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Cell Metabolism

Cell Metabolism

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GW0742

Catalog No. A14958
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PPAR 激动剂

GW0742是PPARδ的选择性激动剂，EC50值为1.1 nM。了解更多

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GW1929

Catalog No. A15099
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PPAR 激动剂

GW1929是一种合成的过氧化物酶体增殖物激活受体-γ（PPARγ）激动剂，对人和人的IC50为6.2 nM和13 nM。了解更多

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Balaglitazone

Catalog No. A15013
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PPAR-γ partial 激动剂

Balaglitazone是PPAR-γ（γ）的新型局部激动剂。了解更多

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BMS-687453

Catalog No. A15836
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PPAR 激动剂

BMS-687453是一种有效的选择性过氧化物酶体增殖物激活受体（PPAR）α激动剂，对人PPARα的EC（50）为10 nM，在PPAR-GAL4反式激活试验中，选择性是对人PPARgamma的410倍。了解更多

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Aleglitazar

Catalog No. A12492
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PPAR-α/γ 激动剂

Aleglitazar是一种新型的双重PPAR-α/γ激动剂，IC50为2.8 nM/4.6 nM。了解更多

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Elafibranor

Catalog No. A15454
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PPAR 激动剂

Elafibranor是过氧化物酶体增殖物激活的受体-α和-δ的激动剂，可诱导非酒精性脂肪性肝炎消退，而不会使纤维化恶化。了解更多

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- Joost Boeckmans, .et al. Transcriptomics Reveals Discordant Lipid Metabolism Effects between In Vitro Models Exposed to Elafibranor and Liver Samples of NAFLD Patients after Bariatric Surgery, Cells, 2022, 11(5), 893 PMID: 35269515
- Tomasz Kostrzewski, .et al. Modelling human liver fibrosis in the context of non-alcoholic steatohepatitis using a microphysiological system, Commun Biol, 2021, 4: 1080 PMID: 34526653
- Joost Boeckmans, .et al. Flow cytometric quantification of neutral lipids in a human skin stem cell-derived model of NASH, MethodsX, 2020, 7: 101068 PMID: 33024711
- Joost Boeckmans, .et al. Human hepatic in vitro models reveal distinct anti-NASH potencies of PPAR agonists, Cell Biol Toxicol, 2020, Jul 1 PMID: 32613381
- Joost Boeckmans, .et al. Transcriptomics data of a human in vitro model of non-alcoholic steatohepatitis exposed to elafibranor, Data in Brief, 2019, June 3 PMID: 31294056
- Boeckmans J, .et al. Elafibranor restricts lipogenic and inflammatory responses in a human skin stem cell-derived model of NASH, Pharmacol Res, 2019, Apr 24. pii: S1043-6618(18)31850-4 PMID: 31028903
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CDDO-Im

Catalog No. A16308
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PPARγ 激动剂

CDDO-Im是一种新型的合成三萜，在体外和体内均比其母体化合物CDDO更有效。PPARγ激动剂。了解更多

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5-Aminosalicylic Acid

Catalog No. A10570
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PPARγ agonist

5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB. 了解更多

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Pioglitazone hydrochloride

Catalog No. A16670
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PPARγ agonist

Pioglitazone hydrochloride is a potent and selective PPARγ agonist with EC50s of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. 了解更多

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Fonadelpar

Catalog No. A20848
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PPARδ agonist

Fonadelpar is a PPARδ agonist, used in the research of neuroparalytic keratopathy. 了解更多

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Tesaglitazar

Catalog No. A20891
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PPAR alpha/gamma agonist

Tesaglitazar is a dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist that is more potent on PPARγ than on PPARα, with EC50s of 13.4 μM and 3.6 μM for rat PPARα and human PPARα, respectively. 了解更多

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Arhalofenate

Catalog No. A21135
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PPARγ agonist

Arhalofenate (MBX 102) is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes. 了解更多

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Indeglitazar

Catalog No. A21148
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PPAR agonist

Indeglitazar is an orally available peroxisome proliferator-activated receptor (PPAR) pan-agonist for all three PPAR subtypes alpha (α), delta (δ) and gamma (γ). 了解更多

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Inolitazone

Catalog No. A21180
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PPARγ agonist

Inolitazone a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC50 of 0.8 nM for growth inhibition. 了解更多

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Rosiglitazone maleate

Catalog No. A10809
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PPAR 激动剂

Rosiglitazone maleate是一种噻唑烷二酮类抗高血糖药，是PPARγ的高亲和、选择性的激动剂。了解更多

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Pioglitazone (Actos)

Catalog No. A11680
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PPARγ 激动剂

Pioglitazone (Actos)是选择性刺激核受体过氧化物酶体增殖物激活的受体γ（PPAR-γ），并在较小程度上刺激PPAR-α。了解更多

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Rosiglitazone (BRL-49653)

