Search Result
Results for "
PPAR-γ Agonists
" in MedChemExpress (MCE) Product Catalog:
16
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-15655
-
|
PPAR
|
Neurological Disease
Metabolic Disease
|
GW 1929 is an orally active peroxisome proliferator-activated receptor-γ (PPARγ) agonist with a pKi of 8.84 for human PPAR-γ, and pEC50s of 8.56 and 8.27 for human PPAR-γ and murine PPAR-γ, respectively. GW 1929 (hydrochloride) has antidiabetic efficacy and neuroprotective potential .
|
-
-
- HY-N0246
-
|
LXR
Bacterial
|
Inflammation/Immunology
Cancer
|
Saikosaponin A is the main active ingredient in Bupleurum chinense, which can regulate lipid metabolism and promote cholesterol efflux in early atherosclerosis. In addition, Saikosaponin A may also serve as a potential peroxisome proliferator-activated receptor γ (PPAR-γ) agonist, significantly promoting the expression of PPAR-γ. Saikosaponin A can be used in the study of hyperlipidemic pancreatitis .
|
-
-
- HY-120160
-
CP-86325
|
PPAR
|
Neurological Disease
Metabolic Disease
|
Darglitazone (CP-86325), a thiazolidinedione, is a potent, selective, and orally active PPAR-γ agonist. Darglitazone is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research .
|
-
-
- HY-146480
-
|
PPAR
|
Cancer
|
PPARγ agonist 5 (Compound 1) is a potent and selective agonist of PPARγ. PPARγ agonist 5 has the potential for the research of cancer diseases .
|
-
-
- HY-110022
-
|
PPAR
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
GW1929 hydrochloride is an orally active peroxisome proliferator-activated receptor-γ (PPARγ) agonist with a pKi of 8.84 for human PPAR-γ, and pEC50s of 8.56 and 8.27 for human PPAR-γ and murine PPAR-γ, respectively. GW1929 hydrochloride has antidiabetic efficacy and neuroprotective potential. GW1929 hydrochloride suppresses neuronal apoptosis and shows anti-inflammatory potential .
|
-
-
- HY-113473
-
|
PPAR
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
10-Nitrolinoleic acid is a potent peroxisome proliferator-activated receptor γ (PPARγ) agonist. 10-Nitrolinoleic acid competes with [ 3H]Rosiglitazone for binding to PPAR-γ, with an IC50 of 0.22 μM .
|
-
-
- HY-14831
-
MBX 102; JNJ 39659100
|
PPAR
|
Metabolic Disease
|
Arhalofenate (MBX 102) is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes.
|
-
-
- HY-N0246R
-
|
LXR
Bacterial
|
Metabolic Disease
Inflammation/Immunology
|
Saikosaponin A (Standard) is the analytical standard of Saikosaponin A. This product is intended for research and analytical applications. Saikosaponin A is the main active ingredient in Bupleurum chinense, which can regulate lipid metabolism and promote cholesterol efflux in early atherosclerosis. In addition, Saikosaponin A may also act as a potential peroxisome proliferator-activated receptor-γ (PPAR-γ) agonist, significantly promoting the expression of PPAR-γ. Saikosaponin A can be used in the study of hyperlipidemic pancreatitis .
|
-
-
- HY-120160A
-
CP 86325 Sodium
|
PPAR
|
Neurological Disease
Metabolic Disease
|
Darglitazone Sodium, a thiazolidinedione, is an orally active, potent, and selective PPAR-γ (peroxisome proliferator-activated receptor) agonist. Darglitazone Sodium is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research .
|
-
-
- HY-106181A
-
R-106056 hydrochloride
|
PPAR
|
Metabolic Disease
|
Rivoglitazone hydrochloride (R-106056 hydrochloride) is a peroxisome proliferator-activated receptor-γ (PPAR-γ) agonist. Rivoglitazone hydrochloride (R-106056 hydrochloride) exerts its anti-diabetic effect by activating PPARγ to regulate the expression of a large number of genes related to lipid and glucose metabolism. Rivoglitazone hydrochloride (R-106056 hydrochloride) can be used to study insulin secretion and insulin resistance in animal models of diabetes .
|
-
-
- HY-146482
-
|
PPAR
|
Cancer
|
PPARγ agonist 6 (Compound 12) is a potent and selective agonist of PPARγ. PPARγ agonist 6 has the potential for the research of cancer diseases .
|
-
-
- HY-146438
-
|
PPAR
|
Cancer
|
PPARγ agonist 3 (Compound 18a) is a potent and selective agonist of PPARγ. PPARγ agonist 3 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 3 exerts antitumor potency only in combination with Imatinib .
|
-
-
- HY-160003
-
|
PPAR
|
Metabolic Disease
|
PPARγ agonist 9 is an agonist of PPARγ. PPARγ agonist 9 is the analogue of lysophosphatidic acid with an EC50 more than 10 μM for LPA3 receptor .
|
-
-
- HY-146439
-
|
PPAR
|
Cancer
|
PPARγ agonist 4 (Compound 18b) is a potent and selective agonist of PPARγ. PPARγ agonist 4 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 4 exerts antitumor potency only in combination with Imatinib .
|
-
-
- HY-147511
-
|
PPAR
|
Others
|
PPARγ agonist 7 (Compound 3a) is a potent and selective agonist of PPARγ. PPARγ agonist 7 promotes adiponectin production in human bone marrow mesenchymal stem cells (hBM-MSCs) as a novel PPARγ full agonist (EC50, 4.34 μM) .
|
-
-
- HY-153982
-
|
PPAR
|
Metabolic Disease
|
PPARγ agonist 8 is an agonist of PPARγ. PPARγ agonist 8 induces peroxisome proliferator response element (PPRE)-luciferase activity with an EC50 of 0.2 μM .
|
-
-
- HY-146731
-
|
PPAR
|
Cardiovascular Disease
Metabolic Disease
|
PPARγ agonist 1 (compound 15) is a potent agonist of PPARγ. PPARγ agonist 1 shows high efficacy to activate hPPARγ without raising a full agonism and probably avoiding adverse effects. PPARγ agonist 1 has the potential for the research of cardiovascular diseases associated with metabolic disorders .
|
-
-
- HY-162320
-
|
PPAR
|
Metabolic Disease
|
PPARγ agonist 12 (compound 9i) is a potent and selective PPARγ agonist with EC50s of 3.98 and 15.42 μM against PPARγ and PPARδ, respectively. PPARγ agonist 12 improves insulin secretion and has anti-diabetic effect .
|
-
-
- HY-N6869
-
|
Antibiotic
PPAR
Bacterial
Fungal
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
Dehydroabietic acid is a diterpene resin acid that can be isolated from Pinus and Picea. Dehydroabietic acid has anti-bacterial, anti-fungal, anti-inflammatory, and anticancer activities. Dehydroabietic acid is a dual PPAR-α/γ agonist and PPAR-γ partial agonist, which can attenuate insulin resistance (IR) and hepatic steatosis induced by HFD-consumption in mice .
|
-
-
- HY-146742
-
|
PPAR
|
Metabolic Disease
|
PPARγ agonist 2 is a potent PPARγ partial agonist and can be used for metabolic disease research .
|
-
-
- HY-116468
-
-
-
- HY-B0205
-
CV 11974
|
Angiotensin Receptor
PPAR
|
Cardiovascular Disease
Endocrinology
Cancer
|
Candesartan (CV 11974) is an orally active angiotensin II AT1-Receptor blocker and PPAR-γ agonist. Candesartan has potent and long-lasting antihypertensive effects. Candesartan can be used for the research of hypertension, chronic heart failure (CHF) and Traumatic brain injury (TBI) .
