PPAR
PPAR(过氧化物酶体增殖剂激活受体)
The peroxisome proliferator-activated receptors (PPARs), belonging to the nuclear receptor superfamily, are a group of nuclear receptor proteins that are composed of three isoforms, including PPARγ, PPARα and PPARδ, encoded by separate genes. PPARs have a modular structure characterized by the presence of two highly conserved domains, including the DNA binding domain (DBD) of two zinc fingers and the ligand binding domain (LBD) of 13 α-helices and a small 4-stranded β-sheet. PPARs are ligand-regulated transcription factors controlling gene expression by binding to specific response elements (PPREs) within promoters, where PPARs bind as heterodimers with a retinoid X receptor and interact with cofactors upon binding leading to the increasing of rate of transcription initiation.
PPAR 相关产品(215)
- GC18147Tretinoin (Aberela)CAS: 302-79-4纯度: >99.50% / >98.00%
Tretinoin (Aberela) 是一种维生素 A 衍生的非肽类亲脂性小分子,可作为核 RA 受体 (RAR) 的配体,将其从转录抑制因子转化为激活因子 .在培养的人系膜细胞中,维甲酸 (Aberela) 以剂量和时间依赖性方式增加还原型谷胱甘肽含量和过氧化氢酶活性,从而阻止 H2O2 的细胞毒性。
- GC19242SeladelparCAS: 851528-79-5纯度: >98.00% / >98.50%
Seladelpar (MBX-8025) 是一种口服有效的(50% 作用浓度 EC50 2 nM)和特异性 PPAR-δ 激动剂。
- GC19280PemafibrateCAS: 848259-27-8
Pemafibrate (K-877) 是一种口服过氧化物酶体增殖物激活受体 (PPAR)-α 激动剂,用于治疗高脂血症,对 Gal4hPPARα 的 EC50 = 1 nM 。
- GC30462Pparδ agonist 1CAS: 1902161-12-9
Pparδagonist1是PPAR-δ的激动剂,EC50值为5.06nM,可用于研究与PPAR-δ相关的疾病,例如:线粒体疾病、肌肉疾病、血管疾病、脱髓鞘疾病和代谢疾病。
- GC31325Saroglitazar MagnesiumCAS: 1639792-20-3纯度: >98.50%
Saroglitazarmagnesium是一种新型的过氧化物酶体增殖物活化受体PPAR的激动剂,具有显著PPARα活性和中度PPARγ活性,在HepG2细胞中的EC50值分别为0.65pMand3nM。
- GC31350AstaxanthinCAS: 472-61-7纯度: >98.00%
Astaxanthin (β-Carotene-4,4'-dione, Trans-Astaxanthin), a xanthophyll carotenoid, is a nutrient with unique cell membrane actions and diverse clinical benefits with excellent safety and tolerability. Astaxanthin, a red dietary carotenoid isolated from Haematococcus pluvialis, is a modulator of PPARγ and a potent antioxidant with antiproliferative, neuroprotective and anti-inflammatory activity.
- GC31396Raspberry ketone (Frambione)CAS: 5471-51-2纯度: >99.50%
Raspberry ketone (p-Hydroxybenzyl acetone, Frambinone, Oxyphenylon, Rheosmin, Rasketone) is a natural phenolic compound that is the primary aroma compound of red raspberries. Raspberry ketone shows cardioprotective action against isoproterenol-induced myocardial infarction in rats, and the effects may be due to its PPAR-α agonistic activity.
- GC31408Indeglitazar (PPM 204)CAS: 835619-41-5纯度: >99.50%
Indeglitazar (PPM 204) (PPM 204) 是一种可口服的 PPAR 泛激动剂,适用于所有三种 PPARα, PPARδ和PPARγ;。
- GC31450Naveglitazar racemateCAS: 916085-47-7
Naveglitazarracemate是Naveglitazar的外消旋体。Naveglitazar是过氧化物酶体增殖物激活受体(PPAR)α-γ双重,γ显性激动剂,在动物模型具有降低葡萄糖潜力。
- GC31451Peliglitazar racemate (BMS 426707-01 racemate)CAS: 331744-72-0
Peliglitazar 外消旋体(BMS 426707-01 外消旋体)是 Peliglitazar 的外消旋体。
| 货号 | 产品名称 | CAS号 | 纯度 | 结构 |
|---|---|---|---|---|
| GC16944 | SR 1664 | 1338259-05-4 | - | |
An inhibitor of Cdk5-mediated PPARγ phosphorylation | ||||
| GC17135 | Ciglitazone | 74772-77-3 | - | |
A potent, selective PPARγ ligand | ||||
| GC17824 | GSK 0660 | 1014691-61-2 | >98.00% | |
GSK 0660是一种强效的PPARβ拮抗剂,IC 50 值为155nM。 | ||||
| GC18024 | GW 7647 | 265129-71-3 | >98.00% / >99.00% | |
