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Search Results for " peroxisome proliferator-activated receptor γ "
Targets Recommended: PPAR

23

抑制剂 & 化合物

7

天然产物

1

重组蛋白

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Cat. No. Product Name Target Signaling Pathways
T15440 GSK376501A

PPAR DNA Damage/DNA Repair; Metabolism
GSK376501A 是一种具有选择性和有效性的的过氧化物酶体增殖物激活受体 γ (PPARγ) 调节剂,可用于研究 2 型糖尿病。
T16022 Arhalofenate

JNJ 39659100,芳卤芬酯,4-氯-ALPHA-[3-(三氟甲基)苯氧基]苯乙酸 2-(乙酰基氨基)乙酯,MBX 102

PPAR DNA Damage/DNA Repair; Metabolism
Arhalofenate (JNJ 39659100) 是一种选择性的(PPAR)-γ部分激动剂,用于研究 2 型糖尿病。
T28589 Ro 41-5253

Ro-41-5253,Ro 415253

Apoptosis; Retinoid Receptor Apoptosis; Metabolism
Ro 41-5253 是一种具有口服活性的 RARα 拮抗剂,是过氧化物酶体增殖物激活受体 (PPAR)-γ 的配体和部分激动剂,具有抗肿瘤活性,抑制 MCF-7 和 ZR-75.1 雌激素受体阳性乳腺癌细胞的增殖并诱导细胞凋亡。
T8780 AMG131

INT-131,AMG-131,CHS 131

PPAR DNA Damage/DNA Repair; Metabolism
AMG131 (CHS 131) 是一种新型非噻唑烷二酮(TZD) 选择性过氧化物酶体增殖物激活受体 (PPAR) γ 调节剂,可用于治疗 2 型糖尿病。
T69146 Suksdorfin

PPAR DNA Damage/DNA Repair; Metabolism
Suksdorfin 具有降血糖作用,可促进脂肪细胞分化并增强脂联素的产生,可激活过氧化物酶体增殖物激活受体 γ (PPARγ),可促进脂肪细胞对胰岛素依赖性葡萄糖的摄取,可用于肥胖相关研究。
T28354 Peliglitazar

BMS-426707-1,BMS 42670701,BMS 426707-01

Peliglitazar is a activator of α/γ peroxisome proliferator-activated receptor.
T68245 PA-082

PA-082 is a Novel partial agonist of peroxisome proliferator-activated receptor-γ (PPARγ), recruiting PPARγ-coactivator-1α, preventing triglyceride accumulation, and potentiating insulin signaling in vitro.
T33415 MK 0767

MK0767,MK-0767

MK 0767 is a dual peroxisome proliferator-activated receptor (PPAR) α/γ agonist that has been investigated as a potential treatment for type 2 diabetes and dyslipidemia.
T37579 GW 1929 hydrochloride

Highly selective orally active peroxisome proliferator-activated receptor (PPAR)γ agonist (pEC50 values are 8.05, < 4 and < 4 for human PPARγ, PPARα and PPARδ receptors respectively). Decreases glucose, fatty acid and triglyceride levels following oral administration in vivo. Brown et al (1999) A novel N-aryl tyrosine activator of peroxisome proliferator-activated receptor-γ reverses the diabetic phenotype of the Zucker diabetic fatty rat. Diabetes 48 1415 PMID:10389847 |Nugent et al (2001) Pote...
T68000 MK 0533

Mk-0533是一种选择性过氧化物酶体增殖激活受体γ调节剂,用于治疗2型糖尿病。
T73519 FX-909

FX-909 是一种共价过氧化物酶体增殖体激活受体 γ (PPARG) 逆激动剂。FX-909 可用于肿瘤的研究。
T28542 Rivoglitazone HCl

CI-1037,CI1037,CS011,CS-011,CI 1037

Rivoglitazone, also known as CI-1037; CS-011; DE-101; R-119702; Rivo, is a peroxisome proliferator-activated receptor γ agonist (PARPγ agonist) potentially for the treatment of type 2 diabetes. Rivoglitazone has been shown, through small clinical studies,
T37827 CAY10506

CAY10506

Anti-diabetic drugs of the thiazolidinedione (TZD) structural class as well as α-lipoic acid activate peroxisome proliferator-activated receptor γ (PPARγ), a nuclear transcription factor that controls glucose metabolism and lipid homeostasis. CAY10506 is a hybrid lipoic acid-TZD derivative that transactivates human PPARγ with an EC50 value of 10 μM.
T62576 Darglitazone Sodium

Darglitazone Sodium 是一种噻唑烷二酮,是一种选择性的、口服具有活力的 PPAR-γ (过氧化物酶体增殖物激活受体)激动剂。Darglitazone Sodium 可以有效控制血糖和脂质代谢,能够用于研究 II 型糖尿病。
T71284 Glimepiride urethane