|
-
-
- HY-16086
-
DRF 2593; NN 2344
|
PPAR
|
Metabolic Disease
|
Balaglitazone is a selective partial PPARγ agonist with an EC50 of 1.351 μM for human PPARγ.
|
-
-
- HY-163294
-
|
PPAR
|
Metabolic Disease
|
PPARγ agonist 10 (compound 33g) is a PPARγ agonist, and stimulats the insulin secretion, glucose uptake and insulin Sensitivity in βTC6 Cells .
|
-
-
- HY-148351
-
|
PPAR
|
Cancer
|
BAY-0069 is a potent and selective PPARγ inverse agonist with an IC50 value of 6.3 nM and 24 nM for human PPARγ and mouse PPARγ. BAY-0069 can be used to research cancer .
|
-
-
- HY-14792
-
Efatutazone; CS-7017; RS5444
|
PPAR
|
Cancer
|
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.
|
-
-
- HY-14601
-
U 72107A; AD 4833
|
PPAR
Ferroptosis
|
Metabolic Disease
Cancer
|
Pioglitazone hydrochloride is a potent and selective PPARγ agonist with EC50s of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.
|
-
-
- HY-N6869R
-
|
Antibiotic
PPAR
Bacterial
Fungal
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
Dehydroabietic acid (Standard) is the analytical standard of Dehydroabietic acid. This product is intended for research and analytical applications. Dehydroabietic acid is a diterpene resin acid that can be isolated from Pinus and Picea. Dehydroabietic acid has anti-bacterial, anti-fungal, anti-inflammatory, and anticancer activities. Dehydroabietic acid is a dual PPAR-α/γ agonist and PPAR-γ partial agonist, which can attenuate insulin resistance (IR) and hepatic steatosis induced by HFD-consumption in mice .
|
-
-
- HY-14792B
-
Efatutazone dihydrochloride; CS-7017 dihydrochloride; RS5444 dihydrochloride
|
PPAR
|
Cancer
|
Inolitazone dihydrochloride (Efatutazone dihydrochloride) is a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC50 of 0.8 nM for growth inhibition.
|
-
-
- HY-150308
-
|
PPAR
|
Cancer
|
SR10221, a noncovalent inverse agonist of PPARγ, represses downstream PPARγ target genes leading to growth inhibition in bladder cancer cell lines .
|
-
-
- HY-154985
-
|
PPAR
Bombesin Receptor
ERK
|
Metabolic Disease
|
DSO-5a is a potent, selective, orally active BB3 agonist. DSO-5a is a representative DMAKO-00 derivative compound. DSO-5a upregulates ppar-γ activity through BB3 and activates ERK1/2 phosphorylation. DSO-5a can be used in diabetes-related research .
|
-
-
- HY-B0205R
-
CV 11974 (Standard)
|
Angiotensin Receptor
PPAR
|
Cardiovascular Disease
Endocrinology
Cancer
|
Candesartan (Standard) is the analytical standard of Candesartan. This product is intended for research and analytical applications. Candesartan (CV 11974) is an orally active angiotensin II AT1-Receptor blocker and PPAR-γ agonist. Candesartan has potent and long-lasting antihypertensive effects. Candesartan can be used for the research of hypertension, chronic heart failure (CHF) and Traumatic brain injury (TBI) .
|
-
-
- HY-50935S
-
-
-
- HY-13956S
-
U 72107-d4
|
PPAR
Ferroptosis
|
Metabolic Disease
Cancer
|
Pioglitazone-d4 is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1].
|
-
-
- HY-116521
-
-
-
- HY-B0287
-
|
PPAR
|
Metabolic Disease
|
Clofibrate is an agonist of PPAR, with EC50s of 50 μM, ∼500 μM for murine PPARα and PPARγ, and 55 μM, ∼500 μM for human PPARα and PPARγ, respectively.
|
-
-
- HY-100428
-
MCC-555; Isaglitazone
|
PPAR
|
Metabolic Disease
|
Netoglitazone is a dual agonist of PPARα and PPARγ with antihyperglycemic activity .
|
-
-
- HY-13956
-
U 72107
|
PPAR
Ferroptosis
|
Metabolic Disease
Cancer
|
Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research .
|
-
-
- HY-13956B
-
U 72107 potassium
|
PPAR
Ferroptosis
|
Metabolic Disease
Cancer
|
Pioglitazone (U 72107) potassium is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone potassium can be used in diabetes research .
|
-
-
- HY-50935
-
CS-045
|
PPAR
Autophagy
Apoptosis
Ferroptosis
|
Metabolic Disease
Cancer
|
Troglitazone is an orally active PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively. Troglitazone has anticancer activity, prevents and inhibits the development of type 2 diabetes.
|
-
-
- HY-106181
-
R-106056
|
PPAR
|
Metabolic Disease
|
Rivoglitazone is a thiazolidinedione-derivative PPARγ agonist for the research of type 2 diabetes mellitus.
|
-
-
- HY-N2025
-
|
PPAR
Glucosidase
|
Metabolic Disease
|
Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .
|
-
-
- HY-117727
-
MIN-102; Hydroxypioglitazone
|
PPAR
|
Metabolic Disease
|
Leriglitazone (MIN-102; Hydroxypioglitazone), a metabolite of pioglitazone. Leriglitazone PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy. Leriglitazone binds to the PPARγ C-terminal ligand-binding domain (LBD) with a Ki of 1.2 μM,Leriglitazone induces transcriptional efficacy of the PPARγ (LBD) with an EC50 of 680 nM .
|
-
-
- HY-117727A
-
MIN-102 hydrochloride; Hydroxypioglitazone hydrochloride
|
PPAR
|
Metabolic Disease
|
Leriglitazone (MIN-102; Hydroxypioglitazone) hydrochloride, a metabolite of pioglitazone. Leriglitazone hydrochloride PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy. Leriglitazone hydrochloride binds to the PPARγ C-terminal ligand-binding domain (LBD) with a Ki of 1.2 μM,Leriglitazone induces transcriptional efficacy of the PPARγ (LBD) with an EC50 of 680 nM .
|
-
-
- HY-110118
-
|
PPAR
|
Metabolic Disease
|
Edaglitazone is a potent, selective and orally active PPARγ agonist, with EC50s of 35.6 nM and 1053 nM for PPARα and PPARγ, respectively. Edaglitazone displays antiplatelet, antidiabetic and anti-hyperglycemic activity .
|
-
-
- HY-108572
-
|
PPAR
|
Cardiovascular Disease
Metabolic Disease
|
S26948 is a specific peroxisome proliferator-activated receptor γ (PPARγ) modulator (EC50=8.83 nM) with potent antidiabetes and antiatherogenic effects. S26948 is a specific high-affinity agonist for PPARγ .
|
-
-
- HY-14601R
-
U 72107A (Standard); AD 4833 (Standard)
|
PPAR
Ferroptosis
|
Metabolic Disease
Cancer
|
Pioglitazone (hydrochloride) (Standard) is the analytical standard of Pioglitazone (hydrochloride). This product is intended for research and analytical applications. Pioglitazone hydrochloride is a potent and selective PPARγ agonist with EC50s of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.
