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13

抑制剂 & 化合物

8

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8505	SC-236 4-(5-(4-氯苯基)-3-(三氟甲基)-1H-,Sc 236	Apoptosis; COX; PPAR	Apoptosis; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; Neuroscience
	SC-236 (Sc 236) 是一种具有口服活性的COX-2特异性抑制剂和PPARγ激动剂。它可通过 c-Jun 氨基端抑制激活蛋白-1活性，在小鼠模型中通过抑制 ERK 的磷酸化发挥抗炎作用。
T4408	Elafibranor GFT505	PPAR	DNA Damage/DNA Repair; Metabolism
	Elafibranor (GFT505) 是过氧化物酶体增殖物激活受体-α (PPAR-α) 和过氧化物酶体增殖物激活受体-δ (PPAR-δ) 的激动剂，EC50 值分别为 45 和 175 nM。
T15575	Indeglitazar PPM 204	PPAR	DNA Damage/DNA Repair; Metabolism
	Indeglitazar (PPM 204) 是 PPAR 的泛激动剂，包括亚型 alpha (α)、delta (δ) 和 gamma (γ)。
T8486	GW6471 GW 6471	PPAR	DNA Damage/DNA Repair; Metabolism
	GW6471 是 PPARα 的拮抗剂，IC50 为 0.24 μM。它增强 PPAR α 配体结合结构域与共抑制蛋白 SMRT 和 NCoR 的结合亲和力。
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。
T17044	Tesaglitazar	PPAR	DNA Damage/DNA Repair; Metabolism
	Tesaglitazar 是一种有效且具有选择性的过氧化物 PPAR α / γ受体双重激动剂，对 PPARγ的亲和力比 PPARα更有效，对大鼠PPARα和人PPARα的EC50分别为13.4 μM 和3.6 μM,对大鼠PPARγ和人类 PPARγ的EC50都是0.2 μM。Tesaglitazar 诱导大鼠皮下组织间质间充质细胞DNA 合成和纤维肉瘤形成。
T1415	Gemfibrozil 吉非罗齐,CI-719,Jezil,Decrelip,Lopid	P450; Adrenergic Receptor; PPAR	DNA Damage/DNA Repair; GPCR/G Protein; Metabolism; Neuroscience
	Gemfibrozil (CI-719) 是一种PPAR-α激活剂，可作为降脂药。它也是P450非选择性抑制剂，对 CYP2C9、2C19、2C8 和 1A2 的Ki 值分别为 5.8、24、69 和 82 μM。
T10506	PPAR agonist 1	PPAR	DNA Damage/DNA Repair; Metabolism
	PPAR agonist 1 is an agonist of PPAR α/γ, used for reducing blood glucose, lipid levels, reducing body weight, and lowering cholesterol.
T12278	NXT629	Estrogen/progestogen Receptor	Endocrinology/Hormones
	NXT629 is a selective and competitive antagonist of PPAR-α(human PPARα with an IC50 of 77 nM).
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.
T60432	NAAA-IN-3
	NAAA-IN-3 (Compound 17a) 是一种有效的、选择性的 NAAA 抑制剂，IC50为 50 nM。NAAA 是一种半胱氨酸酰胺酶，它优先水解内源性生物脂棕榈酰乙醇酰胺 (PEA) 和油酰乙醇酰胺 (OEA)。PEA 是核过氧化物酶体增殖物激活受体-α (PPAR-α) 的内源性激动剂，PPAR-α 是炎症和疼痛的关键调节因子。 NAAA-IN-3 的潜在作用是作为炎症和疼痛的治疗剂。
T79454	Anti-NASH agent 1	PPAR	DNA Damage/DNA Repair; Metabolism
	Anti-NASH agent 1 (compound 3d)，Elafibranor衍生物，高效PPAR-α/δ激动剂，针对非酒精性脂肪性肝炎（NASH）。以3-10 mg/kg剂量，连续4周处理，能显著改善蛋氨酸胆碱缺乏（MCD）诱导的NASH小鼠高脂血症、肝脏脂肪变性及炎症状况，展现出低肝毒性和良好肝脏保护效能。
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) ...