Glimepiride urethane is a third generation sulfonylurea compound, which increases the release of insulin from pancreatic beta cells. In addition, glimepiride increases the activity of intracellular insulin receptors. Glimepiride increases osteoblast proliferation and differentiation, which is thought to be related to its ability to activate the PI3K and Akt pathway. Furthermore, Glimepiride enhances intrinsic peroxisome proliferator-activated receptor γ activity. Glimepiride also increases prote...
T13483 RP 54275

2-Octadecyl-1H-indole-5-carboxylic acid

Others Others
RP 54275 是一种天然存在的脂肪酸衍生物,一种新的降胆固醇化合物。它可以激活过氧化物酶体增殖物激活受体γ(PPARγ)途径,该途径参与脂质代谢、炎症和细胞分化的调节。
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...
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。
T37787 10-Nitrolinoleic acid

10-Nitrolinoleate is the product of nitration of linoleate by NO-derived reactive species. Other nitrolinoleates detected in human plasma and urine include 9-, 12-, and 13-nitrolinoleate. Nitrolinoleates activate peroxisome proliferator-activated receptor γ (PPARγ; Ki = 133 nM), inducing CD36 expression in macrophages, adipocyte differentiation, and glucose uptake. Nitrolinoleates can also be metabolized by smooth muscle cells to produce nitrite derivatives which in turn form NO, leading to incr...
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...
T35813 CAY10592

Peroxisome proliferator-activated receptors (PPARs) α, δ, γ are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism. Pharmacologies of PPARδ receptor agonists, though relatively obscure, have recently been reported to elevate high-density lipoprotein (HDL) cholesterol and lower plasma triglyceride (TG) levels in obese insulin resistant rhesus monkeys. CAY10592 is a full PPARδ agonist (EC50 = 30 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...

化合物

GSK376501A
Cat.No: T15440
Synonym:
Target: PPAR
Arhalofenate
Cat.No: T16022
Synonym: JNJ 39659100,芳卤芬酯,4-氯-ALPHA-[3-(三氟甲基)苯氧基]苯乙酸 2-(乙酰基氨基)乙酯,MBX 102
Target: PPAR
Ro 41-5253
Cat.No: T28589
Synonym: Ro-41-5253,Ro 415253
Target: Apoptosis, Retinoid Receptor
AMG131
Cat.No: T8780
Synonym: INT-131,AMG-131,CHS 131
Target: PPAR
Suksdorfin
Cat.No: T69146
Synonym:
Target: PPAR
Peliglitazar
Cat.No: T28354
Synonym: BMS-426707-1,BMS 42670701,BMS 426707-01
Target:
PA-082
Cat.No: T68245
Synonym:
Target:
MK 0767
Cat.No: T33415
Synonym: MK0767,MK-0767
Target:
GW 1929 hydrochloride
Cat.No: T37579
Synonym:
Target:
MK 0533
Cat.No: T68000
Synonym:
Target:
FX-909
Cat.No: T73519
Synonym:
Target:
Rivoglitazone HCl
Cat.No: T28542
Synonym: CI-1037,CI1037,CS011,CS-011,CI 1037
Target:
CAY10506
Cat.No: T37827
Synonym: CAY10506
Target:
Darglitazone Sodium
Cat.No: T62576
Synonym:
Target:
Glimepiride urethane
Cat.No: T71284
Synonym:
Target:
RP 54275
Cat.No: T13483
Synonym: 2-Octadecyl-1H-indole-5-carboxylic acid
Target: Others
SR1903 TFA
Cat.No: T69671
Synonym:
Target:
XY-4
Cat.No: T83882
Synonym:
Target:
10-Nitrolinoleic acid
Cat.No: T37787
Synonym:
Target:
1-Arachidoyl Lysophosphatidic Acid sodium
Cat.No: T83879
Synonym: 1-Arachidoyl LPA,LPA(20:0),1-Eicosanoyl-Lysophosphatidic Acid
Target:
SR 1903
Cat.No: T35638
Synonym:
Target:
CAY10592
Cat.No: T35813
Synonym:
Target:
MD001
Cat.No: T35800
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T1633 β-Carotene

beta-胡萝卜素,Carotaben,Beta-Carotene,Provitamin A,β-胡萝卜素

Apoptosis; ROS; Endogenous Metabolite Apoptosis; Immunology/Inflammation; Metabolism
β-Carotene (Provitamin A) 是一种天然存在的视黄醇(维生素 A)前体。它是一种 ROS 调节剂,具有抗氧化和抗炎活性。它可作为抗氧化剂或者促氧化剂,可诱导乳腺癌细胞凋亡,具有抗癌活性。
T4S0800 Demethyleneberberine

P450; NOS; NF-κB; HIF; AMPK Angiogenesis; Chromatin/Epigenetic; Immunology/Inflammation; Metabolism; NF-κB; PI3K/Akt/mTOR signaling
Demethyleneberberine 是从黄连中提取的一种天然产物,是线粒体靶向抗氧化剂。它也可作为AMPK 激活剂,用于非酒精性脂肪性肝病的研究。它通过抑制NF-κB 通路和调节 Th 细胞的平衡来减轻小鼠结肠炎并抑制炎症反应。
T2915 Bardoxolone