|
-
-
- HY-13956S1
-
|
Isotope-Labeled Compounds
PPAR
Ferroptosis
|
Metabolic Disease
Cancer
|
Pioglitazone-d4 (alkyl) (U 72107-d4 (alkyl)) is the deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1][2].
|
-
-
- HY-111254
-
|
PPAR
|
Metabolic Disease
|
GQ-16 is a moderate affinity ligand for the ligand-binding domain (LBD) of PPARγ, exhibiting a Ki of 160 nM. GQ-16 is an effective inhibitor of Cdk5-mediated phosphorylation of PPARγ. GQ-16 is a partial agonist of PPARγ with reduced adipogenic actions. GQ-16 promotes insulin Sensitization without weight gain .
|
-
-
- HY-N9333
-
-
- HY-108014
-
|
Others
|
Others
|
(+)-KDT 501 is an inactive enantiomer of KDT 501. KDT 501 is a modest PPARγ agonist, with antidiabetic activity.
|
-
- HY-B0287S
-
|
PPAR
|
Metabolic Disease
|
Clofibrate-d4 is the deuterium labeled Clofibrate. Clofibrate is an agonist of PPAR, with EC50s of 50 μM, ∼500 μM for murine PPARα and PPARγ, and 55 μM, ∼500 μM for human PPARα and PPARγ, respectively.
|
-
- HY-117103
-
INT131
|
PPAR
|
Metabolic Disease
|
AMG131 (INT131), a potent and highly selective PPARγ partial agonist, binds to PPARγ and displaces Rosiglitazone with a Ki of ~10 nM. AMG131 can be used for research of type-2 diabetes mellitus (T2DM) .
|
-
- HY-105074
-
GI262570; GI262570X
|
PPAR
|
Metabolic Disease
|
Farglitazar is a PPARγ agonist that has significant therapeutic benefits such as glycemic control in type 2 diabetic patients.
|
-
- HY-148352
-
|
PPAR
|
Cancer
|
BAY-4931 is a potent, covalent and selective PPARγ inverse-agonist with an IC50 of 0.17 nM .
|
-
- HY-148922
-
|
PPAR
|
Metabolic Disease
|
PPARα/γ agonist 2 is an orally active PPARα full agonist and PPARγ partial agonist. PPARα/γ agonist 2 activates PPARα and PPARγ with EC50 values of 0.95 μM and 0.91 μM respectively. PPARα/γ agonist 2 is also a PTP1B inhibitor. PPARα/γ agonist 2 is an anti-diabetic agent .
|
-
- HY-U00340
-
|
PPAR
|
Metabolic Disease
|
PPAR agonist 1 is an agonist of PPAR α and PPAR γ, used for reducing blood glucose, lipid levels, lowering cholesterol and reducing body weight.
|
-
- HY-101292
-
|
PPAR
|
Metabolic Disease
|
FK614 is an orally active, non-thiazolidinedione (TZD) type, and selective PPARγ modulator (SPPARM). FK614 functions as a PPARγ agonist with potent anti-diabetic activity in vivo. FK614 has different effects on the activation of PPARγ at each stage of adipocyte differentiation. FK614 can be used for the research of hyperglycemia, hypertriglyceridemia, glucose intolerance and type 2 diabetes .
|
-
- HY-13956R
-
|
PPAR
Ferroptosis
|
Metabolic Disease
Cancer
|
Pioglitazone (Standard) is the analytical standard of Pioglitazone. This product is intended for research and analytical applications. Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research .
|
-
- HY-B0287R
-
|
PPAR
|
Metabolic Disease
|
Clofibrate (Standard) is the analytical standard of Clofibrate. This product is intended for research and analytical applications. Clofibrate is an agonist of PPAR, with EC50s of 50 μM, ~500 μM for murine PPARα and PPARγ, and 55 μM, ~500 μM for human PPARα and PPARγ, respectively.
|
-
- HY-N2025R
-
|
PPAR
Glucosidase
|
Metabolic Disease
|
Oroxin A (Standard) is the analytical standard of Oroxin A. This product is intended for research and analytical applications. Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .
|
-
- HY-16995
-
Wy-14643
|
PPAR
|
Metabolic Disease
Inflammation/Immunology
|
Pirinixic acid (Wy-14643) is a potent agonist of PPARα, with EC50s of 0.63 μM, 32 μM for murine PPARα and PPARγ, and 5.0 μM, 60 μM, 35 μM for human PPARα, PPARγ and PPARδ, respectively.
|
-
- HY-117422
-
11-Oxo-prosta-5Z,12E,14Z-trien-1-oic acid
|
PPAR
|
Cancer
|
CAY10410 (11-Oxo-prosta-5Z), a 15d-PGJ2 analog, is a potent PPARγ agonist. CAY10410 has the ability to activate PPARγ in human B cells without killing B lymphocytes .
|
-
- HY-13956C
-
(R)-U 72107
|
PPAR
|
Neurological Disease
|
(R)-Pioglitazone ((+)-pioglitazone) is the R enantiomer of Pioglitazone (HY-13956). (R)-Pioglitazone is an orally active and selective peroxisome proliferator-activated receptor (PPARγ) agonist with high affinity binding to the PPARγ ligand-binding domain. (R)-Pioglitazone can be used for the research of Alzheimer's disease .
|
-
- HY-122235
-
-
- HY-144111
-
|
PPAR
|
Inflammation/Immunology
|
PPARα/δ agonist 1 is a potent PPARα/PPARδ dual agonist (PPARα EC50=7.0 nM; PPARδ EC50=8.4 nM). PPARα/δ agonist 1 is a high selectivity over PPARγ (PPARγ EC50=1316.1 nM). PPARα/δ agonist 1 has the potential for the research of nonalcoholic steatohepatitis .
|
-
- HY-B0637
-
BM15075
|
PPAR
|
Cardiovascular Disease
Metabolic Disease
|
Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.
|
-
- HY-50935R
-
|
PPAR
Autophagy
Apoptosis
Ferroptosis
|
Metabolic Disease
Cancer
|
Troglitazone (Standard) is the analytical standard of Troglitazone. This product is intended for research and analytical applications. Troglitazone is an orally active PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively. Troglitazone has anticancer activity, prevents and inhibits the development of type 2 diabetes.
|
-
- HY-117727S
-
MIN-102-d4; Hydroxypioglitazone-d4
|
Isotope-Labeled Compounds
PPAR
|
Metabolic Disease
|
Leriglitazone-d4 (MIN-102-d4; Hydroxypioglitazone-d4) is deuterium labeled Leriglitazone. Leriglitazone (Hydroxypioglitazone), a metabolite of pioglitazone.Leriglitazone (Hydroxypioglitazone) PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy.Leriglitazone (Hydroxypioglitazone) binds to the PPARγ C-terminal ligand-binding domain (LBD) with Ki of 1.2 μM,induces transcriptional efficacy of the PPARγ (LBD) with EC50 of 680 nM .
|
-
- HY-14817
-
PPM 204
|
PPAR
|
Metabolic Disease
|
Indeglitazar (PPM 204) is an orally available PPAR pan-agonist for all three PPARα, PPARδ and PPARγ .
|
-
- HY-17386S
-
-
- HY-N0234
-
7-O-Methylbavachin; Bavachinin A
|
Amyloid-β
PPAR
HIF/HIF Prolyl-Hydroxylase
|
Inflammation/Immunology
|
Bavachinin is agonist of pan-peroxisome proliferator-activated receptor (PPAR), with the IC50 value of 21.043 μM, 12.819 μM, and 0.622 μM to PPAR-α, RRAR-β/δ, and PPAR-γ, respectively. Bavachinin is an inhibitor of HIF-1α. Bavachinin exhibits antitumor activity against non-small cell lung cancer by targeting RRAR-γ. Bavachinin is a natural compound with anti-inflammatory and anti-angiogenic activities. Bavachinin has orally bioactivity. .
