using the fatty Zucker rat, an animal model for IGT (impaired glucose tolerance).
T28784	SIRT6-IN-1
	SIRT6-IN-1, a novel SIRT6 inhibitor, reduces glycemia and improves oral glucose tolerance in unfed wild-type mice.
T29154	WB403 WB-403,WB 403
	WB403 is a TGR5 activator. WB403 significantly decreases fasting blood glucose, postprandial blood glucose and HbA1c, improves glucose tolerance in type 2 diabetic mice. WB403 increases pancreatic β-cells and restores the normal distribution pattern of α-
T71251	DS-1558
	DS-1558 is a potent and orally available GPR40 agonist.DS-1558 was found to have potent glucose lowering effects during an oral glucose tolerance test in ZDF rats. DS-1558 significantly and dose-dependently improved hyperglycemia and increased insulin secretion during the oral glucose tolerance test in Zucker fatty rats, the model of insulin resistance and glucose intolerance. DS-1558 not only increased the glucose-stimulated insulin secretion by GLP-1 but also potentiated the maximum insulinog...
T11583	HWL-088	Others	Others
	HWL-088 is a potent free fatty acid receptor 1 (FFA1/GPR40) agonist. HWL-088 significantly improves glucose tolerance in normal and diabetic models.
T68132	quercetin-3'-o-phosphate
	Quercetin-3'-O-phosphate belongs to the class of organic compounds known as flavonols,has been used in trials studying the treatment of Insulin Resistance and Impaired Glucose Tolerance.
TP2020	[Pro3]-GIP (Mouse)
	GIP receptor antagonist (IC50 = 2.6μM). Inhibits GIP-stimulated insulin release from pancreatic β cells in vitro. In ob/ob mice, blocks the effects of GIP on insulin release and plasma glucose levels. Also improves intraperitoneal glucose tolerance, insul
T35785	N-Oleoyl Leucine
	N-Oleoyl leucine is an N-acyl amide generated by PM20D1 that uncouples mitochondrial respiration independent of uncoupling protein 1 (UCP1) in vitro. N-Oleoyl leucine (25 mg/kg, i.p.) decreases body weight and food intake, preferentially decreasing fat mass in a diet-induced obesity mouse model. It improves glucose homeostasis in a fasting glucose tolerance test and increases VO2 while slightly decreasing overall locomotor activity.
T60312	FBPase-IN-1
	FBPase-IN-1 is a powerful inhibitor of Fructose-1,6-bisphosphatase (FBPase), a key enzyme involved in Type 2 diabetes (T2D) research. It exhibits an impressive IC50 value of 0.22 μM. Aside from its potency, FBPase-IN-1 also demonstrates the ability to effectively lower blood glucose levels and improve glucose tolerance. Its mechanism of action involves covalently modifying the C128 site, thereby influencing the N125-S124-S123 allosteric pathway of FBPase, ultimately impacting its catalytic activ...
T62542	GPR40 agonist 5
	GPR40 agonist 5 是一种口服具有活力的 GPR40 (G 蛋白偶联受体 40) 激动剂 (EC50: 47 nM)。GPR40 agonist 5 能够减少血糖水平，改善糖耐量。GPR40 agonist 5 对 2 型糖尿病小鼠的高血糖状态表现出充足的控制作用。
T36142	10-PAHSA
	10-PAHSA is a newly identified endogenous lipid that belongs to a collection of branched fatty acid esters of hydroxy fatty acids (FAHFAs). It is a FAHFA in which palmitic acid is esterified to 10-hydroxy stearic acid. Among the FAHFA family members, PAHSAs are the most abundant in the adipose tissue of glucose tolerant AG4OX mice, which overexpress the Glut4 glucose transporter specifically in adipose tissue. As other FAHFAs improve glucose tolerance, stimulate insulin secretion, and have anti-...
T25739	Linogliride McN-3935,McN3935,McN 3935,Linogliridum,Linoglirida
	Linogliride 是一种基于胍的胰岛素分泌抑制剂，也是 pirogliride 的结构类似物，具有降血糖活性。它可以阻断胰腺β细胞膜上对 ATP 敏感的钾通道，从而刺激胰岛素分泌并改善葡萄糖耐受性。
T70390	YM-543 choline
	YM-543, also known as ASP-543, is a selective SGLT2 inhibitor. Sodium-glucose cotransporter 2 (SGLT2) is a specifically expressed transporter in the kidney that plays an important role in renal glucose reabsorption, and its inhibition may present a novel therapeutic strategy for treating diabetes. YM543 potently and selectively inhibited mouse and human SGLT2 activities at nanomolar ranges. In vivo single oral administration of YM543 dose-dependently and significantly reduced blood glucose level...
TP2019	[D-Ala2]-GIP (human)
