| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 100mg | |||
| Other Sizes |
| Targets |
CHPG selectively targets the metabotropic glutamate receptor 5 (mGluR5). It binds to the receptor and activates it, leading to the activation of downstream signaling pathways, including phospholipase C, protein kinase C, and ERK. It has an EC50 in the micromolar range for mGluR5.
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| ln Vitro |
Following SO2 derivative treatment, CHPG (10-500 µM; 24 hours) can dramatically improve cell viability and decrease LDH release [1]. BV2 cells are shielded from SO2-induced apoptosis by CHPG (0.5 mM; 30 min) [1]. TSG-6 is expressed more at the mRNA and protein levels when treated with CHPG (0.5 mM; 30 min) alone [1].
In vitro, CHPG activates mGluR5 in various cell types, including neurons and glial cells. Activation leads to increased intracellular calcium, activation of protein kinase C, and modulation of synaptic transmission. It also promotes neuroprotection and neuroplasticity. |
| ln Vivo |
Brain lesion volume is significantly reduced by CHPG (injection; 250 nM; for 7 days) [2].
In vivo, CHPG has been shown to have neuroprotective effects in animal models of stroke and neurodegeneration. It also modulates pain perception and anxiety. It is used to study the role of mGluR5 in various physiological and pathological processes. |
| Enzyme Assay |
In vitro receptor activation assays are performed using cells expressing mGluR5. Cells are loaded with a calcium-sensitive fluorescent dye, and changes in intracellular calcium are measured upon addition of CHPG. EC50 values are calculated from dose-response curves.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: BV2 Microglia 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. Cells (e.g., HEK293 cells transfected with mGluR5) are cultured. Cells are loaded with Fluo-4 or Fura-2. Various concentrations of CHPG are added, and fluorescence is measured using a fluorescence plate reader. The EC50 is calculated from the dose-response curve. |
| Animal Protocol |
Animal/Disease Models: Adult SD (SD (Sprague-Dawley)) male rats, weight 280-320 g [2]
Doses: 250 nM Route of Administration: injection; 7 days Experimental Results: Brain lesion volume was Dramatically diminished. Animal studies use rodent models. CHPG is administered via intracerebroventricular (ICV) injection or directly into the brain. Neuroprotection is assessed in models of stroke or excitotoxicity. Pain is assessed by measuring withdrawal thresholds. Anxiety-like behavior is assessed using the elevated plus maze. |
| ADME/Pharmacokinetics |
CHPG (MW 203.62) is a small molecule. It has good brain penetration. Its pharmacokinetic properties are not extensively documented. It is typically administered by injection for in vivo studies.
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| Toxicity/Toxicokinetics |
CHPG is generally well-tolerated at pharmacologically active doses. No significant toxicity has been reported. Comprehensive toxicological data are limited. It is a research compound and not intended for human use.
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| References |
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| Additional Infomation |
CHPG is a research tool used to study mGluR5 biology. It is not an approved drug and is not in clinical trials. It is widely used in pharmacological studies to characterize the role of mGluR5 in neurological and psychiatric disorders. It is also known as (RS)-2-chloro-5-hydroxyphenylglycine.
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| Molecular Formula |
C8H8NO3CL
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|---|---|
| Molecular Weight |
201.60702
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| Exact Mass |
201.019
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| CAS # |
170846-74-9
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| Related CAS # |
CHPG sodium salt;1303993-73-8
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| PubChem CID |
3645780
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| Appearance |
White to off-white solid powder
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| LogP |
1.83
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
13
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| Complexity |
200
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
UNIDAFCQFPGYJJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H8ClNO3/c9-6-2-1-4(11)3-5(6)7(10)8(12)13/h1-3,7,11H,10H2,(H,12,13)
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| Chemical Name |
2-amino-2-(2-chloro-5-hydroxyphenyl)acetic acid
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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 |
| 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) |
1M NaOH : 25 mg/mL (~124.00 mM)
DMSO :< 1 mg/mL |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.9601 mL | 24.8004 mL | 49.6007 mL | |
| 5 mM | 0.9920 mL | 4.9601 mL | 9.9201 mL | |
| 10 mM | 0.4960 mL | 2.4800 mL | 4.9601 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.
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