|Description||In vitro, the IC50 for growth inhibition is approximately 0.8 nM while anaplastic thyroid carcinoma (ATC) tumor growth was inhibited three- to fourfold in nude mice. siRNA against PPARgamma and a pharmacological antagonist demonstrated that functional PPARgamma was required for growth inhibitory activity of RS5444. RS5444 upregulated the cell cycle kinase inhibitor, p21WAF1/CIP1. RS5444inhibited culture growth and caused irreversible G1 arrest, but did not induce apoptosis. In addition, RS5444 caused dramatic changes in cellular morphology which were associated with increased motility and diminished cellular adherence, but no increase in the ability of such cells to digest and invade Matrigel. Treatment with RS5444 leads to the up-regulation of RhoB and subsequent activation of p21, and that silencing of RhoB by RNAi blocks the ability of RS5444 to induce p21 and to inhibit ATC cells proliferation. The median peak efatutazone blood level was 8.6 ng/mL for 0.15-mg dosing vs 22.0 ng/mL for 0.3-mg twice daily dosing. Although efatutazone treatment did not reduce percentage of mice developing invasive cancer, it significantly reduced prevalence of noninvasive cancer and total number of cancers per mouse and increased prevalence of well-differentiated cancer subtypes not usually seen in this mouse model.|
|Synonyms||Efatutazone; CS-7017; RS5444; CS 7017; RS 5444|
Naveglitazar is a Dual peroxisome proliferator-activated receptor gamma and alpha (PPARgamma and PPARalpha) agonist
Rosiglitazone exhibits insulin-sensitising activity 60- to 200-fold higher than that of troglitazone, englitazone, or piogliazone in rodent models of insulin re...
CS-7017 monohydrate is a peroxisome proliferator activated receptor gamma (PPAR) agonist. It is a potential therapy for thyroid cancer and liposarcoma. It is al...
The Rs for the separations were 3.5 for balaglitazone enantiomers, 3.5 for pioglitazone enantiomers, and 3.7 for rosiglitazone. The squared correlation coeffici...
LY518674, a phenoxypropionic acid derivative, is a Potent and selective PPAR-alpha agonist produced a dose-dependent increase in serum HDL-c, resulting in 208 +...
L-165041 is a cell permeable PPARδ agonist which induces adipocyte differentiation in NIH-PPARδ cells. It displays more than 100-fold selectivity for both mouse...
PPAR agonist 1
An agonist of PPAR α and PPAR γ
MCC-555, a thiazolidinedion derivative, has been found to be a PPAR agonist that was once studied as hyperglycaemic and hyperlipidaemic. The Phase II trial agai...
GW-9820 is a PPAR-gamma agonist with potential antidiabetic effect.
Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity as a drug for the treatment...
BMS-687453 is a potent and selective peroxisome proliferator activated receptor PPARα agonist. with an IC50 of 10 nM for human PPARalpha and approximately 410-f...
GW0742 is a potent and highly selective PPARβ/δ agonist, with IC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ.
PT-S58 is a full peroxisome proliferator-activated receptor (PPAR) β/δ antagonist as a derivative of GSK0660. But PT-S58 has a three-fold higher affinity for th...
Bezafibrate (marketed as Bezalip and various other brand names) is a fibrate drug used for the treatment of hyperlipidaemia. It helps to lower LDL cholesterol a...
Protopanaxatriol is a dammarane-type tetracyclic triterpene sapogenins found in ginseng (Panax ginseng) and in notoginseng (Panax pseudoginseng). It may have a ...
Seladelpar is a selective peroxisome proliferator-activated receptor -δ receptor agonist. Phase II clinical trials for the treatment of Hyperlipidaemia, Hyperli...
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 adipoc...
Arhalofenateis, also known as JNJ-39659100 and MBX102, as an uricosuric agent it is a selective, partial PPAR-γ agonist.
Pioglitazone HCl is a hydrochloride salt form of pioglitazone which is a cytochrome P450 (CYP)2C8 and CYP3A4 enzymes inhibitor for CYP2C8, CYP3A4 and CYP2C9 wit...
T0070907 was identified as a potent and selective PPARgamma antagonist. T0070907 blocked PPARgamma function in both cell-based reporter gene and adipocyte diffe...