Product Description
Size: 10mg / 50mg
MW 502.8 Da, Purity >99%. Highly potent, selective PPARα agonist (EC 50 values are 6, 1100 and 6200 nM for PPARα, PPARγ and PPARδ respectively). Pharmacologically active in vivo .
Key facts
CAS number:265129-71-3,
Purity:>99%,
Form:SolidSee storage information,
Molecular weight:502.8 Da,
Molecular formula:C29H46N2O3S,
PubChem:3392731,
Nature:Synthetic,
Solubility:Soluble in DMSO to 25 mMSoluble in ethanol to 100 mM,
Biochemical name:2-[(4-{2-[(4-Cyclohexylbutyl)(cyclohexylcarbamoyl)amino]ethyl}phenyl)sulfanyl]-2-methylpropanoic acid,
Biological description:Highly potent, selective PPARα agonist (EC50 values are 6, 1100 and 6200 nM for PPARα, PPARγ and PPARδ respectively). Pharmacologically active in vivo.,
Canonical smiles:CC(C)(C(=O)O)SC1=CC=C(C=C1)CCN(CCCCC2CCCCC2)C(=O)NC3CCCCC3,
InChi:InChI=1S/C29H46N2O3S/c1-29(2,27(32)33)35-26-18-16-24(17-19-26)20-22-31(28(34)30-25-14-7-4-8-15-25)21-10-9-13-23-11-5-3-6-12-23/h16-19,23,25H,3-15,20-22H2,1-2H3,(H,30,34)(H,32,33),
InChiKey:PKNYXWMTHFMHKD-UHFFFAOYSA-N,
IUPAC Name:2-[4-[2-[4-cyclohexylbutyl(cyclohexylcarbamoyl)amino]ethyl]phenyl]sulfanyl-2-methylpropanoic acid
Properties and Storage Information:
Shipped at conditions-Ambient - Can Ship with Ice, Appropriate short-term storage conditions-Ambient, Appropriate long-term storage conditions-Ambient, Storage information-The product can be stored for up to 12 months
Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
The Glucocorticoid Receptor also known as GR is a nuclear receptor that functions mechanically by binding glucocorticoid hormones thereby mediating numerous biological responses. Its molecular weight is about 86 kDa. GR is expressed widely throughout the body with significant presence in tissues like the liver lung muscle and immune cells. Like GR the Estrogen Receptor (ER) also binds hormones primarily estrogens and it plays an integral role in the regulation of gene expression. DNA Polymerase iota and DNA Polymerase Kappan important DNA repair enzymes have vital roles in maintaining the integrity of the genome. Meanwhile PPAR alpha and PPAR gamma 2 are vital for regulating lipid metabolism and are predominantly found in liver adipose tissue and muscle. CYP3A4 a member of the cytochrome P450 family participates in drug metabolism and is highly expressed in the liver. Geminin regulates DNA replication and CBX1 also known as HP1 beta plays an important role in chromatin architecture. BAZ2B and MPP8 are involved in the regulation of gene expression while the Dopamine Receptor D1 is important for dopaminergic signaling within the central nervous system.
Biological function summary
These proteins undertake several functional roles in specific cell types and contexts. The Glucocorticoid Receptor and Estrogen Receptor as nuclear hormone receptors form complexes with co-activators or co-repressors to regulate transcription. DNA Polymerases iota Kappa and eta are important for bypassing DNA lesions during replication contributing to DNA damage tolerance. PPAR alpha and PPAR gamma 2 through their action as transcription factors regulate genes associated with fatty acid oxidation and adipogenesis. Cytochrome P450 3A4 through its enzymatic capacity metabolizes xenobiotics and endogenous substrates. Proteins such as CBX1 and BAZ2B are involved in chromatin remodeling influencing gene expression profiles while the Retinoid X Receptor alpha serves as a partner for many nuclear receptors broadening their regulatory capacity.
Pathways
The involvement of these proteins in different biological processes is vast. The Glucocorticoid Receptor and Estrogen Receptor play essential roles in the steroid hormone signaling pathways affecting development metabolism and immune responses. DNA Polymerases including iota Kappa and eta play a part in the DNA repair pathways like translesion synthesis closely associated with maintaining genomic stability. PPAR alpha and gamma 2 activate pathways governing lipid metabolism impacting insulin signaling and energy homeostasis. CYP3A4 is an important player in the drug metabolism pathway impacting the efficacy and clearance of therapeutics. Additionally the Dopamine Receptor D1 is active in dopaminergic pathways that influence many neurological processes.
These proteins have implications in multiple conditions. Dysfunctional Glucocorticoid Receptor signaling is linked to Cushing's syndrome and its downstream targets can contribute to metabolic syndrome-related pathologies. Estrogen Receptor anomalies are important in breast cancer development. CYP3A4 mutations can lead to variable drug responses and side effects. Dysregulation in CBX1 and BAZ2B can contribute to cancer progression whereas alterations in PPAR pathways are linked to inflammatory diseases such as atherosclerosis. The Dopamine Receptor D1 plays a significant role in neurological disorders notably in Parkinson's disease where the dopaminergic signaling is disrupted. Understanding the interaction of these proteins within disease contexts enhances our potential to develop targeted therapies.
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Collaboration
Tony Tang
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