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19

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
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。
T8763	PTGR2-IN-1 PTGR2-IN-22	Others	Others
	PTGR2-IN-1 是有效的 PTGR2抑制剂，IC50为 ~0.7 μM。它能够提高转染 PTGR2 的 HEK293T 细胞 15-keto-PGE2 依赖的 PPARγ 转录活性。
T28501	Ragaglitazar NNC61-0029,NN-622,(-)-DRF-2725,NNC-61-0029,NN 622,NNC 61-0029	PPAR	DNA Damage/DNA Repair; Metabolism
	Ragaglitazar(NNC-61-0029) 是一种有效的 PPARα和 PPARγ双重激动剂，在动物模型中显示出有效的降脂和胰岛素增敏作用。Ragaglitazar 可用于研究 2 型糖尿病。
T21587	Muraglitazar Pargluva,BMS-298585	PPAR	DNA Damage/DNA Repair; Metabolism
	Muraglitazar (BMS-298585) 是一种 PPAR α/γ的双激动剂，用于治疗2型糖尿病及相关血脂异常。Muraglitazar 对人 PPARα (EC50 = 320 nM)和 PPARγ(EC50 = 110 nM)具有较强的体外活性。
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。
T61743	PPARγ agonist 2
	PPARγ agonist 2 is a highly effective compound that acts as a partial agonist for PPARγ. It exhibits significant potential for utilization in metabolic disease research [1].
T61836	Pioglitazone potassium
	Pioglitazone potassium (U 72107) is an orally active and selective agonist of peroxisome proliferator-activated receptor gamma (PPARγ). It demonstrates high affinity binding to the ligand-binding domain of PPARγ, with an EC50 of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone potassium has applications in diabetes research [2] [3] [4].
T73842	Leriglitazone hydrochloride
	Leriglitazone (Hydroxypioglitazone) hydrochloride，吡格列酮的代谢产物。Leriglitazone (Hydroxypioglitazone) hydrochloride 是PPARγ激动剂，通过稳定PPARγ(AF-2) 共激活剂结合表面和增强共激活剂结合能力，提供高转录效力。 Leriglitazone (Hydroxypioglitazone) hydrochloride 与 PPARγC (LBD) 结合，其Ki 值为 1.2 μM，诱导PPARγ(LBD) 转录效率，EC50为 680 nM。
T35717	N-desmethyl Rosiglitazone
	N-desmethyl Rosiglitazone is a major metabolite of rosiglitazone , a potent and selective PPARγ ligand present in formulations that have been used to treat type 2 diabetes. Rosiglitazone is metabolized by the cytochrome P450 (CYP) isoform CYP2C8 to form N-desmethyl rosiglitazone.
T61848	Rosiglitazone potassium
	Rosiglitazone (BRL 49653) potassium is a potent and selective PPARγ agonist (EC 50: 60 nM, Kd: 40 nM), administered orally. It also serves as an activator of TRPC5 (EC 50: 30 μM) and an inhibitor of TRPM3. This compound, widely used in research, has shown promise in investigating obesity, diabetes, senescence, and ovarian cancer [1] [2] [4] [7].
T37634	17-oxo-7(Z),10(Z),13(Z),15(E),19(Z)-Docosapentaenoic Acid
	Docosapentaenoic acid (DPA) is a ω-3 fatty acid found in fish oils. 17-oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid is a metabolite of lipoxygenase-mediated oxidation of DPA that is produced endogenously by aspirin-enhanced COX-2 activity. It has been shown to activate Nrf2-dependent antioxidant gene expression, to act as a PPARγ agonist (EC50 = ~200 nM), and to inhibit pro-inflammatory cytokine and nitric oxide production at biological concentration ranges (5-25 μM).
T71306	Gemfibrozil-d6
	Gemfibrozil-d6 is intended for use as an internal standard for the quantification of gemfibrozil by GC- or LC-MS. Gemfibrozil is a peroxisome proliferator-activated reporter α and PPARγ agonist. In vivo, gemfibrozil reduces serum total cholesterol, triglyceride, and LDL levels in a rat model of high-cholesterol diet-induced hyperlipidemia. Gemfibrozil reduces atherosclerotic plaque area, superoxide production, and expression of the genes encoding the NF-κB subunit p65 and chemokine (C-C) motif l...
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...
T36889	Methyl alpha-eleostearate
	Methyl alpha-eleostearate (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil. This fatty acid accounts for about 60% of the total fatty acid composition of bitter gourd seed oil and about 70% in tung oil. α-ESA is metabolized and converted to conjugated linoleic acid (9Z,11E-CLA) in rats. It has shown potential as a tumor growth suppressor. In colon cancer Caco-2 cells, α-ESA induced apoptosis through up-regulation of GADD45, p53, and PPARγ. In DLD-1 cells supple...
T36698	9(Z),11(E),13(E)-Octadecatrienoic Acid
	9(Z),11(E),13(E)-Octadecatrienoic Acid (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil. This fatty acid accounts for about 60% of the total fatty acid composition of bitter gourd seed oil and about 70% in tung oil. α-ESA is metabolized and converted to conjugated linoleic acid (9Z,11E-CLA) in rats. It has shown potential as a tumor growth suppressor. In colon cancer Caco-2 cells, α-ESA induced apoptosis through up-regulation of GADD45, p53, and PPARγ. In DLD-1...
T36888	9(Z),11(E),13(E)-Octadecatrienoic Acid ethyl ester
	9(Z),11(E),13(E)-Octadecatrienoic Acid ethyl ester (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil. This fatty acid accounts for about 60% of the total fatty acid composition of bitter gourd seed oil and about 70% in tung oil. α-ESA is metabolized and converted to conjugated linoleic acid (9Z,11E-CLA) in rats. It has shown potential as a tumor growth suppressor. In colon cancer Caco-2 cells, α-ESA induced apoptosis through up-regulation of GADD45, p53, and PPA...
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...
T35468	(±)19(20)-EDP Ethanolamide
	(±)19(20)-EDP ethanolamide is an ω-3 endocannabinoid epoxide and cannabinoid (CB) receptor agonist (EC50s = 108 and 280 nM for CB1 and CB2, respectively). It is produced through direct epoxygenation of docosahexaenoyl ethanolamide by cytochrome P450 (CYP) epoxygenases. (±)19(20)-EDP ethanolamide (25 μM) reduces the viability of 143B metastatic osteosarcoma cells. It decreases the production of IL-6 and increases the production of IL-10 when used at concentrations ranging from 2.5 to 10 μM in BV-...
T65598	Cefminox sodium
	Cefminox (Sodium) is a new cephamycin antibiotic possessing a D-amino acid moiety derived from D-cysteine at the C-7B side chain. Cefminox is active against a wide range of bacteria, especially Gram-negative and anaerobic bacteria. Cefminox shows excellent in vivo efficacy (ED50) which is higher than would be expected from its in vitro activity (MIC). Moreover, cefminox possesses more potent activity in suppression of bacterial regrowth than other cephems[1]. Cefminox (Sodium) was the most activ...