|
-
- HY-111775
-
|
PPAR
|
Metabolic Disease
|
LJ570 is a PPARα/PPARγ dual agonist with EC50s of 1.05 and 0.12 μM, respectively .
|
-
- HY-123654
-
|
PPAR
|
Neurological Disease
|
L-796449 is a potent PPARγ agonist. L-796449 shows neuroprotective. L-796449 has the potential for the research of stroke .
|
-
- HY-107333
-
|
PPAR
|
Metabolic Disease
|
Cinoxate is a hypertrophic peroxisome proliferator activating receptor γ (PPARγ) agonist with Ki value of 18.0 μM. Cinoxate can be used to study obesity .
|
-
- HY-B0637S
-
|
PPAR
|
Cardiovascular Disease
Metabolic Disease
|
Bezafibrate-d6 is the deuterium labeled Bezafibrate. Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.
|
-
- HY-B0637S1
-
BM15075-d4
|
Isotope-Labeled Compounds
PPAR
|
Cardiovascular Disease
Metabolic Disease
|
Bezafibrate-d4 is deuterium labeled Bezafibrate. Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.
|
-
- HY-121798
-
|
PPAR
|
Metabolic Disease
|
TZD18 is a potent and orally active PPARα and PPARγ dual agonist with IC50 values of 0.028, 0.057, >10 µM for PPARα, PPARγ, PPARδ, respectively. TZD18 reduces plasma levels of both glucose and triglycerides in diabetic mice. TZD18 has the potential for the research of type 2 diabetes .
|
-
- HY-117761
-
|
PPAR
|
Metabolic Disease
Cancer
|
MHY908 is a potent dual agonist of PPARα and PPARγ . MHY908 also inhibits melanogenesis through inhibition of mushroom tyrosinase activity .
|
-
- HY-120542
-
|
PPAR
|
Metabolic Disease
|
SR 1824 is a non-agonist PPARγ ligand that blocks Cdk5-mediated phosphorylation. SR 1824 has anti-diabetic effects .
|
-
- HY-B0637R
-
|
PPAR
|
Cardiovascular Disease
Metabolic Disease
|
Bezafibrate (Standard) is the analytical standard of Bezafibrate. This product is intended for research and analytical applications. Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.
|
-
- HY-N0234R
-
|
Amyloid-β
PPAR
HIF/HIF Prolyl-Hydroxylase
|
Inflammation/Immunology
|
Bavachinin (Standard) is the analytical standard of Bavachinin. This product is intended for research and analytical applications. Bavachinin is agonist of pan-peroxisome proliferator-activated receptor (PPAR), with the IC50 value of 21.043 μM, 12.819 μM, and 0.622 μM to PPAR-α, RRAR-β/δ, and PPAR-γ, respectively. Bavachinin is an inhibitor of HIF-1α. Bavachinin exhibits antitumor activity against non-small cell lung cancer by targeting RRAR-γ. Bavachinin is a natural compound with anti-inflammatory and anti-angiogenic activities. Bavachinin has orally bioactivity. .
|
-
- HY-U00450
-
|
PPAR
NF-κB
|
Inflammation/Immunology
Cancer
|
4-O-Methyl honokiol is a natural neolignan isolated from Magnolia officinalis, acts as a PPARγ agonist, and inhibtis NF-κB activity, used for cancer and inflammation research.
|
-
- HY-16421
-
(-)-DRF 2725; NNC 61-0029
|
PPAR
|
Metabolic Disease
|
Ragaglitazar is a PPARα and PPARγ agonist with potent lipid-lowering and insulin-sensitizing efficacy in animal models. Ragaglitazar improves glycemic control and lipid profile in type 2 diabetic.
|
-
- HY-20019
-
|
PPAR
|
Metabolic Disease
|
L-165041 is a cell permeable PPARδ agonist, with Kis of 6 nM and appr 730 nM for PPARδ and PPARγ, respectively, and induces adipocyte differentiation in NIH-PPARδ cells.
|
-
- HY-13861
-
|
PPAR
|
Cardiovascular Disease
|
GW7647 is a potent PPARα agonist, with EC50s of 6 nM, 1.1 μM, and 6.2 μM for human PPARα, PPARγ and PPARδ, respectively.
|
-
- HY-N7624
-
3-Oxoolean-12-en-28-oic acid methyl ester
|
PPAR
|
Cancer
|
Methyl oleanonate is a natural triterpene PPARγ agonist isolated from the species of Pistacia lentiscus var. Chia . Methyl oleanonate is a modified oleanolic acid derivative with anti-cancer effects .
|
-
- HY-160161
-
|
PPAR
|
Cancer
|
BAY-5094 is a PPAR gamma (PPARG) inverse agonist. BAY-5094 has oral activity. BAY-5094 can be used in the research of luminal bladder cancer .
|
-
- HY-163547
-
|
PPAR
|
Inflammation/Immunology
|
PPAR agonist 5 (compound 4b) is a potent PPAR agonist with EC50 values of 3.20, 1.51, 1.92 µM for PPARα, PPARβ/δ, PPARγ, respectively. PPAR agonist 5 shows anti-inflammatory effect .
|
-
- HY-N0163
-
-
- HY-10678
-
|
PPAR
|
Cardiovascular Disease
|
BMS-687453 is a potent and selective PPARα agonist, with an EC50 and IC50 of 10 nM and 260 nM for human PPARα and 4100 nM and >15000 nM for PPARγ in PPAR-GAL4 transactivation assays.
|
-
- HY-106266
-
Carfloglitazar
|
PPAR
|
Metabolic Disease
|
Chiglitazar (Carfloglitazar) is a PPARα/γ dual agonist, with EC50s of 1.2, 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively.
|
-
- HY-19937
-
|
PPAR
|
Metabolic Disease
|
Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
|
-
- HY-19937A
-
|
PPAR
|
Metabolic Disease
|
Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
|
-
- HY-19394
-
|
PPAR
|
Metabolic Disease
|
CLX-0921 is an orally active PPARγ agonist with an IC50 of 1.54 μM. CLX-0921 has a potent antihyperglycemic activity, and can be used for the study of type 2 diabetes .
|
-
- HY-17444
-
|
PPAR
|
Metabolic Disease
Cancer
|
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, and approximately 0.2 μM for both rat and human PPARγ. Tesaglitazar induces interstitial mesenchymal cell DNA synthesis and fibrosarcomas in subcutaneous tissues in rats .
|
-
- HY-143239
-
|
PPAR
|
Metabolic Disease
|
PPARα/γ agonist 1 (compound 5b) is a potent and dual PPARα/γ partial agonist with EC50 values of 28 nM and 69 nM for PPARα and PPARγ, respectively. PPARα/γ agonist 1 is a promising prototype for dyslipidemia and diabetes research .
|
-
- HY-119248
-
MK-0767
|
PPAR
|
Metabolic Disease
|
KRP-297 is a PPARα and PPARγ agonist potentially for the research of type 2 diabetes and dyslipidemia. KRP-297 restores reduced lipid oxidation, and inhibits of enhanced lipogenesis and triglyceride accumulation in the liver.