	Highly potent GIP receptor agonist (EC50 = 630 ± 119 pM). Displays equivalent cAMP stimulating properties and improved resistance to enzymatic degradation compared to native GIP in cells expressing wild type GIP receptor. Improves glucose tolerance, insul
T35798	Massarigenin C
	Massarigenin C is a fungal metabolite that has been found inM. flavoroseaand has enzyme inhibitory activities.1,2Massarigenin C inhibits neuraminidasein vitro(IC50= 4.15 μM).2It is also an inhibitor of yeast α-glucosidase (IC50= 1.25 mM).1It reduces the postprandial peak in blood glucose levels in an oral sucrose tolerance test in normo- and hyperglycemic mice when administered at doses of 3.2, 10, and 31.6 mg/kg.
T25739L	Linogliride fumarate McN 3935,McN-3935,McN3935
	Linogliride fumarate 是Linogliride 的富马酸盐。Linogliride 是一种基于胍的胰岛素分泌抑制剂，也是pirogliride 的结构类似物，具有降血糖活性。它可以阻断胰腺β细胞膜上对ATP 敏感的钾通道，从而刺激胰岛素分泌并改善葡萄糖耐受性。
T79475	GPR119 agonist 2
	GPR119 agonist2（化合物43）是一种口服活性的GPR119激动剂。在啮齿动物中表现出优良的药代动力学特性，并能有效提高小鼠和大鼠的葡萄糖耐受性。GPR119 agonist2有望用于研究II型糖尿病。
T79649	CB1R/AMPK modulator 1	Cannabinoid Receptor	GPCR/G Protein
	CB1R/AMPK modulator 1 (Compound 38-S)为一种口服活性CB1R/AMPK调节剂，具有0.81 nM的Ki及3.9 nM的CB1R IC50。该化合物能够激活AMPK，且能降低食物摄入量和体重，同时改善葡萄糖耐量与胰岛素敏感性。
T69671	SR1903 TFA
	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-190...
T35622	FKGK 18
	FKGK 18 is an inhibitor of group VIA (GVIA) calcium-independent phospholipase A2 (iPLA2). It inhibits GVIA iPLA2 by 99.9% at 0.091 mole fraction in a mixed micelle activity assay and is selective for GVIA iPLA2 over GIVA cPLA2 and GV sPLA2 where it shows 80.8 and 36.8% inhibition, respectively. FKGK 18 inhibits iPLA2β activity in cytosolic extracts from INS-1 cells overexpressing iPLA2β (IC50 = ~50 nM) as well as iPLA2γ activity in mouse heart membrane fractions (IC50s = ~1-3 μM). It inhibits gl...
T35547	YW1128
	YW1128 is an inhibitor of Wnt/β-catenin signaling with an IC50 value of 4.1 nM in a reporter assay.1 It decreases protein levels of β-catenin in the presence of the GSK3β inhibitor lithium chloride and increases protein levels of Axin1 in HEK293 cells. YW1128 decreases lipid accumulation and the expression of gluconeogenic and lipogenic genes in Huh7 cells. It decreases the hepatic expression of Wnt target genes, improves glucose tolerance, and prevents body weight increases and hepatic lipid ac...
T16507	PF-5006739	Casein Kinase	Metabolism; Stem Cells
	PF-5006739 is an effective and selective inhibitor of CK1δ/ε (IC50s: 3.9 nM and 17.0 nM, respectively). PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selecti
T35816	ZLY032
	ZLY032 is a dual agonist of free fatty acid receptor 1 (FFAR1/GPR40; EC50= 68 nM in a FLIPR assay) and peroxisome proliferator-activated receptor δ (PPARδ; EC50= 102 nM in a reporter assay).1It is selective for FFAR1 and PPARδ over PPARα and PPARγ (EC50s = >10 μM for both). ZLY032 (40 mg/kg, twice per day) reduces blood glucose levels in an oral glucose tolerance test and decreases plasma total cholesterol and triglyceride levels in theob/obmouse model of metabolic disease.2It reduces hepatic st...
T36590	9-PAHSA
	Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are newly identified endogenous lipids regulated by fasting and high-fat feeding and associated with insulin sensitivity. Structurally, these esters are comprised of a C-16 or C-18 fatty acid (e.g., palmitoleic, palmitic, oleic, or stearic acid) linked to a hydroxylated C-16 or C-18 lipid. 9-PAHSA is a FAHFA in which palmitic acid is esterified to 9-hydroxy stearic acid. PAHSAs are the most abundant forms of FAHFA in serum as well as whi...
T35638	SR 1903
	SR 1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR).1 It is an inverse agonist of RORγ (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPARγ; IC50 = 209 nM) but does not activate it. SR 1903 (10 μM) inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1) in RAW 264.7 cells. It also inhibits LPS-induced expression of th...
T79358	PF-07247685	Endogenous Metabolite	Metabolism
	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	PF-07238025	Endogenous Metabolite	Metabolism
	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。

