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Evans Blue GluR inhibitor

Name: Evans Blue
Brand: Selleck Chemicals
SKU: S4716
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S4716

Evans Blue (Direct Blue 53,C.I.23860) is a potent inhibitor of the uptake of L-glutamate into synaptic vesicles, also an AMPA/kainate receptor antagonist.

Chemical Structure

Molecular Weight: 960.81

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.05%

99.05

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel MAO Beta Amyloid NMDAR P2 Receptor Trk receptor Serotonin Transporter Notch Cannabinoid Receptor P-gp CaMK Opioid Receptor BACE Sigma Receptor FAAH Neurokinin Receptor OX Receptor CGRP Receptor BChE Adenosine Deaminase CCK receptor MT Receptor
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Chemical Information, Storage & Stability

Molecular Weight	960.81	Formula	C₃₄H₂₄N₆O₁₄S₄.4Na	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	314-13-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Direct Blue 53,C.I.23860			Smiles	CC1=C(C=CC(=C1)C2=CC(=C(C=C2)N=NC3=C(C4=C(C=C3)C(=CC(=C4N)S(=O)(=O)[O-])S(=O)(=O)[O-])O)C)N=NC5=C(C6=C(C=C5)C(=CC(=C6N)S(=O)(=O)[O-])S(=O)(=O)[O-])O.[Na+].[Na+].[Na+].[Na+]

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (104.07 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 100 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5mg/ml (5.20mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.71mg/ml (0.74mM)	Taking the 1 mL working solution as an example, add 50 μL of 14.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	AMPA/kainate receptor ^[7] vesicular glutamate uptake ^[5] 87 nM
In vitro	Evans Blue is found to be inhibiting DNA binding of NF-κB at a low concentration of 100 μM^[1]. It has proven over the years to be a dependable stain for microscopic determination of cell death^[2]. This compound is also a known blocker of a subset of a-amino-3-hydroxy-5-methyl-isoxazole/kainate receptors (IC50=355 nM) for the subunit combination GluR1,2^[5]. This chemical is the first known δ-subunit-specific antagonist of ENaC and activates large-conductance Ca2+-activated K+ channels in sheep bladder myocytes and cultured endothelial cells of human umbilical veins^[5].
In vivo	Evans blue pretreatment could inhibit the mast cells degranulation and that may be the main mechanism for prevent animals from C48/80-triggered anaphylaxis and systemic inflammation^[4]. This compound modulates the non-N-methyl-d-aspartate receptor in rat thalamic neurons, blocks the P2X-purinergic receptor in rat vas deferens, and inhibits the glutamate transporter in rat brain synaptic vesicles^[6].
References	[1] https://pubmed.ncbi.nlm.nih.gov/15546742/ [2] http://link.springer.com/article/10.1007/BF00037585 [3] https://pubmed.ncbi.nlm.nih.gov/17689176/ [4] http://www.fasebj.org/content/30/1_Supplement/723.10 [5] https://pubmed.ncbi.nlm.nih.gov/9802337/ [6] http://jpet.aspetjournals.org/content/315/2/965.long [7] https://pubmed.ncbi.nlm.nih.gov/8967991/

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