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Search Results for " pparγ agonist 1 "

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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T63514	PPARγ agonist 1
	PPARγ agonist 1 是 PPARγ 的有效激动剂，能够高效的激活 hPPARγ ，并不引起完全激动，进而能够避免不良反应。PPARγ agonist 1 对代谢紊乱相关心血管疾病表现出研究潜力。
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。
T62266	PPARα agonist 1
	PPARα agonist 1 是一种完整的、有效的 PPARα激动剂。
T60535	PPARα/γ agonist 1
	PPARα/γ agonist 1 是一种有效的双重 PPARα/γ部分激动剂，是用于研究血脂异常和糖尿病的有前途的化合物。PPARα/γ agonist 1 对 PPARα 和 PPARγ 的EC50值分别为 28 nM 和 69 nM。
T6524	GW0742 GW610742,[4-[[[2-[3-氟-4-(三氟甲基)苯基]-4-甲基-5-噻唑基]甲基]硫代]-2-甲基苯氧基]乙酸	PPAR	DNA Damage/DNA Repair; Metabolism
	GW0742 是一种有效且特异性的 PPARδ 激动剂，对人 PPARδ、PPARα 和 PPARγ 的 EC50值分别为 1、1.1 和 2 μM。
T60184	TUG-499	GPR; PPAR	DNA Damage/DNA Repair; Endocrinology/Hormones; GPCR/G Protein; Metabolism
	TUG-499 是一种选择性游离脂肪酸受体 1 (FFAR1 或 GPR40)激动剂（EC50 ： 7.39）。TUG-499对 FFAR1 或 GPR40的亲和力超过相关受体 FFA2、FFA3 和核受体 PPARγ，以及其他不同的受体、离子通道和转运蛋白。TUG-499 可用于研究 2 型糖尿病。
T61731	PPARγ agonist 4
	PPARγ agonist 4 (Compound 18b), a potent and selective PPARγ agonist, demonstrates antitumor efficacy only when used in conjunction with Imatinib. Notably, PPARγ agonist 4 does not exhibit cytotoxic effects on either non-resistant or resistant cells [1].
T61417	PPARγ agonist 7
	PPARγ agonist 7 (Compound 3a) is a highly potent and selective agonist of the peroxisome proliferator-activated receptor gamma (PPARγ). It specifically stimulates adiponectin production in human bone marrow mesenchymal stem cells (hBM-MSCs), making it an innovative full agonist of PPARγ with an EC 50 value of 4.34 μM [1].
T61465	PPARγ agonist 3
	PPARγ agonist 3, also known as Compound 18a, is a potent and selective agonist of PPARγ. This compound does not exhibit cytotoxicity towards both non-resistant and resistant cells. Notably, PPARγ agonist 3 demonstrates antitumor efficacy exclusively when co-administered with Imatinib [1].
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].
T22154	SR 2595
	SR2595 是一种核受体 PPARγ的反向激动剂，其 IC50为 30 nM。
T37026	Mesalamine impurity P
	Mesalamine impurity P is an impurity of Mesalamine . 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB[1]. [1]. Kyle Dammann, et al.PAK1 modulates a PPARγ/NF-κB cascade in intestinal inflammation.Biochim Biophys Acta. 2015 Oct;1853(10 Pt A):2349-60.
T75009	PPARγ/GR modulator 1
	PPARγ/GR modulator 1 是一种口服活性的 PPARγ和糖皮质激素受体 (GR) 的双动激动剂，Ki 值分别为 3.3 和 33.6 μM。PPARγ/GR modulator 1 可用于研究代谢疾病，例如糖尿病。
T79182	PPARγ agonist 8	PPAR	DNA Damage/DNA Repair; Metabolism
	PPARγ agonist8，作为PPARγ的激动剂，能够诱导过氧化物酶体增殖反应元件(PPRE)-萤光素酶活性，其EC50值为0.2 μM。
T83882	XY-4
	XY-4是1-棕榈酰基溶血磷脂酸(1-palmitoyl LPA094)的衍生物，同时也是过氧化物酶体增殖物激活受体γ(PPARγ)的激动剂。当浓度为5 µM时，能在表达过氧化物酶体增殖物反应元件(PPRE)的RAW 264.7巨噬细胞中诱导报告基因的表达。XY-4不作为溶血磷脂酸受体1(LPA1)、LPA2或LPA3的激动剂。在1 µM的浓度下，它能在体外诱导血小板聚集。XY-4诱导大鼠颈动脉内膜新生。
T21812	LT175
	LT175 是一种双重PPARα/γ配体，具有强大的胰岛素增敏作用和降低的脂肪生成特性。LT175是口服有效 PPARγ 的部分激动剂 (hPPARα:EC50=0.22 μM; mPPARα:EC50=0.26 μM; hPPARγ:EC50=0.48 μM)。LT175 与 PPARγ 相互作用并影响辅助调节因子环 AMP 反应元件结合蛋白结合蛋白和核辅助抑制因子 1 (NCoR1) 的募集。LT175 在“二苯口袋”的疏水区域中与 PPARγ 相互作用。
T64011	GSK1820795A
	GSK1820795A 作为替米沙坦类似物是hGPR132a 的选择性拮抗剂。GSK1820795A 阻断了 N-acylamides 对表达hGPR132a 的酵母细胞的活化。GSK1820795A 也是血管紧张素 II 拮抗剂和部分PPARγ激动剂 (compound 38) 。
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。
T35800	MD001
	MD001 is a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ.1 It binds to PPARα and PPARγ (Kds = 9.55 and 0.14 μM, respectively) but does not bind to PPARβ/δ at concentrations up to 500 μM. It increases transcriptional activity of PPARα and PPARγ in a cell-based luciferase reporter assay when used at a concentration of 10 μM. MD001 (10 μM) increases expression of PPARα, PPARγ, and retinoid X receptor (RXR), as well as PPARα and PPARγ target genes, in HepG2 cells. It...
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].
T37414	CAY10771
	CAY10771 is a dual agonist of farnesoid X receptor (FXR) and peroxisome proliferator-activated receptor δ (PPARδ).1It activates FXR and PPARδ in reporter assays using HEK293T cells (EC50s = 0.94 and 1.5 μM, respectively) and is selective for these receptors over retinoic acid receptor α (RARα), retinoid X receptor α (RXRα), PPARα, PPARγ, and liver X receptor α (LXRα) at 10 μM. 1.Schierle, S., Neumann, S., Heitel, P., et al.Design and structural optimization of dual FXR/PPARδ activatorsJ. Med. Ch...
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...
T83879	1-Arachidoyl Lysophosphatidic Acid sodium 1-Arachidoyl LPA,LPA(20:0),1-Eicosanoyl-Lysophosphatidic Acid
	1-花生四烯酰基溶血磷脂酸（1-arachidoyl LPA）是溶血磷脂酸受体1（LPA1）的激动剂，并且是一种含有花生四烯酸的甘油磷脂，花生四烯酸位于sn-1位置。它能在主要表达LPA1而非LPA2-LPA6的人类肺成纤维细胞中诱导钙离子动员（EC50 = 3.6 µM）。在无细胞试验中，1-Arachidoyl LPA（2.5 µM）还能结合到过氧化物酶体增殖物激活受体γ（PPARγ）的配体结合域。人类尿液中也发现了该化合物。
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...
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...
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...
T83765	Dendrogenin A DDA
	Dendrogenin A (DDA) 作为一种选择性肝X受体(LXR)调节剂(SLiM)、胆固醇环氧水解酶(ChEH; Ki = 120 nM)的抑制剂及胆固醇的活性代谢产物，通过DDA合成酶将5,6α-环氧胆固醇与组胺结合形成。DDA在非癌性人乳腺上皮细胞和上皮黑色素细胞中存在，但在多种乳腺癌细胞或黑色素瘤细胞中未发现，且在分离的人乳腺肿瘤组织中仅以低水平存在。它抑制22(R)-羟基胆固醇诱导的LXRβ和LXRα激活(分别以IC50 = 76和362 nM)，但也是LXR的部分激动剂，在B16/F10小鼠黑色素瘤细胞中增加Nur77、NOR-1、LC3-I和LC3-II的蛋白水平。DDA选择性调节LXRα和LXRβ，而非孕烯X受体(PXR)、芳香烃受体(AhR)、维生素D受体(VDR)、维甲酸X受体γ(RXRγ)、维甲酸受体α(RARα)、过氧化物酶体增殖物激活受体α(PPARα)、PPARγ、糖皮质激素受体、雄激素受体、雌激素受体α(ERα)及ERβ在2.5 µM下。此外，DDA在2.5和5 µM的浓度下增加B16/F10和SK-MEL-28癌细胞中LC3-II的蛋白水平，并在2...