|
-
- HY-130289
-
4-Hydroxy docosahexaenoic acid; (±)4-HDoHE
|
PPAR
|
Metabolic Disease
Inflammation/Immunology
|
(±)4-HDHA (4-Hydroxy docosahexaenoic acid) is an autoxidation product of Docosahexaenoic acid (HY-B2167) (DHA). (±)4-HDHA is a PPARγ agonist, antidiabetic and anti-inflammatory agent .
|
-
- HY-114853
-
|
PPAR
|
Metabolic Disease
|
BVT.13 is an orally active and selective PPARγ agonist with a maximal efficacy similar to that of Rosiglitazone (HY-17386). In addition, BVT.13 exhibits antidiabetic activity in ob/ob mice .
|
-
- HY-14728
-
R1439; RO0728804
|
PPAR
|
Metabolic Disease
|
Aleglitazar (R1439) is a potent dual PPARα/γ agonist, with IC50s of 38 nM and 19 nM for human PPARa and PPARγ, respectively. Aleglitazar can be used for the research of type II diabetes .
|
-
- HY-128344
-
|
PARP
Apoptosis
|
Metabolic Disease
|
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% .
|
-
- HY-163443
-
|
PPAR
|
Others
|
PPAR agonist 4 (Compound 12) is an orally active agonist for peroxisome proliferator-activated receptor (PPAR), which activates PPARα, PPARδ and PPARγ with EC50s of 0.7, 0.7 and 1.8 μM, respectively. PPAR agonist 4 exhibits anti-liver fibrosis efficacy .
|
-
- HY-118514
-
|
PPAR
|
Metabolic Disease
|
CAY10514 is an aromatic of 8(S)-HETE. CAY10514 acts as a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ with IC50 of 0.173 and 0.642 μM, respectively .
|
-
- HY-113631
-
|
PPAR
|
Neurological Disease
Metabolic Disease
|
Amorfrutin B is a highly potent natural peroxisome proliferation-activated receptor γ (PPARγ) agonist with oral activity with Ki values of 19 nM and EC50 values of 73 nM, respectively. Amorfrutin B has hypoglycemic and neuroprotective activities .
|
-
- HY-139172
-
|
PPAR
|
Metabolic Disease
|
MD001 is a PPARα/γ dual agonist and can increase the transcriptional activity of PPARα and PPARγ. MD001 enhances the expression of genes related to β-oxidation and fatty acid and glucose uptake .
|
-
- HY-15027
-
-
- HY-19522A
-
MBX-8025 sodium salt; RWJ-800025 sodium salt
|
PPAR
|
Metabolic Disease
|
Seladelpar sodium salt (MBX-8025) is an orally active, potent and specific PPARδ agonist with an EC50 of 2 nM, showing more than 750-fold and 2500-fold selectivity over the PPARα and PPARγ receptors, respectively.
|
-
- HY-N7687
-
|
PPAR
|
Metabolic Disease
Inflammation/Immunology
|
Caulophyllogenin is a triterpene saponin extracted from M. polimorpha. Caulophyllogenin is a partial PPARγ agonist, with an EC50 of 12.6 μM. Caulophyllogenin can be used for the research of type-2 diabetes, obesity, metabolic syndrome and inflammation .
|
-
- HY-13928
-
-
- HY-108523
-
UVI 2112
|
RAR/RXR
|
Metabolic Disease
|
LG100754 (UVI 2112) is a RXR dimers modulater. LG100754 acts as a RXR:RXR homodimer antagonist, but functions as a agonist towards RXR:PPARα and RXR:PPARγ heterodimers. LG100754 is an insulin sensitizer that functions through RXR .
|
-
- HY-106278
-
|
PPAR
|
Metabolic Disease
|
GW 590735 is a potent and selective PPARα agonist. GW 590735 showsEC50=4 nM on PPARα and at least 500-fold selectivity versus PPARδ and PPARγ. GW 590735 can be used for the research of dyslipidemia .
|
-
- HY-113827
-
|
Nuclear Hormone Receptor 4A/NR4A
|
Inflammation/Immunology
|
THPN is a potent Nur77 agonist. THPN specifically binds the LBD of Nur77 (TR3) but not that of retinoic acid receptor α and PPARγ with a Kd of 270 nM. THPN leads to Nur77 translocation to the mitochondria to induce autophagic cell death in melanoma .
|
-
- HY-111616
-
|
PPAR
Angiotensin Receptor
|
Cardiovascular Disease
Others
|
GSK1820795A, as a telmisartan analog, is a selective hGPR132a antagonist. GSK1820795A blocks activation of yeast cells expressing hGPR132a by N-acylamides . GSK1820795A is also a angiotensin II antagonists and partial PPARγ agonists (compound 38) .
|
-
- HY-161999
-
|
Glucosidase
|
Metabolic Disease
Inflammation/Immunology
|
α-Glucosidase-IN-73 (compound 16b) is an α-Glucosidase inhibitor with IC50 of 0.158 μM. α-Glucosidase-IN-73 can activate PPAR γ. α-Glucosidase-IN-73 can be used in anti-diabetic and anti-inflammatory studies .
|
-
- HY-15027S
-
-
- HY-17386
-
-
- HY-N6642
-
|
PPAR
Apoptosis
|
Inflammation/Immunology
Cancer
|
Ankaflavin, isolated from Monascus-Fermented red rice, is an orally active PPARγ agonist. Ankaflavin exhibits selective cytotoxic effect and induces cell death through apoptosis on cancer cells. Ankaflavin has anti-inflammatory, anti-cancer, antiatherosclerotic, and hypolipidemic effects .
|
-
- HY-17386A
-
-
- HY-17386B
-
-
- HY-151963
-
|
PPAR
Glucocorticoid Receptor
|
Metabolic Disease
|
PPARγ/GR modulator 1 is an orally active dual agonist of PPARγ and glucocorticoid receptor (GR), with Kis of 3.3 and 33.6 μM, respectively. PPARγ/GR modulator 1 can be used for the research of metabolic diseases, such as diabetes .
|
-
- HY-N0163R
-
-
- HY-124581
-
|
PPAR
|
Metabolic Disease
|
DS-6930 is a potent and selective agonist of PPARγ, with an EC50 of 41 nM. DS-6930 could robust reduce plasma glucose (PG), and with fewer PPARγ-related adverse effects than Rosiglitazone. DS-6930 can be used for the research of diabetes .
|
-
- HY-112813
-
-
- HY-134997
-
4-oxo DHA
|
Others
|
Cancer
|
4-oxo Docosahexaenoic acid (4-oxo DHA) is a putative metabolite of Docosahexaenoic acid (HY-B2167) with antiproliferative and PPARγ agonist activity. It inhibits the growth of several triple negative breast cancer cell lines (MCF-10F, trMCF, bsMCF, MDA-MB-231, and BT549) at 50-100 μM, however it increased proliferation of MCF-7 cells. 4-oxo DHA binds covalently to PPARγ and activates gene transcription in luciferase reporter assays and in dendritic cells with EC50 values of approximately 8-16 μM.
|
-
- HY-19848
-
LBM-642
|
PPAR
|
Metabolic Disease
|
Cevoglitazar (LBM-642) is an orally active and highly potent PPARα and PPARγ dual agonist. Cevoglitazar can reduce food intake, body weight, and fasting plasma insulin in obese mice and cynomolgus monkeys. Cevoglitazar has the potential for diabetes and obesity-related disorders research .