Catalog No. A10807
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PPAR 激动剂

Rosiglitazone (BRL-49653)是有效的降糖药，也是有效的噻唑烷二酮类胰岛素增敏剂，在大鼠，3T3-L1和人体脂肪细胞中IC50分别为12，4和9 nM。Rosiglitazone是PPAR-gamma的配体，对PPAR-alpha没有结合力。了解更多

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Troglitazone

Catalog No. A11981
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PPARγ 激动剂

Troglitazone是一种选择性PPARγ受体激动剂（鼠和人PPARγ受体的EC50值分别为780和555 nM）。了解更多

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- Julien Allard, .et al. Drug-induced Hepatic Steatosis in Absence of Severe Mitochondrial Dysfunction in HepaRG Cells: Proof of Multiple Mechanism-Based Toxicity, Cell Biol Toxicol, 2020, Jun 14 PMID: 32535746
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GW 7647

Catalog No. A11982
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PPARα 激动剂

GW 7647是一种有效且高度选择性的PPARα激动剂（人PPARα，PPARγ和PPARδ受体的EC50值分别为6、1100和6200 nM）。了解更多

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L-165,041

Catalog No. A11983
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PPARδ 激动剂

L-165,041是有效的PPARδ激动剂（Ki = 6 nM）；与其他亚型相比，对小鼠和人类PPARδ受体的选择性显示> 100倍。了解更多

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pirinixic acid (WY 14643)

Catalog No. A12360
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PPARα 激动剂

pirinixic acid (WY 14643)是一种高效pparα激动剂。了解更多

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GW 501516

Catalog No. A11437
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PPARδ receptor 激动剂

GW501516是一种合成pparδ特异性激动剂，对pparδ (ki=1.1 nm)显示出高亲和力，其选择性超过pparα和pparγ的1000倍。了解更多

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Inolitazone dihydrochloride

Catalog No. A15129
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PPARγ 激动剂

Inolitazone dihydrochloride是一种新型的高亲和力PPARγ激动剂，可激活PPARγ，其EC50约为罗格列酮的EC50，对RIE细胞无影响。了解更多

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Bezafibrate

Catalog No. A16307
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PPAR 激动剂

Bezafibrate是首个经过临床测试的双重和泛PPAR共同激动剂。了解更多

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Clofibric Acid

Catalog No. A16463
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PPARα 激动剂

Clofibric Acid是PPARα激动剂和降血脂药。了解更多

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Etofylline

Catalog No. A17491
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PPAR agonist

Etofylline, also known as BRN-0251760, is a peroxisome proliferator-activated receptor (PPAR) agonist used to treat respiratory and cardiovascular disorders. Etofylline is often used as a bronchodilator. 了解更多

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BR102375

Catalog No. A18849
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PPAR γ agonist

BR102375 is a non-TZD peroxisome proliferator-activated receptor γ (PPAR γ) full agonist for the treatment of type 2 diabetes, reveals EC50 value of 0.28?μM and Amax ratio?of 98%. 了解更多

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VCE-004.8

Catalog No. A18549
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PPARγ and CB2 receptor dual agonist

VCE-004.8, a semi-synthetic multitarget cannabinoquinoid, is a specific PPARγ and CB2 receptor dual agonist with potent anti-inflammatory activity. 了解更多

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LJ570

Catalog No. A20081
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PPARα/PPARγ dual agonist

LJ570 is a PPARα/PPARγ dual agonist with EC50s of 1.05 and 0.12 μM, respectively. 了解更多

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Leriglitazone

Catalog No. A18636
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PPAR gamma agonist

Leriglitazone is a peroxisome proliferator activated receptor (PPAR) gamma agonist. 了解更多

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Chiglitazar

Catalog No. A12701
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PPARα/γ dual agonist

Chiglitazar is a PPARα/γ dual agonist, with EC50s of 1.2, 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively. 了解更多

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LXR-623

Catalog No. A21366
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LXRα and full LXRβ agonist

LXR-623 is a brain-penetrant partial LXRα and full LXRβ agonist, with IC50s of 24 nM and 179 nM, respectively. 了解更多

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RGX-104 free Acid

Catalog No. A21513
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LXR agonist

RGX-104 free Acid is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene. 了解更多

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AZ876

Catalog No. A21026
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LXR agonist

AZ876 is a novel high-affinity LXR agonist. 了解更多

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GW3965 HCl

Catalog No. A11204
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LXR-like receptors 激动剂

GW3965 HCl是一种选择性的口服活性肝X受体（LXR）完全激动剂。了解更多

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- Mohácsik P, .et al. A Transgenic Mouse Model for Detection of Tissue-Specific Thyroid Hormone Action, Endocrinology, 2018, Feb 1;159(2):1159-1171 PMID: 29253128
- Pencheva N, .et al. Broad-spectrum therapeutic suppression of metastatic melanoma through nuclear hormone receptor activation., Cell., 2014, 156(5):986-1001 PMID: 24581497
- Bin Dong, .et al. High-fructose diet downregulates long-chain acyl-CoA synthetase 3 expression in liver of hamsters via impairing LXR/RXR signaling pathway, J Lipid Res., 2013, May; 54(5): 1241-1254. PMID: 23427282
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T0901317

