PPAR

シグナル伝達経路

研究分野

  • 阻害剤の選択性比較
  • 溶解度
カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S2505 Rosiglitazone maleate <1 mg/mL 94 mg/mL <1 mg/mL
S2556 Rosiglitazone <1 mg/mL 71 mg/mL <1 mg/mL
S2915 GW9662 <1 mg/mL 55 mg/mL <1 mg/mL
S2871 T0070907 <1 mg/mL 26 mg/mL <1 mg/mL
S2590 Pioglitazone <1 mg/mL 10 mg/mL <1 mg/mL
S5615 GW501516 -1 mg/mL 90 mg/mL -1 mg/mL
S3868 Harmine -1 mg/mL 42 mg/mL -1 mg/mL
S3878 Bavachinin -1 mg/mL 67 mg/mL -1 mg/mL
S3786 Glabridin -1 mg/mL 64 mg/mL -1 mg/mL
S3720 Elafibranor <1 mg/mL 76 mg/mL 76 mg/mL
S8029 WY-14643 (Pirinixic Acid) <1 mg/mL 64 mg/mL 52 mg/mL
S8025 GSK3787 <1 mg/mL 79 mg/mL <1 mg/mL
S8020 GW0742 <1 mg/mL 94 mg/mL 44 mg/mL
S1729 Gemfibrozil <1 mg/mL 50 mg/mL 50 mg/mL
S2665 Ciprofibrate <1 mg/mL 58 mg/mL 58 mg/mL
S4159 Bezafibrate <1 mg/mL 72 mg/mL 18 mg/mL
S4207 Clofibric Acid <1 mg/mL 43 mg/mL 43 mg/mL
S1794 Fenofibrate <1 mg/mL 72 mg/mL 46 mg/mL
S2075 Rosiglitazone HCl <1 mg/mL 79 mg/mL 79 mg/mL
S7767 AZ6102 <1 mg/mL 85 mg/mL <1 mg/mL
S8432 Troglitazone (CS-045) <1 mg/mL 88 mg/mL 15 mg/mL
S7484 FH535 <1 mg/mL 72 mg/mL <1 mg/mL
S4527 Fenofibric acid 63 mg/mL 63 mg/mL 63 mg/mL
S4708 Palmitoylethanolamide <1 mg/mL 59 mg/mL 59 mg/mL

亜型選択性的な製品

製品コード 製品説明 文献中の使用例 お客様のフィードバック
S2505

Rosiglitazone maleate

Rosiglitazone, a member of the thiazolidinedione class of antihyperglycaemic agents, is a high-affinity selective agonist of the peroxisome proliferator-activated receptor-γ with IC50 of 42 nM.

S2556

Rosiglitazone

Rosiglitazone is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-alpha-binding action.

S2915

GW9662

GW9662 is a selective PPAR antagonist for PPARγ with IC50 of 3.3 nM in a cell-free assay, with at least 10- to 600-fold functional selectivity in cells with PPARγ versus PPARα and PPARδ.

S2871

T0070907

T0070907 is a potent and selective PPARγ inhibitor with IC50 of 1 nM in a cell-free assay, with a >800-fold selectivity over PPARα and PPARδ.

S2590

Pioglitazone

Pioglitazone is a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist, used to treat diabetes; A weak activator for full-length hPPARα, but not full-length hPPARδ.

S5615

GW501516

S3868

Harmine

Harmine is an alkaloid of the β-carboline family that regulates PPARγ expression through inhibition of the Wnt signaling pathway. It also selectively binds to MAO-A and reversibly inhibits monoamine oxidase A (MAO-A) but not the variant MAO-B.

S3878

Bavachinin

Bavachinin is a novel natural pan-PPAR agonist from the fruit of the traditional Chinese glucose-lowering herb malaytea scurfpea. It shows stronger activities with PPAR-γ than with PPAR-α and PPAR-β/δ (EC50 = 0.74 μmol/l, 4.00 μmol/l and 8.07 μmol/l in 293T cells, respectively).

S3786

Glabridin

Glabridin, one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory.

S5121

Phytol

Phytol, a diterpene alcohol from chlorophyll widely used as a food additive and in medicinal fields, shows antinociceptive and antioxidant activities as well as anti-inflammatory and antiallergic effects. It is a specific activator of PPARα.

S3720

Elafibranor

Elafibranor is an agonist of the peroxisome proliferator-activated receptor-α(PPAR-alpha) and peroxisome proliferator-activated receptor-δ(PPAR-δ). It improves insulin sensitivity, glucose homeostasis, and lipid metabolism and reduces inflammation.

S8029

WY-14643 (Pirinixic Acid)

WY 14643 (Pirinixic Acid) is a potent peroxisome proliferator and activator of PPARα with EC50 of 1.5 μM.

S8025

GSK3787

GSK3787 is as a selective and irreversible antagonist of PPARδ with pIC50 of 6.6, with no measurable affinity for hPPARα or hPPARγ.

S8020

GW0742

GW0742 is a potent and highly selective PPARβ/δ agonist, with IC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ.

S1729

Gemfibrozil

Gemfibrozil is an activator of peroxisome proliferator-activated receptor-alpha (PPARα), used for the treatment of hypercholesterolemia and hypertriglyceridemia.

S2665

Ciprofibrate

Ciprofibrate is a peroxisome proliferator-activated receptor agonist.

S4159

Bezafibrate

Bezafibrate is the first clinically tested dual and pan-PPAR co-agonism.

S4207

Clofibric Acid

Clofibric acid is a PPARα agonist and hypolipidemic agent.

S1794

Fenofibrate

Fenofibrate (Tricor, Trilipix) is a compound of the fibrate class and fibric acid derivative.

S2075

Rosiglitazone HCl

Rosiglitazone HCl is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.

S7767

AZ6102

AZ6102 is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows IC50 of 5 nM for Wnt pathway inhibition in DLD-1 cells.

S8432

Troglitazone (CS-045)

Troglitazone is a potent agonist for the peroxisome proliferator-activated receptor-(PPAR) that is a ligand activated transcription factor regulating cell differentiation and growth.

S7484

FH535

FH535 is a Wnt/β-catenin signaling inhibitor and also a dual PPARγ and PPARδ antagonist.

S4527

Fenofibric acid

Fenofibric acid is a fibrate that acts as a lipid-lowering agent, decreasing low-density lipoprotein cholesterol and triglycerides.

S4708

Palmitoylethanolamide

Palmitoylethanolamide(PEA) is an endogenous fatty acid amide and selectively activates PPAR-α in vitro with an EC50 value of 3.1±0.4 μM.