|
-
- HY-19937S1
-
|
Isotope-Labeled Compounds
|
Others
|
Saroglitazar-d4 is the deuterium-labeled Saroglitazar (HY-19937). Saroglitazar-d4 is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
|
-
- HY-121671
-
|
Others
|
Neurological Disease
|
TBTC is a selective agonist with the activity of improving behavioral deficits in Alzheimer's disease model mice. TBTC can effectively activate the heterodimerization of RXRα with LXRα or PPARγ. TBTC stimulates the expression of apoE, ABCA1, and ABCG1 genes and reduces Aβ content in cells and animal models .
|
-
- HY-162578
-
|
PPAR
|
Metabolic Disease
|
PPARα/γ agonist 4 (Compound (S)-7) is an orally active dual potent agonist of PPARα and PPARγ, with EC50 values of 0.061 μM and 1.42 μM respectively. PPARα/γ agonist 4 acts through an insulin-independent mechanism and exhibits mitochondrial pyruvate carrier inhibition and anti-diabetic properties. PPARα/γ agonist 4 is expected to be used in research for dyslipidemic type 2 diabetes .
|
-
- HY-N6641
-
|
Keap1-Nrf2
PPAR
|
Inflammation/Immunology
Cancer
|
Monascin is a kind of azaphilonoid pigments extracted from Monascus pilosus-fermented rice (red-mold rice). Monascin also exhibits anti-tumor-initiating activity and anti-inflammatory activity with oral administration. Monascin inhibits the activation of NOR 1 (an NO donor). Monascin is a Nrf2 activator and PPARγ agonist .
|
-
- HY-116699
-
|
PPAR
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
CP-868388 free base is a potent, selective and orally active PPARα agonist with a Ki value of 10.8 nM. CP-868388 free base has little or no affinity for PPARβ (Ki of 3.47 μM) and PPARγ. CP-868388 free base has hypolipidemic and anti-inflammatory actions .
|
-
- HY-15027S1
-
-
- HY-115357
-
|
PPAR
|
Metabolic Disease
|
BMS711939 is a selective agonist for peroxisome proliferator-activated receptor α (PPAR α), with EC50 of 4 nM and 4.5 μM, for human PPARα and human PPARγ. BMS711939 exhibits good pharmacokinetic characters in rats models. BMS711939 increases HDL cholesterol, reduces LDL cholesterol and triglycerides .
|
-
- HY-121900
-
|
PPAR
|
Metabolic Disease
Endocrinology
|
LT175, a dual PPARα/γ ligand, is an orally active partial agonist against PPARγ(hPPARα:EC50=0.22 μm; mPPARα:EC50=0.26 μm; hPPARγ:EC50=0.48 μm). LT175 interacts with PPARγ and affects the recruitment of the coregulators cyclic-AMP response element-binding protein-binding protein and nuclear corepressor 1 (NCoR1). LT175 interacts with PPARγ in a hydrophobic region called “diphenyl pocket”. LT175 has potent insulin-sensitizing effects and reduced adipogenic properties .
|
-
- HY-15027S2
-
Mesalamine-13C6; 5-ASA-13C6; Mesalazine-13C6
|
PPAR
PAK
NF-κB
Endogenous Metabolite
|
Inflammation/Immunology
|
5-Aminosalicylic acid- 13C6 is the 13C labeled 5-Aminosalicylic Acid[1]. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB[2][3][4].
|
-
- HY-128872
-
EHP-101; VCE-004.8
|
PPAR
Cannabinoid Receptor
HIF/HIF Prolyl-Hydroxylase
|
Metabolic Disease
Inflammation/Immunology
|
Etrinabdione (EHP-101; VCE-004.8) is an orally active, specific PPARγ and CB2 receptor dual agonist. Etrinabdione inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. Etrinabdione, a semi-synthetic multitarget cannabinoquinoid, has potent anti-inflammatory activity. Etrinabdione attenuates adipogenesis and prevents diet-induced obesity .
|
-
- HY-128932
-
MT-141
|
Bacterial
PPAR
Prostaglandin Receptor
Antibiotic
|
Infection
Cardiovascular Disease
Endocrinology
|
Cefminox sodium (MT-141) is a semisynthetic cephamycin, which exhibits a broad spectrum of antibacterial activity . Cefminox sodium (MT-141) also acts as a dual agonist of prostacyclin receptor (IP) and PPARγ, upregulates cAMP production and PTEN expression and inhibits Akt/mTOR signaling. Cefminox sodium (MT-141) also prevents pulmonary arterial hypertension .
|
-
- HY-17386S1
-
-
- HY-17386R
-
-
- HY-15027R
-
|
PPAR
PAK
NF-κB
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
5-Aminosalicylic Acid (Standard) is the analytical standard of 5-Aminosalicylic Acid. This product is intended for research and analytical applications. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB. 5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).
|
-
- HY-19425
-
|
PPAR
|
Metabolic Disease
|
NS-220 is an orally active PPARα agonist with high subtype selectivity, with EC50 values of 1.9×10 -8 M, 9.6×10 -6 M and >10 -4 M for PPARα, PPAR γ and PPARδ, respectively. NS-220 is used in the research for hyperlipidemia or metabolic disorders in type-2 diabetes .
|
-
- HY-15027S3
-
Mesalamine-d3 disodium; 5-ASA-d3 disodium; Mesalazine-d3 disodium
|
PPAR
NF-κB
Endogenous Metabolite
PAK
Isotope-Labeled Compounds
|
Inflammation/Immunology
|
5-Aminosalicylic acid-d3 disodium is deuterated labeled 5-Aminosalicylic Acid (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).
|
-
- HY-119311
-
|
Others
|
Metabolic Disease
|
Pioglitazone ketone is an active metabolite of the PPARγ agonist Pioglitazone (HY-13956). Formation of pioglitazone ketone occurs primarly through cytochrome P450 (CYP) isoform CYP2C8-mediated metabolism of pioglitazone. Pioglitazone ketone (100 mg/kg in the diet) reduces blood glucose levels in a KKAy mouse model of type 2 diabetes.
|
-
- HY-W011220
-
ADD-3878; U-63287
|
PPAR
|
Cardiovascular Disease
Cancer
|
Ciglitazone is a potent and selective PPARγ agonist (EC50=3 μM). Ciglitazone inhibits proliferation and differentiation of th17 cells. Ciglitazone is a hypoglycemic agent orally active in the obese-hyperglycemic animal models. Ciglitazone induces apoptosis accompanied by activation of p38 MAPK and nuclear translocation of apoptosis inducing factor (AIF) in opossum kidney (OK) renal epithelial cells .
|
-
- HY-A0087
-
|
Biochemical Assay Reagents
PPAR
Estrogen Receptor/ERR
Cytochrome P450
|
Others
|
Octocrylene is an organic ultraviolet (UV) filter that absorbs mainly UVB radiation and shorter UVA wavelengths. Octocrylene acts as a partial agonist of PPARγ, which alters the gene transcription profile of lipid metabolism enzymes. In addition, Octocrylene is cytotoxic and genotoxic to human skin fibroblasts and mediates the biosynthesis of estrogens such as estriol in zebrafish larvae, while affecting antioxidant pathways including glutathione transferase and peroxisomes .
|
-
- HY-120327
-
KY-226
1 Publications Verification
|
Phosphatase
|
Neurological Disease
Metabolic Disease
|
KY-226 is a potent, selective, orally active and allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 0.25 μM, and without PPARγ agonist activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. KY-226 also protects neurons from cerebral ischemic injury .
