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3
Cat. No. | Product Name | Target | Signaling Pathways |
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T12580 |
PTUPB
|
COX; Epoxide Hydrolase | Immunology/Inflammation; Metabolism; Neuroscience |
PTUPB 是强效的sEH(IC50:0.9 μM)和COX-2(IC50:1.26 μM)的双向抑制剂。 | |||
T27061 |
CP-24879 hydrochloride
CP-24879 HCl |
Others | Others |
CP-24879 hydrochloride (CP-24879 HCl) 是选择性的 delta5D/delta6D 联合抑制剂。它能显著降低肝细胞内脂质积聚和炎症损伤。它在脂肪-1 和 ω-3 处理的肝细胞中表现出优越的抗脂肪变性和抗炎作用,可用于非酒精性脂肪性肝炎的研究。 | |||
T2601 |
Vidofludimus
SC12267,4sc-101 |
Dehydrogenase; DNA/RNA Synthesis; Interleukin | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism |
Vidofludimus (SC12267) 是一种新型的二氢乳清酸脱氢酶 (DHODH) 小分子抑制剂,可在不影响淋巴细胞增殖的条件下抑制IL-17的分泌。 | |||
T77099 |
Nimacimab
JNJ 2463,RYI-018 |
Others | Others |
Nimacimab是一种重组人源化单克隆抗体可改善糖尿病和非酒精性脂肪性肝炎。 | |||
T14301 |
Apararenone
MT-3995 |
Glucocorticoid Receptor | Endocrinology/Hormones |
Apararenone (MT-3995) 是一种新型的、非甾体类盐皮质激素受体 (mineralocorticoid receptor) 拮抗剂,正在开发用于糖尿病性肾病和非酒精性脂肪性肝炎的研究。 | |||
T37184 |
CX08005
2-[(2-tetradecoxyphenyl)carbamoyl]benzoic acid |
Phosphatase | Metabolism |
CX08005 是一种蛋白酪氨酸磷酸酶 1B 抑制剂,可减轻与非酒精性脂肪肝相关的肝脏脂质蓄积和微循环障碍。 | |||
T65815 |
H-Asp(OtBu)-OtBu HCl
|
Amino Acids and Derivatives | Metabolism |
H-Asp(OtBu)-OtBu HCl 是一种天冬氨酸衍生物,可能用于研究神经功能的比较和非酒精类肝炎类代谢性疾病。 | |||
T9186 |
Ervogastat
PF-06865571 |
Transferase | Metabolism |
Ervogastat (PF-06865571) 是一种有效且耐受性良好的二酰基甘油酰基转移酶 2 抑制剂。 Ervogastat 可降低非酒精性脂肪性肝炎 (NASH) 中的脂肪变性和肝脏甘油三酯水平。 | |||
T76700 |
Simtuzumab
GS 6624,AB 0024 |
Monoamine Oxidase | Neuroscience |
Simtuzumab 是一种针对赖氨酰氧化酶样蛋白 2 (LOXL2) 的单克隆抗体。Simtuzumab 可用于治疗原发性硬化性胆管炎 (PSC),对非酒精性脂肪性肝炎引起的桥接性纤维化或代偿性肝硬化患者无效 。 | |||
T64334 |
Glycolithocholic acid, sodium salt
|
Others | Others |
Glycolithocholic acid, sodium salt 是 Glycolithocholic acid 的钠盐。Glycolithocholic acid 是一种甘氨酸结合的次级胆汁酸。Glycolithocholic acid 可用于诊断溃疡性结肠炎 (UC),非酒精性脂肪性肝炎 (NASH0) 和原发性硬化性胆管炎 (PSC)。 | |||
T67974 |
Berberine ursodeoxycholate
HTD1801,BUDCA |
||
Berberine ursodeoxycholate (HTD1801) 是一种口服有效的降血脂剂 ,是 Berberine 和 Ursodeoxycholic acid 的一种离子盐。Berberine ursodeoxycholate 具有广泛的代谢活性,可显著降低肝脏脂肪含量。Berberine ursodeoxycholate 可用于研究高脂血症、非酒精性脂肪性肝炎 (NASH) 和糖尿病。 | |||
T77059 |
Leronlimab
PRO 140 |
CCR | Immunology/Inflammation; Microbiology/Virology |
Leronlimab (PRO 140) 是一种人源化 IgG4 抗 CCR5 单克隆抗体。leronlimumab 具有抗 HIV 病毒活性和抗肿瘤活性, 抑制 CCR 介导的 HIV-1 病毒和小鼠肿瘤模型中癌细胞转移。Leronlimab 可用于研究 HIV 非酒精性脂肪性肝炎 (NASH) 和乳腺癌。 | |||
T17236 |
Volixibat
SHP626,LUM002 |
Others | Others |
