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Cat. No. | Product Name | Target | Signaling Pathways |
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T4524 |
SBC-110736
SBC110736 |
Others; Serine/threonin kinase | Cell Cycle/Checkpoint; Metabolism; Others |
SBC-110736 是一种蛋白转化酶枯草杆菌蛋白酶 9 型 (PCSK9) 抑制剂。 | |||
T3283 |
Cetilistat
新利司他,ATL-962 |
Lipid | Metabolism |
Cetilistat (ATL-962) 是胰腺脂肪酶 (pancreatic lipase) 抑制剂,能够抑制大鼠脂肪酶(IC50:54.8 nM)和人胰脂肪酶(IC50:5.95 nM)的活性,可用作有效的抗肥胖药。 | |||
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。 | |||
T10035 |
10,12-Tricosadiynoic acid
TDA,TCDA |
Acyltransferase | Metabolism |
10,12-Tricosadiynoic acid 是一种口服有效的酰基辅酶 A 氧化酶-1 (ACOX1) 抑制剂,具有高特异性,选择性,高亲和力的特点。10,12-Tricosadiynoic acid 可改善线粒体脂质和 ROS 代谢,在高脂饮食或肥胖引起的代谢性疾病中有研究的价值。 | |||
T9025 |
KY19382
2H-Indol-2-one, 5,6-dichloro-3-[1,3-dihydro-3-(methoxyimino)-2H-indol-2-ylidene]-1,3-dihydro-Ky19382,A3051 |
Others; GSK-3; Wnt/beta-catenin | Cytoskeletal Signaling; Others; PI3K/Akt/mTOR signaling; Stem Cells |
KY19382 (2H-Indol-2-one, 5,6-dichloro-3-[1,3-dihydro-3-(methoxyimino)-2H-indol-2-ylidene]-1,3-dihydro-Ky19382) 是一种具有口服活性的 CXXC5-DVL (IC50:19 nM) 和 GSK3β (IC50:10 nM) 的双重抑制剂。它通过对 CXXC5-DVL 相互作用和 GSK3β 活性的抑制作用激活 Wnt/β-catenin 信号传导。它可用于高脂饮食诱发的代谢性疾病的研究。 | |||
T8732 |
CTPI-2
|
Others; Mitochondrial Metabolism | Metabolism; Others |
CTPI-2 是一种特异性线粒体柠檬酸盐载体SLC25A1抑制剂,KD=3.5 μM,具有抗肿瘤作用。它能够抑制糖酵解、PPARγ 及其下游靶点葡萄糖转运蛋白 GLUT4。它阻断非酒精性脂肪性肝炎逆转脂肪变性的显著改变,防止演变为脂肪性肝炎,减少肝脏和脂肪组织中炎性巨噬细胞的浸润,并显著减轻由高脂肪饮食引起的肥胖。 | |||
T61619 | XN methyl pyrazole | ||
XN methyl pyrazole exhibits beneficial effects on diet-induced obesity and enhances energy expenditure in mice fed with a high-fat diet [1]. | |||
T37904 |
Gadoleic Acid
|
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Gadoleic acid is a monounsaturated fatty acid.1,2It inhibits the dsDNA binding activity of p53 when used at a concentration of 1.2 nM.1Hepatic levels of gadoleic acid are reduced in rats fed a high-fat or a high-fat high-cholesterol diet and increased in rats fed a high-cholesterol diet.2 1.Iijima, H., Kasai, N., Chiku, H., et al.The inhibitory action of long-chain fatty acids on the DNA binding activity of p53Lipids41(6)521-527(2006) 2.Serviddio, G., Bellanti, F., Villani, R., et al.Effects of ... | |||
T40950 | A3334 | ||
A3051, is a robust and orally active inhibitor of CXXC5-DVL with an IC 50 of 63.06 nM. Its applications include research into phenotypes associated with obesity, diabetes, and NASH that are induced by high fat diet (HFD) and methionine-choline deficient diet (MCD). | |||
TP1552 |
TLQP-30
|
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Chronic intracerebroventricular (ICV) injection of a VGF peptide named TLQP-21 increased resting energy expenditure and temperature in mice. Furthermore, in mice fed a high-fat diet, the same peptide prevented the increase in body and white adipose tissue | |||
T33663 |
Nicotinamide Riboside Triflate
SRT 647 Triflate,SRT 647,Nicotinamide Riboside,Nicotinamide Ribose,SRT-647,SRT647,SRT647 Triflate,SRT-647 Triflate |
Sirtuin | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Nicotinamide Riboside Triflate (SRT647 Triflate) 是一种天然NAD前体,可增加NAD水平,可增强氧化代谢并防止高脂肪饮食引起的肥胖,KE 激活SIRT3可防止噪音引起的听力损失,可用于研究肌肉萎缩。 | |||
T34767 |