|
-
- HY-W010983
-
SC-236
1 Publications Verification
|
COX
PPAR
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
SC-236 is an orally active COX-2 specific inhibitor (IC50 = 10 nM) and a PPARγ agonist. SC-236 suppresses activator protein-1 (AP-1) through c-Jun NH2-terminal kinase. SC-236 exerts anti-inflammatory effects by suppressing phosphorylation of ERK in a murine model .
|
-
- HY-147757
-
|
PPAR
|
Metabolic Disease
|
PPARγ/δ modulator 1 (compound 3e) is a potent PPAR modulator. PPARγ/δ modulator 1 is a PPARδ antagonist and a PPARγ partial agonist , with Ki values of 14.4 nM and 5.31 μM, respectively. PPARγ/δ modulator 1 has the EC50 of 7.3 and 12.6 μM for PPARδ corepression and adiponectin production, respectively .
|
-
- HY-119790
-
|
Others
|
Metabolic Disease
|
Palmitoyllactic acid is a long-chain fatty acid with lipogenic activity. Palmitoyllactic acid can induce a brown fat-like phenotype in 3T3-L1 cells. Palmitoyllactic acid enhances the expression of a variety of brown/beige cell-specific genes, such as Prdm16 and Pgc1a. Palmitoyllactic acid acts similarly to PPARγ agonists, significantly enhancing adipogenesis in the presence of dexamethasone. Palmitoyllactic acid can be used in obesity research .
|
-
- HY-128932R
-
|
Bacterial
PPAR
Prostaglandin Receptor
Antibiotic
|
Infection
Cardiovascular Disease
Endocrinology
|
Cefminox (sodium) (Standard) is the analytical standard of Cefminox (sodium). This product is intended for research and analytical applications. Cefminox sodium (MT-141) is a semisynthetic cephamycin, which exhibits a broad spectrum of antibacterial activity . Cefminox sodium (MT-141) also acts as a dual agonist of prostacyclin receptor (IP) and PPARγ, upregulates cAMP production and PTEN expression and inhibits Akt/mTOR signaling. Cefminox sodium (MT-141) also prevents pulmonary arterial hypertension .
|
-
- HY-N10361
-
|
RAR/RXR
PPAR
|
Cancer
|
Drupanin is an orally active selective AKR1C3 enzyme inhibitor and an RXRα agonist with an EC50 value of 4.8 μM, which is isolated from green propolis. Drupanin also activates PPARγ moderately. Drupanin induces adipogenesis and elevates aP2 mRNA levels in 3T3-L1 fibroblasts Drupanin has the potential for the research of breast and prostate cancers .
|
-
- HY-101676
-
NID 525
|
Leukotriene Receptor
PPAR
Cytochrome P450
|
Metabolic Disease
|
RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 µM.
|
-
- HY-121746
-
|
PPAR
Calcium Channel
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
|
GW7845 is an orally active non-thiazolidinedione, tyrosine-derived PPARγ agonist. GW7845 is effective at inhibiting voltage-dependent calcium channels (VDCC) and relaxing pressurized arteries with IC50 of 3 μM by using Ba 2+ as the charge carrier through VDCC. GW7845-induced apoptosis is mitochondria- and apoptosome-dependent. GW7845 induces rapid mitochondrial membrane depolarization and release of cytochrome c in primary pro-B cells and BU-11 cells .
|
-
- HY-168049
-
|
PPAR
Akt
|
Metabolic Disease
|
ZLY06 is an orally active dual agonist of peroxisome proliferator-activated receptor (PPAR) δ and γ (PPAR δ: EC50=341 nM; PPAR γ: EC50=237 nM). ZLY06 induces hepatic lipid accumulation by inhibiting the phosphorylation of AKT1, mediating the upregulation of CD36. In addition, ZLY06 significantly improves glucose and lipid metabolism without increasing body weight, and alleviates fatty liver by promoting β-oxidation of fatty acids and inhibiting hepatic lipogenesis .
|
-
- HY-162713
-
|
EGFR
PI3K
PPAR
|
Cancer
|
MTX-531 is an oral drug that inhibits EGFR (with an IC50 of 14.7 nM) and PI3K (with IC50 values of 6.4, 233, 8.3, and 1.1 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ respectively), and it has anti-tumor effects. MTX-531 also acts as a weak agonist of PPARγ, with an IC50 of 2.5 µM, helping to alleviate hyperglycemia induced by PI3K inhibitors .
|
-
- HY-15697
-
TUG-770
3 Publications Verification
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
TUG-770 is a potent, selective and orally active GPR40/FFA1 agonist with an EC50 of 6 nM for human FFA1. TUG-770 shows a high selectivity for FFA1 over FFA2, FFA3, FFA4, PPARγ, other receptors, transporters, and enzymes. TUG-770 can be uesd for type 2 diabetes research . TUG-770 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-143704S
-
Mesalamine-13C6 hydrochloride; 5-ASA-13C6 hydrochloride; Mesalazine-13C6 hydrochloride
|
PPAR
NF-κB
PAK
|
Metabolic Disease
|
5-Aminosalicylic acid-13C6 hydrochloride?(Mesalamine-13C6 hydrochloride; 5-ASA-13C6 hydrochloride; Mesalazine-13C6 hydrochloride) is the 13C labeled 5-Aminosalicylic Acidhydrochloride. 5-Aminosalicylic acid-13C6 hydrochloride?acts as a PPARγ agonist, and also inhibits p21-activated kinase 1 (PAK1) and NF-κB .
|
-
- HY-139408
-
17-Oxo-DHA; 17-Oxo-4(Z),7(Z),10(Z),13(Z),15(E),19(Z)-DHA
|
PPAR
Keap1-Nrf2
|
Metabolic Disease
|
17-Oxo-4(Z),7(Z),10(Z),13(Z),15(E),19(Z)-docosahexaenoic acid (17-Oxo-DHA) is a metabolite of lipoxygenase-mediated oxidation of DHA. 17-Oxo-4(Z),7(Z),10(Z),13(Z),15(E),19(Z)-docosahexaenoic acid is a PPARγ agonist and activates a Nrf2 dependent antioxidant reaction .
|
-
- HY-108568
-
15d-PGJ2; 15-Deoxy-Δ12,14-PGJ2
|
PPAR
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
Cancer
|
15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC50 of 2 µM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC50 of 7 μM .
|
-
- HY-148418
-
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) (Free Fatty Acid Receptor) agonist with a pEC50 of 7.39. TUG-499 exhibits >100-fold selectivity over the related receptors FFA2, FFA3, and the nuclear receptor PPARγ and other diverse receptors, ion channels, and transporters. TUG-499 can be used for the research of type 2 diabetes . TUG-499 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-108568S
-
15d-PGJ2-d4; 15-Deoxy-Δ12,14-PGJ2-d4
|
PPAR
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
Cancer
|
15-Deoxy-Δ-12,14-prostaglandin J2-d4 is the deuterium labeled 15-Deoxy-Δ-12,14-prostaglandin J2. 15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC50 of 2 µM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC50 of 7 μM[1][2].
|
-
- HY-108568R
-
|
PPAR
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
Cancer
|
15-Deoxy-Δ-12,14-prostaglandin J2 (Standard) is the analytical standard of 15-Deoxy-Δ-12,14-prostaglandin J2. This product is intended for research and analytical applications. 15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC50 of 2 μM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC50 of 7 μM .