Volixibat is a highly selective and competitive apical sodium-dependent bile acid transporter inhibitor. Volixibat has the potential for treatment for non-alcoholic steatohepatitis. | |||
T11448 | GOAT-IN-1 | Others | Others |
GOAT-IN-1 is an inhibitor of ghrelin O-acyltransferase (GOAT), which could be useful for the prophylaxis or treatment of diabetes, hyperlipidemia, non-alcoholic fatty liver, Alzheimer’s disease, Parkinson’s disease, cerebrovascular dementia, cerebral infa | |||
T35801 |
ML-262
|
||
ML-262 is an inhibitor of hepatic lipid droplet formation (IC50 = 6.4 nM in murine AML-12 cells), which is associated with non-alcoholic fatty liver disease. ML-262 does not induce cytotoxicity (up to 33 μM) or inhibit fatty acid uptake (up to 50 μM). | |||
T11661 |
INT-767
|
FXR; GPCR19 | GPCR/G Protein; Metabolism |
INT-767 是一种高效的法尼类固醇 X 受体 (FXR)/TGR5 双激动剂,可预防 NASH 并促进内脏脂肪棕色脂肪生成和线粒体功能,可用于研究非酒精性脂肪性肝炎。 | |||
T62029 |
ML261
|
||
ML261 是肝脂滴形成的抑制剂,IC50值为 69.7 nM。ML261 在非酒精性脂肪性肝病 (NAFLD) 和炎症中具有研究价值。 | |||
T83421 |
1-Palmitoyl-sn-glycerol 3-phosphate
1-P-GPA |
||
1-Palmitoyl-sn-glycerol 3-phosphate (1-P-GPA) 是内源性代谢物,常用于非酒精性脂肪性肝病的研究。 | |||
T74421 |
Pemvidutide
|
||
Pemvidutide 是一种GLP-1R/GCGR 双重激动剂,可导致体重、肝脏脂肪和血清脂质的显著降低。Pemvidutide 可用于非酒精性脂肪性肝炎 (NASH) 和肥胖症的研究。 | |||
T78658 |
Pemvidutide TFA
|
||
Pemvidutide (TFA) 是一款针对GLP-1R/GCGR的双重激动剂,有助于显著降低体重、肝脏脂肪以及血清脂质水平。该化合物主要适用于非酒精性脂肪性肝炎(NASH)和肥胖症的研究领域。 | |||
T21978 |
p-nitro-Pifithrin-α
|
||
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]. | |||
T78093 |
Cisd2 agonist 1
|
Others | Others |
Cisd2 agonist 1 (Compound 4q)为一种EC50值为34 nM的Cisd2激动剂,可增强Cisd2表达并改善非酒精性脂肪肝疾病(NAFLD)的病理改变,同时具备良好的代谢稳定性,适用于NAFLD研究。 | |||
T63777 |
QH536
|
||
QH536 是 HMGCR 的有效降解剂 (EC50: 0.22 μM)。QH536 表现出抗炎效果,并没有诱导胆固醇在细胞内积聚的副作用。QH536 能够用于研究心血管疾病和非酒精性脂肪性肝炎。 | |||
T81802 |
MGAT2-IN-4
|
||
MGAT2-IN-4(compound 33)是一种针对单酰基甘油转移酶2(MGAT2)的抑制剂,显示出良好的肝脏代谢稳定性,适用于肥胖症、糖尿病以及非酒精性脂肪性肝炎(NASH)的研究。 | |||
T35443 |
1-Palmitoyl-2-Stearoyl-3-Oleoyl-rac-glycerol
|
||
1-Palmitoyl-2-stearoyl-3-oleoyl-rac-glycerol is a triacylglycerol that contains palmitic , stearic , and oleic acid at the sn-1, sn-2, and sn-3 positions, respectively. It has been detected in RAW 264.7 cells by neutral loss MS. Increased serum levels of 1-palmitoyl-2-stearoyl-3-oleoyl-rac-glycerol are a potential biomarker for non-alcoholic fatty liver disease (NAFLD). | |||
T74996 |
FXR agonist 3
|
||
FXR agonist3 是一种抗 NASH 试剂,通过激活 FXR 起作用。FXR agonist3 抑制 COL1A1、TGF-β1、α-SMA 和 TIMP1的表达,具有抗纤维化活性。FXR agonist3 显著减轻肝脏脂肪变性和炎症,改善肝纤维化水平。 | |||
T79698 |
S217879
|
||
S217879是一种选择性高效的NRF2激活剂,能够破坏KEAP1-NRF2之间的相互作用,从而强有力地激活NRF2通路。它可应用于非酒精性脂肪性肝炎(NASH)的研究领域。 | |||
T35636 |
SHS4121705
|
||
