Product Details
Product Name:
CPPHA |
CAS No.:
693288-97-0 |
Purity:
99.61% |
Supply Ability:
10g |
Release date:
2024/11/19 |
Product Introduction
Bioactivity
Name | CPPHA |
Description | CPPHA, a positive allosteric modulator of glutamate receptors mGluR5 and mGluR1, is commonly used in development for central nervous system diseases. |
Cell Research | CPPHA potentiated the response to a subthreshold concentration of 3,5-dihydroxy-phenylglycine (DHPG) on extracellular signal-regulated protein kinase (ERK) and cyclic-AMP responsive element-binding protein (CREB) activity, as well as N-methyl d-aspartate (NMDA) receptor subunit NR1 phosphorylation in cortical and hippocampal slices [1]. CPPHA potentiated threshold responses to glutamate in fluorometric Ca(2+) assays 7- to 8-fold (EC50s: 400 to 800 nM), and at 10 μM shifted mGluR5 agonist concentration-response curves to glutamate, quisqualate, and DHPG 4- to 7-fold to the left. CPPHA (10 μM) potentiated NMDA receptor currents in hippocampal slices induced by threshold levels of DHPG, whereas having no effect on these currents by itself. Similarly, 10 μM CPPHA also potentiated mGluR5-mediated DHPG-induced depolarization of rat subthalamic nucleus neurons [2]. CPPHA induced an increase in basal mGluR5-mediated ERK1/2 phosphorylation and potentiated the effect of low concentrations of agonists. In contrast, CPPHA significantly decreased ERK1/2 phosphorylation induced by high concentrations of agonists [3]. |
In vitro | CPPHA potentiated the response to a subthreshold concentration of 3,5-dihydroxy-phenylglycine (DHPG) on extracellular signal-regulated protein kinase (ERK) and cyclic-AMP responsive element-binding protein (CREB) activity, as well as N-methyl d-aspartate (NMDA) receptor subunit NR1 phosphorylation in cortical and hippocampal slices [1]. CPPHA potentiated threshold responses to glutamate in fluorometric Ca(2+) assays 7- to 8-fold (EC50s: 400 to 800 nM), and at 10 μM shifted mGluR5 agonist concentration-response curves to glutamate, quisqualate, and DHPG 4- to 7-fold to the left. CPPHA (10 μM) potentiated NMDA receptor currents in hippocampal slices induced by threshold levels of DHPG, whereas having no effect on these currents by itself. Similarly, 10 μM CPPHA also potentiated mGluR5-mediated DHPG-induced depolarization of rat subthalamic nucleus neurons [2]. CPPHA induced an increase in basal mGluR5-mediated ERK1/2 phosphorylation and potentiated the effect of low concentrations of agonists. In contrast, CPPHA significantly decreased ERK1/2 phosphorylation induced by high concentrations of agonists [3]. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 90.0 mg/mL (221.2 mM), Sonication is recommended.
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Keywords | CPPHA |
Inhibitors Related | IDRA-21 | Topiramate | Decanoic Acid | Urethane | L-Cysteic acid monohydrate | Evans blue | L-Glutamine | Direct Blue 1 | L-Glutamic acid monosodium salt | Piracetam | O-Phospho-L-serine | Memantine hydrochloride |
Related Compound Libraries | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
Product name |
Price |
|
Suppliers |
Update time |
|
$33.00/5mg |
VIP3Y
|
TargetMol Chemicals Inc.
|
2024-11-19 |