|
-
- HY-116028
-
15-Deoxy-Δ12,14-PGD2
|
Endogenous Metabolite
|
Cardiovascular Disease
|
15-deoxy-Δ12,14-PGD2 is a metabolite of PGD2. It is an agonist of PGD2 receptor 2 (DP2) that binds DP2 (Ki=50 nM for the mouse receptor expressed in HEK293 cell membranes) and induces activation of eosinophils (EC50=8 nM). It also stimulates the recruitment of steroid receptor coactivator-1 (SRC-1) to peroxisome proliferator-activated receptor γ (PPARγ) and induces PPARγ-mediated transcription in a reporter assay when used at a concentration of 5 μM.1 15-deoxy-Δ12,14-PGD2 is cytotoxic to L1210 murine leukemia cells (IC50=0.3 μg/mL). It inhibits ADP-induced platelet aggregation (IC50=320 ng/ml) less potently than PGD2.
|
-
- HY-116115
-
17-Oxo-DPA; 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-DPA
|
NF-κB
PPAR
|
Inflammation/Immunology
|
17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid (17-Oxo-DPA; 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-DPA) is an electrophilic oxo-derivative (EFOX) of the docosahexaenoic acid (DHA) (HY-B2167). 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid is generated during inflammation by COX-2-catalyzed mechanism in activated macrophages. 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid acts as an agonist for PPARγ and a modulator for NF-κB signaling pathway, inhibits the production of pro-inflammatory cytokines and nitric oxide, and exhibits anti-inflammatory efficacy .
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-
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N0246
-
-
-
- HY-N6869
-
-
-
- HY-N2025
-
-
-
- HY-N0234
-
-
-
- HY-N0246R
-
-
-
- HY-N6869R
-
|
Structural Classification
Microorganisms
other families
Terpenoids
Source classification
Diterpenoids
Plants
|
Antibiotic
PPAR
Bacterial
Fungal
|
Dehydroabietic acid (Standard) is the analytical standard of Dehydroabietic acid. This product is intended for research and analytical applications. Dehydroabietic acid is a diterpene resin acid that can be isolated from Pinus and Picea. Dehydroabietic acid has anti-bacterial, anti-fungal, anti-inflammatory, and anticancer activities. Dehydroabietic acid is a dual PPAR-α/γ agonist and PPAR-γ partial agonist, which can attenuate insulin resistance (IR) and hepatic steatosis induced by HFD-consumption in mice .
|
-
-
- HY-N9333
-
-
-
- HY-13956R
-
|
Human Gut Microbiota Metabolites
Source classification
Endogenous metabolite
|
PPAR
Ferroptosis
|
Pioglitazone (Standard) is the analytical standard of Pioglitazone. This product is intended for research and analytical applications. Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research .
|
-
-
- HY-N2025R
-
|
Structural Classification
Flavonoids
Flavones
Source classification
Bignoniaceae
Plants
Oroxylum indicum (Linn.) Bentham ex Kurz
|
PPAR
Glucosidase
|
Oroxin A (Standard) is the analytical standard of Oroxin A. This product is intended for research and analytical applications. Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .
|
-
-
- HY-N0234R
-
-
-
- HY-U00450
-
-
-
- HY-N7624
-
-
-
- HY-N0163
-
-
-
- HY-113631
-
-
-
- HY-15027
-
-
-
- HY-N7687
-
-
-
- HY-111616
-
-
-
- HY-N6642
-
-
-
- HY-N0163R
-
-
-
- HY-N6641
-
-
-
- HY-15027R
-
-
-
- HY-N10361
-
-
-
- HY-108568
-
-
-
- HY-108568R
-
|
Structural Classification
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
|
PPAR
Endogenous Metabolite
|
15-Deoxy-Δ-12,14-prostaglandin J2 (Standard) is the analytical standard of 15-Deoxy-Δ-12,14-prostaglandin J2. This product is intended for research and analytical applications. 15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC50 of 2 μM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC50 of 7 μM .
|
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-13956S
-
|
Pioglitazone-d4 is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1].
|
-
-
- HY-13956S1
-
|
Pioglitazone-d4 (alkyl) (U 72107-d4 (alkyl)) is the deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1][2].
|
-
-
- HY-B0637S
-
|
Bezafibrate-d6 is the deuterium labeled Bezafibrate. Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.
|
-
-
- HY-15027S
-
|
5-Aminosalicylic Acid-d3 (hydrochloride) is the deuterium labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) hydrochloride acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
|
-
-
- HY-50935S
-
|
Troglitazone-d4 is deuterium labeled Troglitazone. Troglitazone is a PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively.
|
-
-
- HY-B0287S
-
|
Clofibrate-d4 is the deuterium labeled Clofibrate. Clofibrate is an agonist of PPAR, with EC50s of 50 μM, ∼500 μM for murine PPARα and PPARγ, and 55 μM, ∼500 μM for human PPARα and PPARγ, respectively.
|
-
-
- HY-117727S
-
|
Leriglitazone-d4 (MIN-102-d4; Hydroxypioglitazone-d4) is deuterium labeled Leriglitazone. Leriglitazone (Hydroxypioglitazone), a metabolite of pioglitazone.Leriglitazone (Hydroxypioglitazone) PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy.Leriglitazone (Hydroxypioglitazone) binds to the PPARγ C-terminal ligand-binding domain (LBD) with Ki of 1.2 μM,induces transcriptional efficacy of the PPARγ (LBD) with EC50 of 680 nM .
|
-
-
- HY-17386S
-
|
Rosiglitazone-d3 is the deuterium labeled Rosiglitazone. Rosiglitazone (BRL 49653) is a selective, orally active PPARγ agonist with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively. Rosiglitazone binds to PPARγ with a Kd of approximately 40 nM. Rosiglitazone is also an activator of TRPC5 (EC50=~30 μM) and an inhibitor of TRPM3[1][2][3][4].
|
-
-
- HY-B0637S1
-
|
Bezafibrate-d4 is deuterium labeled Bezafibrate. Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.
|
-
-
- HY-19937S1
-
|
Saroglitazar-d4 is the deuterium-labeled Saroglitazar (HY-19937). Saroglitazar-d4 is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
|
-
-
- HY-15027S1
-
|
5-Aminosalicylic acid-d3 is the deuterium labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB[1][2][3][4].
|
-
-
- HY-15027S2
-
|
5-Aminosalicylic acid- 13C6 is the 13C labeled 5-Aminosalicylic Acid[1]. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB[2][3][4].
|
-
-
- HY-17386S1
-
|
Rosiglitazone-d4 is deuterated labeled Rosiglitazone (HY-17386). Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone is an TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer .
|
-
-
- HY-15027S3
-
|
5-Aminosalicylic acid-d3 disodium is deuterated labeled 5-Aminosalicylic Acid (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).
|
-
-
- HY-143704S
-
|
5-Aminosalicylic acid-13C6 hydrochloride?(Mesalamine-13C6 hydrochloride; 5-ASA-13C6 hydrochloride; Mesalazine-13C6 hydrochloride) is the 13C labeled 5-Aminosalicylic Acidhydrochloride. 5-Aminosalicylic acid-13C6 hydrochloride?acts as a PPARγ agonist, and also inhibits p21-activated kinase 1 (PAK1) and NF-κB .
|
-
-
- HY-108568S
-
|
15-Deoxy-Δ-12,14-prostaglandin J2-d4 is the deuterium labeled 15-Deoxy-Δ-12,14-prostaglandin J2. 15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC50 of 2 µM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC50 of 7 μM[1][2].
|
-
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