SHS4121705 is an orally bioavailable mitochondrial uncoupler.1It increases oxygen consumption rate in L6 rat myoblast cells with an EC50value of 4.3 μM. SHS4121705 (25 mg/kg per day in the diet) reduces hepatic steatosis, liver triglyceride levels, and plasma alanine aminotransferase (ALT) levels in Stelic animal model (STAM) mice, a model of non-alcoholic steatohepatitis (NASH). 1.Salamoun, J.M., Garcia, C.J., Hargett, S.R., et al.6-Amino[1,2,5]oxadiazolo[3,4-b]pyrazin-5-ol derivatives as effic... | |||
T72889 | FXR agonist 4 | ||
FXR agonist4,一种法尼酯X受体(FXR)激动剂,具有1.05 μM的EC50值。该化合物在DIO小鼠模型中有效地改善了高脂血症、肝脏脂肪变性、胰岛素抵抗以及肝脏炎症,因此可用于非酒精性脂肪性肝病(NAFLD)的研究。 | |||
T77175 | Efruxifermin | ||
Efruxifermin为Fc-FGF21融合蛋白,由人IgG1Fc结构域与修饰的人FGF21连接。相较于天然人FGF21,Efruxifermin展示了增强的受体亲和力及延长的半衰期,适用于非酒精性脂肪性肝炎研究。 | |||
T79733 | NLRP3-IN-20 | NOD-like Receptor (NLR) | Immunology/Inflammation |
NLRP3-IN-20(compound 11)是一款口服活性的NLRP3炎症小体抑制剂,其抑制IL-1β分泌的IC50值为25 nM。该化合物展现出卓越的药代动力学性质,并在非酒精性脂肪性肝炎、致命性感染性休克以及结肠炎模型中证明了其显著疗效。 | |||
T62594 |
THR-β agonist 2
|
||
THR-β agonist 2 是一种 THR-β 的有效激动剂。THR-β agonist 2 具有潜力进行代谢疾病的研究(如肥胖、高脂血症、高胆固醇血症、糖尿病和其他病症,如脂肪变性和非酒精性脂肪性肝炎 (NASH)、动脉粥样硬化和其他相关病症和疾病)。 | |||
T63697 | THR-β agonist 3 | ||
THR-β agonist 3 是 THR-β 的有效激动剂。THR-β agonist 3 对代谢疾病表现出研究潜力,例如肥胖、高脂血症、高胆固醇血症、糖尿病和其他病症如脂肪变性和非酒精性脂肪性肝炎 (NASH)、动脉粥样硬化和其他相关病症和疾病。 | |||
T63515 |
THR-β agonist 4
|
||
THR-β agonist 4 是 THR-β 的有效激动剂。THR-β agonist 4 对代谢疾病表现出研究潜力,如高脂血症、肥胖、高胆固醇血症、糖尿病和其他病症如脂肪变性和非酒精性脂肪性肝炎 (NASH)、动脉粥样硬化和其他相关病症和疾病 。 | |||
T62968 | PPARα/δ agonist 1 | ||
PPARα/δ agonist 1 是一种有效的 PPARα/PPARδ 双重激动剂,对 PPARα和 PPARδ 的 EC50 值分别为 7.0 nM 和 8.4 nM。PPARα/δ agonist 1 对 PPARγ 表现出很高的选择性 (EC50: 1316.1 nM)。PPARα/δ agonist 1 具有潜力进行非酒精性脂肪性肝炎的研究。 | |||
T78095 |
Demethyleneberberine chloride
|
NF-κB | NF-κB |
Demethyleneberberine chloride是一种具有线粒体靶向性的天然抗氧化剂,能通过抑制NF-κB通路及调节Th细胞平衡来缓解小鼠结肠炎并抑制炎症。此外,作为一种AMPK激活剂,该化合物亦用于非酒精性脂肪性肝病(NAFLD)的研究。 | |||
T10964L |
DB1976 dihydrochloride
DB1976 hydrochloride,DB1976 2HCl |
Apoptosis; NF-κB | Apoptosis; NF-κB |
DB1976 dihydrochloride (DB1976 2HCl) ,一种转录因子 PU.1 抑制剂,具有潜在抗炎活性,可在体内实验中减缓小鼠的炎症和纤维化,改善了葡萄糖稳态和血脂异常。DB1976 dihydrochloride 促进细胞凋亡,可用于研究代谢功能障碍和非酒精性脂肪性肝炎。 | |||
T62052 |
AMPK activator 6
|
||
AMPK activator 6 (Compound GC) 可降低 HepG2 和 3T3-L1 细胞中的脂质含量并激活AMPK 通路。AMPK activator 6 对血清中甘油三酯 (TG)、总胆固醇 (TC)、低密度脂蛋白-C (LDL-C) 和其他生化指标的增加有显著的抑制作用。AMPK activator 6 在非酒精性脂肪肝(NAFLD)和代谢综合征中有研究价值。 | |||
T79783 |
NSC 48160
|
Apoptosis | Apoptosis |
NSC 48160对胰腺癌细胞具有抑制作用,IC50分别针对CPFAC-1为84.3μM,对BxPC-3为94.5μM。此外,NSC 48160能够诱导胰腺癌细胞(apoptosis)。该化合物亦能改善代谢综合征症状,包括NASH、肥胖及脂质代谢紊乱。 | |||
T73414 | EDP-305 | ||