化合物

Cat.No: T2014

Synonym: CCG1423

Target: LRRK2, Rho, Ras

Cat.No: T11765

Target: Dehydrogenase, PDK

Cat.No: T3312

Synonym: AM2394

Target: Glucokinase

AMPK activator 4

Cat.No: T62238

Target: AMPK

P32/98 (hemifumarate)

Cat.No: T21979

Cat.No: T30169

Synonym: UNII-GC7THT248G,ASP8497,ASP 8497

Cat.No: T38771

Synonym: P32/98

Cat.No: T28784

Cat.No: T29154

Synonym: WB-403,WB 403

Cat.No: T71251

Cat.No: T11583

Target: Others

quercetin-3'-o-phosphate

Cat.No: T68132

[Pro3]-GIP (Mouse)

Cat.No: TP2020

N-Oleoyl Leucine

Cat.No: T35785

Cat.No: T60312

GPR40 agonist 5

Cat.No: T62542

Cat.No: T36142

Cat.No: T25739

Synonym: McN-3935,McN3935,McN 3935,Linogliridum,Linoglirida

Cat.No: T70390

[D-Ala2]-GIP (human)

Cat.No: TP2019

Cat.No: T35798

Linogliride fumarate

Cat.No: T25739L

Synonym: McN 3935,McN-3935,McN3935

GPR119 agonist 2

Cat.No: T79475

CB1R/AMPK modulator 1

Cat.No: T79649

Target: Cannabinoid Receptor

Cat.No: T69671

Cat.No: T35622

Cat.No: T35547

Cat.No: T16507

Target: Casein Kinase

Cat.No: T35816

Cat.No: T36590

Cat.No: T35638

Cat.No: T79358

Target: Endogenous Metabolite

Cat.No: T79357

Target: Endogenous Metabolite

Cat. No.	Product Name	Target	Signaling Pathways
T5S0669	Bergamottin 5-Geranoxypsoralen,Bergamotine,Bergaptin,佛手柑素	P450	Metabolism
	Bergamottin (5-Geranoxypsoralen) 是竞争性CYP1A1抑制剂(Ki:10.703 nM)。
T2740	trans-Cinnamic acid Isocinnamic acid,反式肉桂酸,Cinnamic acid,trans-3-Phenylacrylic acid,Phenylacrylic acid,Cinnamylic acid,3-Phenylacrylic acid,肉桂酸,Myricitrine	Endogenous Metabolite; Antibacterial	Metabolism; Microbiology/Virology
	trans-Cinnamic acid (Myricitrine) 通过改善体内葡萄糖耐量和体外刺激胰岛素分泌而发挥抗糖尿病活性。它是一种杀菌剂，对鱼的病原菌温和气单胞菌的 MIC 值为 250 μg/mL。
T4785	Oxfenicine 4-羟基-L-苯甘氨酸,4-Hydroxy-L-phenylglycine	Others	Others
	Oxfenicine (4-Hydroxy-L-phenylglycine) 是具有口服活性的肉碱棕榈酰转移酶-1 抑制剂。它在缺血期间保护心脏免受坏死组织的损害。它可抑制心脏中脂肪酸的氧化。