化合物

PPARγ agonist 1

Cat.No: T63514

PPARα/δ agonist 1

Cat.No: T62968

PPARα agonist 1

Cat.No: T62266

PPARα/γ agonist 1

Cat.No: T60535

Cat.No: T6524

Synonym: GW610742,[4-[[[2-[3-氟-4-(三氟甲基)苯基]-4-甲基-5-噻唑基]甲基]硫代]-2-甲基苯氧基]乙酸

Target: PPAR

Cat.No: T60184

Target: GPR, PPAR

PPARγ agonist 4

Cat.No: T61731

PPARγ agonist 7

Cat.No: T61417

PPARγ agonist 3

Cat.No: T61465

PPARγ agonist 2

Cat.No: T61743

Cat.No: T22154

Mesalamine impurity P

Cat.No: T37026

PPARγ/GR modulator 1

Cat.No: T75009

PPARγ agonist 8

Cat.No: T79182

Target: PPAR

Cat.No: T83882

Cat.No: T21812

Cat.No: T64011

Leriglitazone hydrochloride

Cat.No: T73842

Cat.No: T35800

Rosiglitazone potassium

Cat.No: T61848

Cat.No: T37414

MBX-8025 (sodium salt)

Cat.No: T35799

1-Arachidoyl Lysophosphatidic Acid sodium

Cat.No: T83879

Synonym: 1-Arachidoyl LPA,LPA(20:0),1-Eicosanoyl-Lysophosphatidic Acid

Cat.No: T35638

Cat.No: T35816

Cefminox sodium

Cat.No: T65598

Cat.No: T83765

Synonym: DDA

Cat. No.	Product Name	Target	Signaling Pathways
T75690	Wistin
	Wistin 可从 Caragana sinica 根部分离得到，是 PPARα和 PPARγ的激动剂。

天然产物

Cat.No: T75690

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