TA-1887
TA 1887,TA1887 |
||
TA-1887 is a new type of selective inhibitor of sglt2 for the treatment of type 2 diabetes. It has a significant hypoglycemic effect in KK (HF-KK) mice fed a high-fat diet. TA-1887 has good pharmacokinetic characteristics and significantly increases UGE | |||
T35603 |
Oleic Acid-2,6-diisopropylanilide
|
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AcylCoA:cholesterol acyltransferase (ACAT) is an intracellular cholesteryl ester synthase tied closely to the absorption of dietary cholesterol. Oleic acid-2,6-diisopropylanilide is an inhibitor of acylCoA:cholesterol acyltransferase with an IC50 of 7 nM. When co-administered to rabbits or rats fed a high fat, high cholesterol diet, oleic acid-2,6-diisopropylanilide decreased low density lipoproteins and elevated high density lipoprotein levels when administered at 0.05%. | |||
T64006 |
Lipid-lowering agent-1
|
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Lipid-lowering agent-1 是有效的降脂剂,能够明显抑制低密度脂蛋白胆固醇 (LDLC) 和促进高密度脂蛋白胆固醇 (HDLC) 产生的药理作用。Lipid-lowering agent-1 能够明显降低高脂饮食大鼠的脂肪。 | |||
T40059 | Nicotinamide riboside tartrate | ||
Nicotinamide riboside tartrate (NRT) is an oral NAD+ precursor that raises NAD+ levels, activates SIRT1 and SIRT3, and serves as a vitamin B3 (niacin) source. NRT also improves oxidative metabolism and protects against metabolic abnormalities induced by a high-fat diet. Furthermore, NRT mitigates cognitive decline in a transgenic mouse model of Alzheimer's disease. | |||
T40060 |
Nicotinamide riboside malate
|
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Nicotinamide riboside malate is an orally active NAD+ precursor that elevates NAD+ levels and stimulates the activity of SIRT1 and SIRT3. Functioning as a vitamin B3 (niacin) source, it augments oxidative metabolism and provides protection against metabolic abnormalities induced by a high-fat diet. Additionally, Nicotinamide riboside malate mitigates cognitive decline in a genetically modified mouse model of Alzheimer's disease. | |||
T21978 |
p-nitro-Pifithrin-α
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p-nitro-Pifithrin-α is a cell-permeable analog of pifithrin-α, a potent p53 inhibitor. It suppresses p53-mediated TGF-β1 expression in HK-2 cells and inhibits the activation of caspase-3 by Zika virus (ZIKV) strains. Moreover, p-nitro-Pifithrin-α attenuates steatosis and liver injury in mice subjected to a high-fat diet, mitigating the effects of non-alcoholic fatty liver disease [1] [2] [3] [4]. | |||
T36130 |
22(S)-hydroxy Cholesterol
22(S)-hydroxy Cholesterol,22β-hydroxy Cholesterol |
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22(S)-hydroxy Cholesterol is a synthetic oxysterol and a modulator of the liver X receptor (LXR). [1] t prevents monocyte chemoattractant protein 1 (MCP-1) expression induced by the LXR agonist GW 3965 in primary hepatocytes and downregulates mRNA expression of the LXR target genes CD36, ACSL1, and SCD-1 in human myotubes. It decreases triacylglycerol and diacylglycerol synthesis from labeled palmitate and acetate, respectively, in human myoblasts by 50% when used at a concentration of 10 uM. 22... | |||
T79678 | PPARγ-IN-2 | PPAR | DNA Damage/DNA Repair; Metabolism |