EDP-305是一种具有选择性的口服farnesoid X受体(FXR)激动剂,其EC50值分别为34 nM(CHO细胞嵌合性FXR)和8 nM(HEK细胞全长FXR)。该化合物展现了强大且持久的抗纤维化效果,并适用于原发性胆道胆管炎(PBC)与非酒精性脂肪性肝炎(NASH)的研究。 | |||
T82254 | GSK-LSD1 | Histone Demethylase | Chromatin/Epigenetic |
GSK-LSD1是一种LSD1抑制剂,能够降低肥胖小鼠模型的摄食量和体重,同时提升胰岛素敏感性与血糖控制。此外,GSK-LSD1对NAFLD也有改善作用,并能抑制COVID-19患者PBMC中SARS-CoV-2诱导的细胞因子释放。GSK-LSD1对抑制癌症的生长与转移也显示出潜在效果。 | |||
T64144 |
FXR antagonist 1
|
||
FXR antagonist 1 是一种选择性的、口服具有活力的肠道 FXR 拮抗剂,其 IC50 值为 2.1 μM。FXR antagonist 1 能够拮抗肠道 FXR,并反馈激活肝脏 FXR,进而选择性地抑制肠道 FXR 信号。FXR antagonist 1 可改善 NASH (非酒精性脂肪性肝炎) 模型中的肝脏脂肪变性、炎症和纤维化,能够用于研究 NASH。 | |||
T82848 | BMS-986172 | Acyltransferase | Metabolism |
BMS-986172是一种高选择性的口服MGAT2抑制剂,针对hMGAT2和mMGAT2显示出的IC50分别为4.6 nM和20 nM。该化合物在体外具有较长的半衰期(T1/2>120分钟),能够减少食物摄入和体重。BMS-986172在治疗肥胖和NASH等代谢性疾病方面显示出研究潜力。 | |||
T35799 |
MBX-8025 (sodium salt)
|
||
MBX-8025 is an agonist of peroxisome proliferator-activated receptor δ (PPARδ).1 It is greater than 750- and 2,500-fold selective for PPARδ over PPARα and PPARγ. MBX-8025 (10 mg/kg per day for eight weeks) reduces increases in fasting blood glucose and serum insulin levels, and decreases insulin resistance in Alms1 mutant (foz/foz) mice fed an atherogenic diet as a model of diet-induced obesity, type 2 diabetes, and non-alcoholic steatohepatitis (NASH).2 It also decreases serum alanine transamin... | |||
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... | |||
T35881 |
Resolvin E2
|
||
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... | |||
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。 | |||
T37522 | Teneligliptin | ||
Teneligliptin (MP-513) is a potent chemotype prolylthiazolidine-based DPP-4 inhibitor, which competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM. Teneligliptin (MP-513) inhibits all these DPP-4 enzymes in a concentration-dependent manner. The IC50s of Teneligliptin (MP-513) for rhDPP-4, human plasma, and rat plasma are 0.889, 1.75, and 1.35 nM, respectively. A study of enzyme inhibition kinetics is conducted for Teneligliptin (M... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T31964 |
Glycolithocholic acid
Lithocholic acid glycine conjugate,甘氨石胆酸,Lithocholylglycine |
Others | Others |
Glycolithocholic acid (Lithocholic acid glycine conjugate) 属于内源性代谢产物,是甘氨酸结合的次级胆汁酸。它可用于诊断非酒精性脂肪性肝炎,溃疡性结肠炎和原发性硬化性胆管炎。 | |||
T37526 |
2-Oleoylglycerol
2-Oleoyl Glycerol,2-OG,2-Monoolein |
GPR | Endocrinology/Hormones; GPCR/G Protein |
2-Oleoylglycerol 是一种存在于棕榈仁、葵花籽和米糠中的脂质。2-Oleoylglycerol 可当作一种 GPR119 激动剂,具有神经保护作用,可诱导胰高血糖素样肽 1 (GLP-1) 分泌。2-Oleoylglycerol 可用于非酒精性脂肪性肝炎造模。 | |||
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... |