化合物

Cat.No: T79678

Target: PPAR

Cat.No: T8763

Synonym: PTGR2-IN-22

Target: Others

Cat.No: T28501

Synonym: NNC61-0029,NN-622,(-)-DRF-2725,NNC-61-0029,NN 622,NNC 61-0029

Target: PPAR

Cat.No: T21587

Synonym: Pargluva,BMS-298585

Target: PPAR

Cat.No: T8732

Target: Others, Mitochondrial Metabolism

PPARγ agonist 2

Cat.No: T61743

Pioglitazone potassium

Cat.No: T61836

Leriglitazone hydrochloride

Cat.No: T73842

N-desmethyl Rosiglitazone

Cat.No: T35717

Rosiglitazone potassium

Cat.No: T61848

17-oxo-7(Z),10(Z),13(Z),15(E),19(Z)-Docosapentaenoic Acid

Cat.No: T37634

Cat.No: T71306

MBX-8025 (sodium salt)

Cat.No: T35799

Methyl alpha-eleostearate

Cat.No: T36889

9(Z),11(E),13(E)-Octadecatrienoic Acid

Cat.No: T36698

9(Z),11(E),13(E)-Octadecatrienoic Acid ethyl ester

Cat.No: T36888

Cat.No: T35816

(±)19(20)-EDP Ethanolamide

Cat.No: T35468

Cefminox sodium

Cat.No: T65598

Cat. No.	Product Name	Target	Signaling Pathways
TN1475	Caulophyllogenin Segetalic acid	IL Receptor; TNF; PPAR; Immunology/Inflammation related	Apoptosis; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism
	Caulophyllogenin 是一种部分 PPARγ 激动剂 (EC50 = 12.6 μM)，来源于 Kalopanax pictus (五加科) 的茎皮。 Caulophyllogenin 抑制促炎细胞因子分泌，可用于预防和治疗炎症性疾病、2 型糖尿病、肥胖和代谢综合征的研究。
TMA0127	Ficusin A	transporter; PPAR	DNA Damage/DNA Repair; Metabolism
	Ficusin has antioxidant, antilipidemic and antidiabetic effects, it can lower the levels of fasting blood glucose, plasma insulin, body weight gain in HFD-STZ induced diabetic rats, and can significantly enhance the PPARγ expression and improve the transl

天然产物

Caulophyllogenin

Cat.No: TN1475

Synonym: Segetalic acid

Target: IL Receptor, TNF, PPAR, Immunology/Inflammation related

Cat.No: TMA0127

Target: transporter, PPAR

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