T3849	Kinsenoside 金线莲苷,(+)-Kinsenoside	Apoptosis; Nrf2	Apoptosis; Immunology/Inflammation
	Kinsenoside ((+)-Kinsenoside) 是从金盏花属植物中分离得到的主要活性成分，以 Nrf2 依赖的方式保护髓核细胞在氧化应激下的生存能力，防止细胞凋亡、衰老和线粒体功能障碍。它显示出显着的抗肝毒性和抗炎活性。
T38596	9,10-Dihydroxystearic acid
	9,10-Dihydroxystearic acid, an oxidation derivative of oleic acid, exhibits beneficial effects on glucose tolerance and insulin sensitivity in KKAy mice.
T73074	Phanginin A
	Phanginin A 是有效的口服活性SIK1激活剂，通过抑制糖异生、增加p-SIK1表达及降低p-CREB表达，达到降低血糖水平、改善葡萄糖耐量和血脂异常的效果，显示出其在2型糖尿病研究中的潜力。
T80007	Stevisalioside A	Phosphatase	Metabolism
	Stevisalioside A (Compound 2)，一种从甜叶菊根提取的化合物，展现出抗糖尿病的口服活性。该化合物有效抑制PTP1B，IC50为526.8 μM，并能降低Stevisalioside A引起的高血糖小鼠血糖水平，改善餐后血糖峰值及口服葡萄糖和胰岛素耐量测试结果。
TN3070	4beta-Hydroxywithanolide E	PARP; HSP; NF-κB; COX	Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; Neuroscience; NF-κB
	4beta-Hydroxywithanolide E(4bHWE) can inhibit the growth of colon cancer monolayer and spheroid cultures, it assert its anti-tumor activity in carcinogenic progression and develop into a dietary chemopreventive agent, it affects alternative splicing by mo

天然产物

Cat.No: T5S0669

Synonym: 5-Geranoxypsoralen,Bergamotine,Bergaptin,佛手柑素

Target: P450

trans-Cinnamic acid

Cat.No: T2740

Synonym: Isocinnamic acid,反式肉桂酸,Cinnamic acid,trans-3-Phenylacrylic acid,Phenylacrylic acid,Cinnamylic acid,3-Phenylacrylic acid,肉桂酸,Myricitrine

Target: Endogenous Metabolite, Antibacterial

Cat.No: T4785

Synonym: 4-羟基-L-苯甘氨酸,4-Hydroxy-L-phenylglycine

Target: Others

Cat.No: T3849

Synonym: 金线莲苷,(+)-Kinsenoside

Target: Apoptosis, Nrf2

9,10-Dihydroxystearic acid

Cat.No: T38596

Cat.No: T73074

Stevisalioside A

Cat.No: T80007

Target: Phosphatase

4beta-Hydroxywithanolide E

Cat.No: TN3070

Target: PARP, HSP, NF-κB, COX

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