| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
CHPG sodium salt targets the metabotropic glutamate receptor subtype 5 (mGluR5), a group I metabotropic glutamate receptor. mGluR5 is a G protein-coupled receptor that is coupled to the Gq family of G proteins. Upon activation by glutamate or selective agonists such as CHPG, mGluR5 stimulates phospholipase C, leading to the production of inositol trisphosphate (IP3) and diacylglycerol (DAG), which mobilizes intracellular calcium and activates protein kinase C. mGluR5 is highly expressed in the central nervous system, particularly in the hippocampus, cortex, and striatum, where it plays critical roles in synaptic plasticity, learning, and memory. mGluR5 has also been implicated in neurodegenerative diseases, pain, and drug addiction. By selectively activating mGluR5, CHPG sodium salt is a valuable tool for studying the functions of this receptor.
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| ln Vitro |
After SO2 model treatment, CHPG sodium salt (10-500 μM; 24 hours) dramatically enhanced cell survival and reduced LDH release [1]. CHPG sodium salt (0.5 mM; 30 minutes) protects the BV2 cell scaffold SO2 cell model. Treatment with CHPG sodium salt (0.5 mM; 30 minutes) alone increases the expression of TSG-6 at the mRNA and protein levels [1].
CHPG sodium salt demonstrates potent in vitro activity as a selective mGluR5 agonist. The compound activates mGluR5 and stimulates downstream signaling pathways including ERK and Akt. In BV2 microglial cells, CHPG sodium salt attenuates SO2-induced oxidative stress and inflammation through the TSG-6/NF-kappaB pathway. The compound's activity has been characterized in various cell-based systems. CHPG sodium salt is widely used in neuroscience research to study mGluR5 function. Its selectivity for mGluR5 over other mGluR subtypes makes it a valuable pharmacological tool. The compound's effects are concentration-dependent, with activity observed at micromolar concentrations. |
| ln Vivo |
In vivo, CHPG sodium salt has been studied for its effects on mGluR5-mediated behaviors and neuroprotection. As a mGluR5 agonist, the compound has been investigated for its potential in treating neurodegenerative diseases, psychiatric disorders, and pain. In preclinical studies, mGluR5 agonists have demonstrated effects on learning, memory, anxiety, and pain perception. CHPG sodium salt has also been studied for its neuroprotective effects, including attenuation of oxidative stress and inflammation. The compound's ability to activate ERK and Akt signaling pathways may contribute to its neuroprotective effects. Comprehensive in vivo efficacy data for CHPG sodium salt have been reported in the literature.
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| Enzyme Assay |
In vitro receptor binding assays for CHPG sodium salt are not standard, as the compound is a receptor agonist rather than an antagonist or enzyme inhibitor. However, functional assays can be performed to measure receptor activation. Cells expressing mGluR5 are loaded with a calcium-sensitive fluorescent dye and treated with varying concentrations of CHPG sodium salt. The increase in intracellular calcium is measured using a fluorescence plate reader. EC50 values are calculated from dose-response curves using non-linear regression analysis. Alternatively, inositol phosphate accumulation assays can be performed using [3H]-myo-inositol-labeled cells. Selectivity assays compare the compound's activity against other mGluR subtypes. The assay is performed in appropriate buffer conditions with controls for non-specific signaling.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: BV2 microglial cells Tested Concentrations: 10, 50, 100 and 500 µM Incubation Duration: 24 hrs (hours) Experimental Results: Increased cell viability. Apoptosis analysis[1] Cell Types: BV2 microglia Tested Concentrations: 0.5 mM Incubation Duration: 30 minutes Experimental Results: Protection of BV2 cells from SO2-induced apoptosis. Western Blot Analysis[1] Cell Types: BV2 Microglia Tested Concentrations: 0.5 mM Incubation Duration: 30 minutes Experimental Results: TSG-6 mRNA and protein level expression increased. In vitro cellular assays for CHPG sodium salt are performed using cells expressing mGluR5 or primary neuronal cultures. Commonly used cell lines include HEK293 or CHO cells stably expressing human mGluR5. Cells are treated with varying concentrations of CHPG sodium salt, and receptor activation is measured by calcium mobilization using fluorescent calcium indicators such as Fluo-4 or Fura-2. Alternatively, inositol phosphate accumulation can be measured using [3H]-myo-inositol-labeled cells. In BV2 microglial cells, the compound's effects on oxidative stress and inflammation can be assessed by measuring ROS production, inflammatory cytokine levels (TNF-alpha, IL-1beta), and NF-kappaB activation. Cell viability is assessed using standard assays such as MTT to ensure that observed effects are not due to cytotoxicity. EC50 values are calculated from dose-response curves. |
| Animal Protocol |
Animal/Disease Models: Adult SD (SD (Sprague-Dawley)) male rats, body weight 280-320 g[2]
Doses: 250 nM Route of Administration: injection; CHPG sodium salt (injection; 250 nM; 7 days) Dramatically reduces the volume of brain damage[2 ]. Results for 7 days: The size of the brain lesions was Dramatically diminished. In vivo animal studies for CHPG sodium salt are conducted using rodent models. The compound is administered via intraperitoneal injection, subcutaneous injection, or intracerebroventricular injection. Behavioral tests are used to assess the compound's effects on mGluR5-mediated behaviors, including tests of learning and memory (Morris water maze, novel object recognition), anxiety (elevated plus maze), and pain (formalin test, von Frey test). In models of neurodegenerative disease, the compound's neuroprotective effects can be assessed by measuring neuronal survival, oxidative stress markers, and inflammatory markers. Pharmacokinetic studies assess drug concentrations in plasma and brain tissue. Animals are monitored for clinical signs and body weight. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of CHPG sodium salt have been characterized in preclinical studies. The compound has a molecular formula of C8H7ClNNaO3 and a molecular weight of 223.59 g/mol. Its chemical name is sodium 2-amino-2-(2-chloro-5-hydroxyphenyl)acetate. CHPG sodium salt is soluble in water and DMSO. The compound is typically administered by injection due to its polarity. Comprehensive pharmacokinetic parameters including half-life, volume of distribution, clearance, and bioavailability have been characterized in animal models. The compound's ability to cross the blood-brain barrier has been studied. Its pharmacokinetic profile supports its use as a research tool.