RTA 401,齐墩果烷三萜化合物,CDDO

Others; Nrf2 Immunology/Inflammation; Others
Bardoxolone (CDDO) 是新型核调节因子激活剂。
TN2601 12-O-Methylcarnosic acid

Reductase Endocrinology/Hormones; Metabolism
12-O-Methylcarnosic acid 是分离自小叶丹参的丙酮提取物的一种二萜肉桂酸,可抑制 5α-还原酶 (5α-reductase) 活性,IC50为 61.7 μM。它抑制 LNCaP 细胞的增殖。它具有抗微生物活性、抗氧化和抗癌活性。
TN4860 Pueroside B

COX; PPAR DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; Neuroscience
Pueroside B may can treat coronary heart disease, it can interact with two or more targets[peroxisome proliferator activated receptor γ (PPAR-γ), angiotensin-converting enzyme (ACE), hydroxymethylglutaryl coenzyme A receptor (HMGR), cyclooxygenase-2 (COX2
T75611 Tibesaikosaponin V

Tibesaikosaponin V 是一种三萜双糖苷,可从北柴胡 (Bupleurum chinense DC) 的根的甲醇提取物中分离得到。Tibesaikosaponin V (TKV) 是一种三萜双糖苷,可从 Bupleurum chinense DC 根的甲醇提取物中分离得到。Tibesaikosaponin V 抑制脂质积累和甘油三酯含量的发生,对脂肪细胞没有细胞毒性。Tibesaikosaponin V 抑制核转录因子的 mRNA 表达,例如过氧化物酶体增殖物激活受体 γ (PPARγ) 和 CCAAT/增强子结合蛋白 α (C/EBPα)。Tibesaikosaponin V 抑制 3T3-L1 前脂肪细胞分化。Tibesaikosaponin V 可用于肥胖及其相关代谢紊乱的研究。
T83915 Norbixin hydrate

Norbixin是一种在B. orellana中发现的类胡萝卜素,具有多样的生物活性。在无细胞测试中,它与过氧化物酶体增殖物激活受体γ (PPARγ)结合(Ki = 1.15 µM)。在心脑血管代谢综合征大鼠模型中,Norbixin (47.7 mg/kg) 能够减轻高血糖、高胰岛素血症和胰岛素抗性,降低血清脂质水平及心脏中硫代巴比妥酸反应性物质(TBARS)和谷胱甘肽(GSH)的水平。在胆固醇诱导的动脉粥样硬化兔模型中,它降低氧化型LDL和主动脉蛋白氧化水平,并减少动脉粥样硬化面积。Norbixin(每天0.1和1 mg/kg)减少汞诱导的大鼠肝细胞和白细胞DNA损伤。此外,它还能预防与年龄相关的黄斑变性(AMD)Abca4-/- Rdh8-/-小鼠模型中的光感受器退化。

天然产物

β-Carotene
Cat.No: T1633
Synonym: beta-胡萝卜素,Carotaben,Beta-Carotene,Provitamin A,β-胡萝卜素
Target: Apoptosis, ROS, Endogenous Metabolite
Demethyleneberberine
Cat.No: T4S0800
Synonym:
Target: P450, NOS, NF-κB, HIF, AMPK
Bardoxolone
Cat.No: T2915
Synonym: RTA 401,齐墩果烷三萜化合物,CDDO
Target: Others, Nrf2
12-O-Methylcarnosic acid
Cat.No: TN2601
Synonym:
Target: Reductase
Pueroside B
Cat.No: TN4860
Synonym:
Target: COX, PPAR
Tibesaikosaponin V
Cat.No: T75611
Synonym:
Target:
Norbixin hydrate
Cat.No: T83915
Synonym:
Target:
Cat. No. Product Name Species Expression System
TMPY-02575 PPAR gamma/PPARG Protein, Human, Recombinant (His & GST)

CIMT1,PPARγ,GLM1,PPARgamma,PPARG1,PPARG2,NR1C3,...

Human Baculovirus Insect Cells
Peroxisome proliferator-activated receptor gamma (PPARG), a nuclear hormone receptor, plays a critical role in the lipid and glucose homeostasis, adipocyte differentiation, as well as intracellular insulin-signaling events. The peroxisome proliferator-activated receptor gamma (PPARgamma) regulates osteoblast and osteoclast differentiation, and is the molecular target of thiazolidinediones (TZDs), insulin sensitizers that enhance glucose utilization and adipocyte differentiation. Peroxisome proli...

重组蛋白

PPAR gamma/PPARG Protein, Human, Recombinant (His & GST)
Cat.No: TMPY-02575
Species: Human
Expression System: Baculovirus Insect Cells
TargetMol Loading
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