Catalog No. A12652
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LXR/FXR 激动剂

T0901317是有效的，高亲和力的肝X受体（LXR）激动剂（EC50~50 nM，LXR-β和LXR-β的Kd值分别为7和22 nM）。了解更多

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- Tian Yongsong, .et al. Tritium hydrogen-isotope exchange with electron-poor tertiary benzenesulfonamide moiety; application in late-stage labeling of T0901317, J Labelled Comp Radiopharm, 2022, Feb;65(2):36-44 PMID: 34957593
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GW3965

Catalog No. A15100
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Liver X Receptor 激动剂

GW3965是hLXRα和hLXRβ的有效选择性LXR激动剂，EC50分别为190和30 nM。了解更多

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- B Dong ,etc. High-fructose diet downregulates long-chain acyl-CoA synthetase 3 expression in liver of hamsters via impairing LXR/RXR signaling pathway. Journal of lipid research, 2013, 54(5), 1241-1254.
- N Pencheva ,etc. Broad-spectrum therapeutic suppression of metastatic melanoma through nuclear hormone receptor activation. Cell, 2014, 156(5), 986-1001.
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Sobetirome

Catalog No. A15241
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TRβ 激动剂

Sobetirome是一种甲状腺激素受体β（TRβ）特异性激动剂，Sobetirome设计用于选择性结合TRβ-1，EC50为0.16 μM。了解更多

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SR9243

Catalog No. A15535
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LXR 激动剂

SR9243是有效的选择性LXR反向激动剂。SR9243通过抑制脂质产生和Warburg效应杀死癌细胞。它在多种类型的癌症中诱导细胞死亡，并且不会引起副作用，而这些副作用已使先前针对这些过程的尝试脱轨。了解更多

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SR9238

Catalog No. A15763
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LXR Inverse 激动剂

SR9238是有效的选择性LXR反向激动剂（LXRβ和LXRα的IC50值分别为43和214 nM）。了解更多

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Cilofexor

Catalog No. A13143
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FXR agonist

Cilofexor (GS-9674) is a farnesoid X receptor (FXR) agonist. 了解更多

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Nidufexor

Catalog No. A12625
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FXR agonist

Nidufexor is a farnesoid X receptor (FXR) agonist. 了解更多

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INT-767

Catalog No. A21494
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dual FXR/TGR5 agonist

INT-767 is a dual farnesoid X receptor (FXR)/TGR5 agonist with mean EC50s of 30 and 630 nM, respectively. 了解更多

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Fexaramine

Catalog No. A21771
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FXR agonist

Fexaramine is a small molecule farnesoid X receptor (FXR) agonist with 100-fold increased affinity relative to natural compounds. 了解更多

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GW4064

Catalog No. A11141
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FXR 激动剂

GW4064是选择性的非甾体类法尼醇X受体（FXR）激动剂（EC50 = 15 nM）。了解更多

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- Dong-Hyun Kim, .et al. The critical role of FXR is associated with the regulation of autophagy and apoptosis in the progression of AKI to CKD, Cell Death Dis, 2021, Apr; 12(4): 320 PMID: 33767132
- Takae K, .et al. Evidence for the involvement of FXR signaling in ovarian granulosa cell function, J Reprod Dev, 2018, Nov 16 PMID: 30449821
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WAY-362450

Catalog No. A11186
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FXR 激动剂

WAY-362450是一种高效，选择性和口服可生物利用的法呢类X受体（FXR）激动剂（EC50：4 nM，eff = 149％）。了解更多

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- Dong-Hyun Kim, .et al. The critical role of FXR is associated with the regulation of autophagy and apoptosis in the progression of AKI to CKD, Cell Death Dis, 2021, Apr; 12(4): 320 PMID: 33767132
- Dong-Hyun Kim, .et al. Src-mediated crosstalk between FXR and YAP protects against renal fibrosis, FASEB J, 2019, Jul 12:fj201900325R PMID: 31298930
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Lithocholic acid

Catalog No. A12547
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FXR 激动剂

Lithocholic acid是胆汁酸，用作去污剂以溶解脂肪以供吸收。了解更多

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Obeticholic Acid

Catalog No. A13866
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FXR 激动剂

Obeticholic Acid是一种有效的选择性法呢类X受体（FXR）激动剂，EC50为99 nM。了解更多

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- Tomasz Kostrzewski, .et al. A Microphysiological System for Studying Nonalcoholic Steatohepatitis, Hepatol Commun, 2019, 13 November
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LY2562175

Catalog No. A17016
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FXR 激动剂

LY2562175是体外有效的选择性FXR激动剂，其EC50值为193 nM。具有强大的脂质调节特性，可降低临床前物种中的LDL和甘油三酸酯，同时提高HDL。了解更多

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Px-104

Catalog No. A16999
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FXR 激动剂

Px-104，也称为Px-102，是一种潜在的法呢素X受体（FXR）激动剂，可用于治疗非酒精性脂肪肝。了解更多

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