PPARγ-IN-2 (Compound 5a) 是一款PPARγ抑制剂,可在3T3-L1前脂肪细胞中抑制TG积累,EC50值为0.106 μM。该化合物能够减轻HFC诱导的肥胖及相关代谢综合症状,同时降低脂肪组织内脂质的堆积。 | |||
T35786 |
O-7460
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In humans, two forms of diacylglycerol lipase, DAGLα and DAGLβ, generate the endocannabinoid 2-arachidonoyl glycerol by attacking DAG at the sn-1 position. O-7460 is a selective inhibitor of 2-AG biosynthesis via DAGLα (IC50 = 690 nM). It demonstrates much weaker inhibition towards human monoacylglycerol lipase and rat brain fatty acid amide hydrolase (IC50s > 10 μM) and does not bind to CB1 or CB2 cannabinoid receptors (Kis > 10 μM). At 0-12 mg/kg, i.p. in mice, O-7460 was reported to dose-depe... | |||
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... | |||
T35547 |
YW1128
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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... | |||
T36586 |
12-PAHSA
|
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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 either a C-16 or C-18 hydroxy substituent. 12-PAHSA is a FAHFA in which palmitic acid is esterified at the 12th carbon of hydroxy stearic acid. Among the FAHFA family members, PAHSAs ar... | |||
T72635 |
AMPD2 inhibitor 2
|
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AMPD2 inhibitor 2是一种针对AMP脱氨酶2 (AMPD2) 的高效抑制剂,具有针对hAMPD2和mAMPD2较低的IC50值,分别为0.1 μM 和 0.28 μM。该化合物可能对于探究AMPD2在高脂肪饮食小鼠模型中的生理功能具有重要意义。 | |||
T35638 |
SR 1903
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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... | |||
T35881 |
Resolvin E2
|
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Resolvin E2 (RvE2) is a member of the specialized pro-resolving mediator (SPM) family of bioactive lipids.1It is produced from eicosapentaenoic acidviaan 18-HEPE intermediate, which is formed by aspirin-acetylated COX-2-mediated oxidation of EPA, by 5-lipoxygenase (5-LO) in human polymorphonuclear (PMN) neutrophils.2,3RvE2 (20 ng/animal) inhibits increases in inflammatory exudate neutrophil infiltration in a mouse model of peritonitis induced by zymosan A .3Hepatic RvE2 levels are increased in m... | |||
T79446 |
INF200
|
NOD-like Receptor (NLR) | Immunology/Inflammation |
INF200(compound 5)是一种磺酰脲衍生的抑制剂,既能抑制NLRP3也能抑制NLRP3介导的焦亡(pyroptosis)。在HFD诱导的大鼠模型上,INF200对心脏代谢表现出有益效果,并且在(10 μM)浓度下减少了人巨噬细胞中IL-1β的释放,表现出抗炎特性。它还能改善血糖控制和脂质水平,降低全身炎症和心功能障碍的标志物(尤其是BNP水平)。此外,INF200在血流动力学评估中还可提升心肌损伤后的缺血/再灌注损伤(IRI)恢复。 | |||
T83906 |
Tirzepatide sodium
LY3298176 |
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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... | |||
T35787 |
Obestatin (human) (trifluoroacetate salt)
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Obestatin is a 23 amino acid peptide hormone with a conserved C-terminal glycine residue and amidation site that is formed by cleavage of the ghrelin and obestatin prepropeptide.1It binds to the orphan receptor GPR39 (Kd= 1 nM) and stimulates cAMP production in CHO and HEK293 cells overexpressing human GPR39. Obestatin inhibits contraction of isolated mouse jejunum muscle strips induced by ghrelin .In vivo, obestatin (12.5-1,000 nmol/kg) suppresses food intake in a time- and dose-dependent manne... |
Cat. No. | Product Name | Target | Signaling Pathways |
