CHPG sodium salt is a selective mGluR5 agonist and attenuates SO2-induced oxidative stress and inflammation in BV2 microglia via the TSG-6/NF-κB pathway. CHPG sodium salt prevents traumatic brain injury (TBI) through the ERK and Akt pathways in vitro & in vivo.

Physicochemical Properties

Molecular Formula	C8H7CLNNAO3
Molecular Weight	223.58885216713
Exact Mass	223.001
CAS #	1303993-73-8
Related CAS #	CHPG;170846-74-9
PubChem CID	52974246
Appearance	White to off-white solid powder
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	2
Heavy Atom Count	14
Complexity	205
Defined Atom Stereocenter Count	0
InChi Key	KZRZZIISUUINJT-UHFFFAOYSA-M
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
Chemical Name	sodium;2-amino-2-(2-chloro-5-hydroxyphenyl)acetate
HS Tariff Code	2934.99.9001
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)

Biological Activity

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].
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.
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.
References	[1]. The selective mGluR5 agonist CHPG attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. Neurochem Int. 2015 Jun-Jul;85-86:46-52. [2]. The selective mGluR5 agonist CHPG protects against traumatic brain injury in vitro and in vivo via ERK and Akt pathway. Int J Mol Med. 2012 Apr;29(4):630-6.

Solubility Data

Solubility (In Vitro)

DMSO : ~100 mg/mL (~447.25 mM) H2O : ~6.67 mg/mL (~29.83 mM)

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. 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. 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 corn oil and mix evenly. 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).  (Please use freshly prepared in vivo formulations for optimal results.)

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.