化合物

Cat.No: T8505

Synonym: 4-(5-(4-氯苯基)-3-(三氟甲基)-1H-,Sc 236

Target: Apoptosis, COX, PPAR

Cat.No: T4408

Synonym: GFT505

Target: PPAR

Cat.No: T15575

Synonym: PPM 204

Target: PPAR

Cat.No: T8486

Synonym: GW 6471

Target: PPAR

Cat.No: T21587

Synonym: Pargluva,BMS-298585

Target: PPAR

Cat.No: T17044

Target: PPAR

Cat.No: T1415

Synonym: 吉非罗齐,CI-719,Jezil,Decrelip,Lopid

Target: P450, Adrenergic Receptor, PPAR

PPAR agonist 1

Cat.No: T10506

Target: PPAR

Cat.No: T12278

Target: Estrogen/progestogen Receptor

Cat.No: T33415

Synonym: MK0767,MK-0767

Cat.No: T60432

Anti-NASH agent 1

Cat.No: T79454

Target: PPAR

Cat.No: T35813

Cat. No.	Product Name	Target	Signaling Pathways
T2824	Pedunculoside	Others; Fatty Acid Synthase	Metabolism; Others
	Pedunculoside 是从 Ilex rotunda Thunb 中提取的，通过对脂质形成和脂肪酸 β-氧化的调节而发挥降脂作用。
TN1990	Norathyriol 芒果苷元	Akt; DNA/RNA Synthesis; AMPK; PPAR	Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; Metabolism; PI3K/Akt/mTOR signaling
	Norathyriol 是来自芒果的芒果苷代谢物，具有抗氧化、抗癌、抗菌和抗炎活性。它以非竞争性方式抑制 α-葡萄糖苷酶，IC50为 3.12 μM。它还抑制PPARα、PPARβ和PPARγ，IC50分别为 92.8、102.4 和 153.5 µM。
T12296	Oleoylethanolamide 油酰单乙醇胺,N-Oleoylethanolamide,Oleamide MEA,Oleic acid monoethanolamide	Endogenous Metabolite; PPAR	DNA Damage/DNA Repair; Metabolism
	Oleoylethanolamide (N-Oleoylethanolamide) 是一种PPAR-α 的高亲和力内源性激动剂，可用于肥胖和动脉硬化的相关研究。
T2932	Ginsenoside Rh1 Sanchinoside B2,人参皂苷 Rh1,人参皂苷Rh1,Prosapogenin A2,20(S)-Ginsenoside Rh1,Sanchinoside Rh1	IL Receptor; TNF; Endogenous Metabolite; PPAR; Interleukin	Apoptosis; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism
	Ginsenoside Rh1 (Sanchinoside B2) 是人参的一种主要成分，具有抗炎作用，抑制PPAR-γ，TNF-α，IL-6和IL-1β的表达。
T2985	Gypenoside XLIX 绞股蓝皂苷 XLIX,绞股蓝皂苷XLIX	PPAR	DNA Damage/DNA Repair; Metabolism
	Gypenoside XLIX 是一种达玛烷型糖苷，是绞股蓝的主要成分。它是选择性过氧化物酶体增殖物激活受体 (PPAR)-α激活剂，可抑制细胞因子诱导的血管细胞粘附分子-1 (VCAM-1) 在人体内皮细胞中过度活跃和表达。
T2S0633	Raspberry ketone Oxyphenalon,Rasketone,Aloenin,4-(4-Hydroxyphenyl)-2-butanone,p-Hydroxybenzyl acetone,Frambinone,覆盆子酮	PPAR	DNA Damage/DNA Repair; Metabolism
	Raspberry ketone (p-Hydroxybenzyl acetone) 是覆盆子中主要的芳香族天然产物，主要用作化妆品的香料和食品增味剂，也可作 PPAR-α激动剂。
TN3219	7,8-Didehydrocimigenol	ERK; IκB/IKK; TNF; NF-κB; Akt; PPAR	Apoptosis; Cytoskeletal Signaling; DNA Damage/DNA Repair; MAPK; Metabolism; NF-κB; PI3K/Akt/mTOR signaling
	7,8-Didehydrocimigenol can be used for the treatment of cardiovascular disorders such as atherosclerosis. It upregulates PPAR-γ in EC inhibits NF-kB activity of TNF-α-activated EC which leads to selective inhibition of VCAM-1 expression.
TN3655	Cimiside E	ERK; TNF; ROS; Akt; PI3K; PKC; PPAR	Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; Immunology/Inflammation; MAPK; Metabolism; PI3K/Akt/mTOR signaling
	Cimiside E has anti-inflammatory activity, it selectively inhibits TNF-α-induced expression of VCAM-1 at least by upregulation of PPAR-γ, and signals for ERK1/2, PI3K, and PKC are involved in this effect.Cimiside E may be an effective chemopreventive agen

天然产物

Cat.No: T2824

Target: Others, Fatty Acid Synthase

Cat.No: TN1990

Synonym: 芒果苷元

Target: Akt, DNA/RNA Synthesis, AMPK, PPAR

Oleoylethanolamide

Cat.No: T12296

Synonym: 油酰单乙醇胺,N-Oleoylethanolamide,Oleamide MEA,Oleic acid monoethanolamide

Target: Endogenous Metabolite, PPAR

Ginsenoside Rh1

Cat.No: T2932

Synonym: Sanchinoside B2,人参皂苷 Rh1,人参皂苷Rh1,Prosapogenin A2,20(S)-Ginsenoside Rh1,Sanchinoside Rh1

Target: IL Receptor, TNF, Endogenous Metabolite, PPAR, Interleukin

Gypenoside XLIX

Cat.No: T2985

Synonym: 绞股蓝皂苷 XLIX,绞股蓝皂苷XLIX

Target: PPAR

Raspberry ketone

Cat.No: T2S0633

Synonym: Oxyphenalon,Rasketone,Aloenin,4-(4-Hydroxyphenyl)-2-butanone,p-Hydroxybenzyl acetone,Frambinone,覆盆子酮

Target: PPAR

7,8-Didehydrocimigenol

Cat.No: TN3219

Target: ERK, IκB/IKK, TNF, NF-κB, Akt, PPAR

Cat.No: TN3655

Target: ERK, TNF, ROS, Akt, PI3K, PKC, PPAR

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