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| Toxicity/Toxicokinetics |
CHPG sodium salt is intended for laboratory research use only and has not undergone comprehensive toxicology testing. As a mGluR5 agonist, the compound would be expected to have effects on neuronal function and behavior. Standard in vitro cytotoxicity assays in cell lines are typically performed alongside efficacy studies to rule out nonspecific toxicity. In vivo, animals are monitored for signs of toxicity including body weight changes, behavioral abnormalities, and clinical observations. Comprehensive toxicological characterization including genotoxicity, cardiotoxicity, and repeated-dose toxicity studies has not been reported in the public domain. The compound is not approved for human use and is strictly intended for research purposes.
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| References |
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| Additional Infomation |
CHPG sodium salt is a selective agonist of the metabotropic glutamate receptor subtype mGluR5. It activates mGluR5 and stimulates downstream signaling pathways including ERK and Akt. The compound has a molecular formula of C8H7ClNNaO3 and a molecular weight of 223.59 g/mol. CHPG sodium salt attenuates SO2-induced oxidative stress and inflammation through the TSG-6/NF-kappaB pathway in BV2 microglial cells. It is widely used in neuroscience research to investigate mGluR5 function in learning, memory, and neurodegenerative diseases such as Alzheimer's and Parkinson's. CHPG sodium salt has not entered clinical trials and has not received regulatory approval for any indication. It is available from research chemical suppliers for non-clinical research purposes only. CHPG sodium salt is a valuable research tool for studying mGluR5 biology and developing new therapies for neurological disorders.
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| Molecular Formula |
C8H7CLNNAO3
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| Molecular Weight |
223.58885216713
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| Exact Mass |
223.001
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| CAS # |
1303993-73-8
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| Related CAS # |
CHPG;170846-74-9
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| PubChem CID |
52974246
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
14
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| Complexity |
205
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=C(C=C1O)C(C(=O)[O-])N)Cl.[Na+]
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| InChi Key |
KZRZZIISUUINJT-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C8H8ClNO3.Na/c9-6-2-1-4(11)3-5(6)7(10)8(12)13;/h1-3,7,11H,10H2,(H,12,13);/q;+1/p-1
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| Chemical Name |
sodium;2-amino-2-(2-chloro-5-hydroxyphenyl)acetate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~447.25 mM)
H2O : ~6.67 mg/mL (~29.83 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.18 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (11.18 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (11.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5 mg/mL (22.36 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.4725 mL | 22.3624 mL | 44.7247 mL | |
| 5 mM | 0.8945 mL | 4.4725 mL | 8.9449 mL | |
| 10 mM | 0.4472 mL | 2.2362 mL | 4.4725 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Link: https://clinicaltrials.gov/ct2/show/NCT06231381
Conditions:Generalized Pustular Psoriasis (GPP)Link: https://clinicaltrials.gov/ct2/show/NCT06477536
Conditions:Generalized Pustular PsoriasisLink: https://clinicaltrials.gov/ct2/show/NCT06716151
Conditions:Healthy
Title:HB0034 in Patients With Generalized Pustular Psoriasis (GPP)
Status:Completed
updateDate:2024-01-23
Ctid:NCT05512598
Link: https://clinicaltrials.gov/ct2/show/NCT05512598
Conditions:Generalized Pustular PsoriasisLink: https://clinicaltrials.gov/ct2/show/NCT05064345
Conditions:HealthyProducts are for research use only; We do not sell to patients
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