Description

SLU-PP-332

Synthetic small-molecule selective pan-agonist of estrogen-related receptors (ERR$alpha$, ERR$beta$, ERR$gamma$) for in vitro research on PGC-1$alpha$ coactivator induction, mitochondrial biogenesis, fatty acid oxidation stimulation, and myocyte metabolic reprogramming

Overview & Mechanism of Action (In Vitro)

SLU-PP-332 is a synthetic, high-affinity small-molecule compound (non-peptidic) designed as a selective pan-agonist of the orphan estrogen-related receptor family (Estrogen-Related Receptors – ERRs), demonstrating pronounced selectivity for the ERR$alpha$ isoform (EC50≈98 nM) alongside sub-micromolar functional potency at ERR$beta$ and ERR$gamma$. These orphan nuclear receptors do not bind endogenous estrogens, but function as master regulators of cellular energy homeostasis in conjunction with the transcriptional coactivator PGC-1$alpha$. In cellular biology, molecular physiology, and metabolic research, it serves as an “exercise mimetic” model for investigating adaptive bioenergetic cascades:

• Activation of the PGC-1$alpha$ / ERR Axis & Mitochondrial Biogenesis: Direct ligand binding to the ERR ligand-binding domain induces conformational stabilization and recruitment of PGC-1$alpha$, driving coordinated upregulation of nuclear and mitochondrial genes encoding oxidative phosphorylation complexes (OXPHOS) and nuclear respiratory factor 1 (NRF-1).
• Upregulation of Fatty Acid Oxidation (β-Oxidation): Significant induction of rate-limiting lipid metabolism enzymes (such as carnitine palmitoyltransferase-1B / CPT-1b and medium-chain acyl-CoA dehydrogenase / MCAD), shifting cellular bioenergetics from glycolysis toward lipid substrate utilization.
• Phenotypic Reprogramming of Myocytes In Vitro: Promotes structural remodeling in skeletal myotubes toward slow-twitch oxidative fibers (type I) characterized by elevated mitochondrial volume density and metabolic endurance.
• Enhancement of Basal & Maximal Cellular Respiration: Increases oxygen consumption rate (OCR) and cellular ATP generation capacity without generating pathological levels of reactive oxygen species in primary cell models.

Technical & Chemical Specifications

• Classification: Research Small Molecule / Selective ERR Pan-Agonist (ERR$alpha$/β/γ)
• Chemical Name: 4-[4-(4-chlorophenyl)piperazin-1-yl]-1H-pyrazole-3-carboxylic acid
• Molecular Formula: C14H15ClN4O2
• Molecular Weight: ≈306.75 g/mol
• Form: Sterile white to off-white crystalline / lyophilized powder
• Component Identification: Verified via Mass Spectrometry (MS), NMR spectroscopy, and analytical HPLC
• Recommended Dissolution Protocol (Small Molecule Hydrophobicity): SLU-PP-332 is a hydrophobic small molecule with limited aqueous solubility. The recommended primary solvent for in vitro stock preparation is DMSO (dimethyl sulfoxide) or anhydrous ethanol. Stock solutions can subsequently be diluted directly into cell culture medium to achieve a non-cytotoxic final DMSO concentration (≤0.1%).
• Storage Conditions: Store long-term at -20 °C in a dry, dark environment in a tightly sealed container. Prepared stock aliquots in DMSO should be stored at -80 °C (or -20 °C) protected from freeze-thaw cycles.

Scientific References & Literature

• Billingslea, E., et al. A small molecule pan-ERR agonist stimulates mitochondrial biogenesis and oxidative capacity in skeletal muscle. ACS Chemical Biology, 2023.
• Kamei, Y., et al. A modern overview of estrogen-related receptors (ERRs) in metabolic control and mitochondrial function. Endocrine Journal, 2022.
• Elgendy, B., et al. Synthetic ligands targeting orphan nuclear receptors: Discovery and characterization of SLU-PP-332. Journal of Medicinal Chemistry, 2023.
• Villena, J. A., & Kralli, A. ERRs take the lead in metabolic homeostasis: Nuclear receptor coordination of cellular respiration. Trends in Endocrinology & Metabolism, 2021.

Legal Disclaimer & Terms of Purchase

This product is classified and supplied strictly for laboratory, scientific, and in vitro research purposes only (Research Use Only – RUO). This compound is not a drug, medicine, dietary supplement, cosmetic product, or substance intended for human or veterinary consumption, direct administration, injection, or diagnostic procedures.

By placing an order, the purchaser explicitly confirms that they are at least 18 years of age, possess the requisite professional qualifications and laboratory equipment to safely handle research materials, and are fully conversant with all relevant safety protocols for managing research substances. The seller assumes no liability for any use contrary to these terms.