A selective PPARα agonist | ||||
| GC18037 | Tesaglitazar | 251565-85-2 | >98.00% | |
A PPARα/γ agonist | ||||
| GC18147 | Tretinoin (Aberela) | 302-79-4 | >99.50% / >98.00% | |
Tretinoin (Aberela) 是一种维生素 A 衍生的非肽类亲脂性小分子,可作为核 RA 受体 (RAR) 的配体,将其从转录抑制因子转化为激活因子 .在培养的人系膜细胞中,维甲酸 (Aberela) 以剂量和时间依赖性方式增加还原型谷胱甘肽含量和过氧化氢酶活性,从而阻止 H2O2 的细胞毒性。 | ||||
| GC18876 | CAY10599 | 1143573-33-4 | - | |
An agonist of PPARγ | ||||
| GC19242 | Seladelpar | 851528-79-5 | >98.00% / >98.50% | |
Seladelpar (MBX-8025) 是一种口服有效的(50% 作用浓度 EC50 2 nM)和特异性 PPAR-δ 激动剂。 | ||||
| GC19280 | Pemafibrate | 848259-27-8 | - | |
Pemafibrate (K-877) 是一种口服过氧化物酶体增殖物激活受体 (PPAR)-α 激动剂,用于治疗高脂血症,对 Gal4hPPARα 的 EC50 = 1 nM 。 | ||||
| GC19450 | MA-0204 | 2095128-17-7 | >99.50% | |
MA-0204 是一种有效的、高选择性和可口服的过氧化物酶体增殖物激活受体 δ (PPARδ) 调节剂,对人类、小鼠和大鼠 PPARδ 的 EC50 分别为 0.4 nM、7.9 nM 和 10 nM。 | ||||
| GC19504 | LJ570 | 2252488-69-8 | - | |
LJ570 是一种 PPARα/PPARγ 双重激动剂,EC50 分别为 1.05 和 0.12 μM。 | ||||
| GC30379 | Saroglitazar | 495399-09-2 | >98.00% | |
A PPARα and PPARγ dual agonist | ||||
| GC30462 | Pparδ agonist 1 | 1902161-12-9 | - | |
Pparδagonist1是PPAR-δ的激动剂,EC50值为5.06nM,可用于研究与PPAR-δ相关的疾病,例如:线粒体疾病、肌肉疾病、血管疾病、脱髓鞘疾病和代谢疾病。 | ||||
| GC31325 | Saroglitazar Magnesium | 1639792-20-3 | >98.50% | |
Saroglitazarmagnesium是一种新型的过氧化物酶体增殖物活化受体PPAR的激动剂,具有显著PPARα活性和中度PPARγ活性,在HepG2细胞中的EC50值分别为0.65pMand3nM。 | ||||
| GC31350 | Astaxanthin | 472-61-7 | >98.00% | |
Astaxanthin (β-Carotene-4,4'-dione, Trans-Astaxanthin), a xanthophyll carotenoid, is a nutrient with unique cell membrane actions and diverse clinical benefits with excellent safety and tolerability. Astaxanthin, a red dietary carotenoid isolated from Haematococcus pluvialis, is a modulator of PPARγ and a potent antioxidant with antiproliferative, neuroprotective and anti-inflammatory activity. | ||||
| GC31396 | Raspberry ketone (Frambione) | 5471-51-2 | >99.50% | |
Raspberry ketone (p-Hydroxybenzyl acetone, Frambinone, Oxyphenylon, Rheosmin, Rasketone) is a natural phenolic compound that is the primary aroma compound of red raspberries. Raspberry ketone shows cardioprotective action against isoproterenol-induced myocardial infarction in rats, and the effects may be due to its PPAR-α agonistic activity. | ||||
| GC31408 | Indeglitazar (PPM 204) | 835619-41-5 | >99.50% | |
Indeglitazar (PPM 204) (PPM 204) 是一种可口服的 PPAR 泛激动剂,适用于所有三种 PPARα, PPARδ和PPARγ;。 | ||||
| GC31450 | Naveglitazar racemate | 916085-47-7 | - | |
Naveglitazarracemate是Naveglitazar的外消旋体。Naveglitazar是过氧化物酶体增殖物激活受体(PPAR)α-γ双重,γ显性激动剂,在动物模型具有降低葡萄糖潜力。 | ||||
| GC31451 | Peliglitazar racemate (BMS 426707-01 racemate) | 331744-72-0 | - | |
Peliglitazar 外消旋体(BMS 426707-01 外消旋体)是 Peliglitazar 的外消旋体。 | ||||
| GC31452 | AVE-8134 | 304025-09-0 | - | |
AVE-8134是PPARα的有效激动剂,对人体和啮齿类动物的PPARα的EC50值分别为100和3000nM。 | ||||
| GC31462 | Arhalofenate (MBX 102) | 24136-23-0 | - | |
A prodrug form of a PPARγ partial agonist | ||||
| GC31471 | GSK376501A | 1010412-80-2 | >99.00% | |
GSK376501A是一种选择性的过氧化物酶体增殖物激活受体γ(PPARγ)调节剂。可用于治疗2型糖尿病。 | ||||
| GC31497 | KD-3010 | 934760-92-6 | - | |
KD3010是一种具有口服活性的有效的选择性PPARδ激动剂。 | ||||
| GC31510 | Pparδ agonist | 942594-93-6 | - | |
PPARδagonist是PPARδ的激动剂,来自专利US20180071304,化合物实例10。 | ||||