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T3804 |
Neomangiferin
Mangiferin 7-glucoside,新芒果苷 |
Phosphatase | Metabolism |
Neomangiferin (Mangiferin 7-glucoside) 是一种天然的 C-glucosyl xanthone,分离自干燥的Anemarrhena asphodeloides 的根茎中。它能够减轻大鼠高脂饮食诱导的非酒精性脂肪性肝病 (NAFLD)。 | |||
T19924 |
Rhododendrol
Betuligenol,Frambinol,杜鹃醇 |
Others | Others |
Rhododendrol (Frambinol) 是一种黑色素合成物,防止雄性小鼠高脂饮食引起的体重升高和增加雄性小鼠白色脂肪细胞的脂肪分解。Rhododendrol 可用作美白/美白化妆品抑制剂。 | |||
T13795 |
Nicotinamide riboside
|
Sirtuin | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Nicotinamide riboside 是维生素 B3 的来源,可以增强氧化代谢并防止高脂肪饮食诱导的代谢异常。它是具有口服活性的 NAD+的前体,增加 NAD+水平并激活SIRT1和SIRT3,可用于研究阿尔茨海默氏病的认知退化。 | |||
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。 | |||
T3921 |
Punicalagin
安石榴甙,安石榴苷 |
SARS-CoV; HBV | Microbiology/Virology |
Punicalagin 是一种在石榴中发现的主要鞣花单宁,是可逆且非竞争性的3CLpro 抑制剂,有抗氧化、抗炎和抗癌作用。它有潜力研究 COVID-19 。 | |||
T4S2128 |
Bilobetin
白果双黄酮,白果素 |
PKA; PPAR | DNA Damage/DNA Repair; Metabolism; Tyrosine Kinase/Adaptors |
Bilobetin 是银杏的活性成分,可改善胰岛素抵抗,增加肝脏对脂质的吸收和氧化,降低极低密度脂蛋白甘油三酯分泌和血液甘油三酯水平,增强组织中 β-氧化的酶的表达和活性,并减弱甘油三酯及其代谢产物的积累。它还增加了 PPARα的磷酸化,核转位和活性,并伴随着 cAMP 水平和 PKA 活性的升高。 | |||
T3S1513 |
(20R)-Protopanaxadiol
Protopanaxadiol,20R-Protopanaxadiol,(20R)-原人参二醇,(20R)-Protopanaxdiol |
Others; Antibacterial | Microbiology/Virology; Others |
(20R)-Protopanaxadiol ((20R)-Protopanaxdiol) 是黑参中20(R)-人参皂甙 Rg3的一种三萜皂苷代谢物。它抑制幽门螺杆菌的生长,有抗肿瘤活性和细胞毒性。 | |||
T6S0221 |
Eriocitrin
eriodictyol 7-rutinoside,圣草次甙,Eriodictyol-7-O-Rutinoside,Eriodictioside,圣草次甙;圣草次苷,Eriodictyol glycoside |
Apoptosis; Carbonic Anhydrase | Apoptosis; Metabolism |
Eriocitrin (Eriodictyol-7-O-Rutinoside) 是从柠檬中分离出来的一种黄酮类天然产物,是强效的抗氧化剂。它通过激活线粒体涉及的内在信号传导途径来触发细胞凋亡。它通过上调 p53、cyclin A、cyclin D3 和 CDK6 使 S 期细胞周期停滞,从而抑制肝癌细胞的增殖。 | |||
TN1206 |
2,4,6-Trihydroxybenzaldehyde
|
Others | Others |
2,4,6-Trihydroxybenzaldehyde 是一种天然产物。 2,4,6-三羟基苯甲醛是一种潜在的抗肥胖治疗药物,可抑制 C57BL/6 小鼠的 3T3-L1 细胞中的脂肪细胞分化和高脂饮食诱导的脂肪积累。它也是一种有效的抗糖尿病药物。 2,4,6-三羟基苯甲醛具有潜在的抗癌活性。 | |||
T3976 |
Cytosporone B
Csn-B,Dothiorelone G |
Others | Others |
Cytosporone B (Dothiorelone G) 是一种天然存在的核孤儿受体Nur77/NR4A1激动剂(EC50=0.278 nM)。 | |||
T36585 |
Isodeoxycholic Acid
isoDCA |
Chloride channel; Antibacterial | Membrane transporter/Ion channel; Microbiology/Virology |
Isodeoxycholic Acid 是一种胆汁酸,由肠道细菌通过脱氧胆酸的表聚作用形成。Isodeoxycholic acid 的临界胶束浓度高于二氯苯甲醚,这表明它的去污活性降低了,而且在抑制七种肠道共生细菌生长方面的活性低于二氯苯甲醚。Isodeoxycholic Acid(0.1%)能抑制几种艰难梭菌菌株在牛磺胆酸诱导下的孢子萌发,并能降低艰难梭菌培养上清对 Vero 细胞的细胞毒性。在高脂饮食诱发肥胖的大鼠模型中,血浆中的Isodeoxycholic acid 水平比正常饮食的大鼠低。 | |||
TN4997 |
Serpentine
|
IGF-1R | Tyrosine Kinase/Adaptors |
Serpentine 是一种玫瑰花根中的生物碱,可用作胰岛素增敏剂,以协助胰岛素降低血糖。Serpentine 可激活 AMPK 磷酸化,从而刺激C2C12细胞对葡萄糖的摄取。Serpentine 可增加了肌肉组织中GSK-3β mRNA的表达,从而增强葡萄糖摄取。Serpentine 显著增加胰高血糖素分泌和肝糖异生。在高脂肪饮食/链脲佐菌素(HFD/STZ)诱导的糖尿病小鼠中,Serpentine 显著延长了胰岛素的降血糖时间,显著降低了外源性胰岛素的使用,抑制了内源性胰岛素的分泌。 | |||
T35624 | Ajoene | ||
Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities, including antibacterial, anticancer, antiplatelet, and antioxidant properties.1,2,3,4It is active against Gram-positive (MICs = 5-160 µg/ml) and Gram-negative bacteria (MICs = 136-200 µg/ml), as well as yeasts (MICs = 10-20 µg/ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 µM), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 µM).2It reduces... |