A-804598 (A804598)

Alias: A-804598; A 804598; A804598
Cat No.:V0084 Purity: ≥98%
A-804598(A 804598) is a structurally novel, CNS penetrant, potent, competitive, and selective antagonist of the purinergic P2X7 receptors (IC50 = 10 nM, 9 nM and 11 nM for rat, mouse and human P2X7 receptors respectively) with potential anti-inflammatory activity.
A-804598 (A804598) Chemical Structure CAS No.: 1125758-85-1
Product category: P2 Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Product Description

A-804598 (A 804598) is a structurally novel, CNS penetrant, potent, competitive, and selective antagonist of the purinergic P2X7 receptors (IC50 = 10 nM, 9 nM and 11 nM for rat, mouse and human P2X7 receptors respectively) with potential anti-inflammatory activity. Purinergic P2X7 receptors (P2X7Rs) play an important role in the generation of inflammatory responses during a number of CNS pathologies. A804598 treatment reversed the changes in microglia and astrocytes, reduced/abolished increases in mRNA levels of number of inflammatory markers, including IL-1β, iNOS, CXCR2, and components of inflammatory signaling pathways, such as TLR2, CASP1, NF-kB1 and CREB1, as well in the protein levels of pro-IL-1β and Nf-kB1.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
In a concentration-dependent manner, pre-incubation with A-804598 (0.1-10 μM; 1 hour) greatly reduces BzATP-induced cell loss. The highest protective effect against BzATP-induced cytotoxicity is shown by 3 μM A-804598[2].
ln Vivo
In the lumbar spinal cord in the end stage of the disease, chroni therapy with A-804598 (intraperitoneal injection; 30 mg/kg; five times a week) reduces the expression of LC3B-II and SQSTM1/p62[3].
Cell Assay
Cell Cytotoxicity Assay[2]
Cell Types: microglial cell
Tested Concentrations: 0.1, 0.3, 1, 3, 10 μM
Incubation Duration: 1 hour
Experimental Results: Protected against BzATP-induced cytotoxicity in both inactivated and activated microglia.
Animal Protocol
Animal/Disease Models: Adult B6 .Cg-Tg (SOD1-G93A) 1Gur/J female mice [3]
Doses: 30 mg/kg
Route of Administration: intraperitoneal (ip)injection; five times a week
Experimental Results: diminished SQSTM1/p62 expression.
References
[1]. Donnelly-Roberts DL et al. [3H]A-804598 ([3H]2-cyano-1-[(1S)-1-phenylethyl]-3-quinolin-5-ylguanidine) is a novel, potent, and selective antagonist radioligand for P2X7 receptors. Neuropharmacology, 2009 Jan, 56(1):223-9.
[2]. Yingbo He et al. The role of microglial P2X7: modulation of cell death and cytokine release. Neuroinflammation, 2017 Jul, 14(1):135.
[3]. Paola Fabbrizio et al. P2X7 Receptor Activation Modulates Autophagy in SOD1-G93A Mouse Microglia.Cell Neurosci, 2017 Aug, 11:249.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H17N5
Molecular Weight
315.38
CAS #
1125758-85-1
SMILES
C[ C@H](/N=C(NC1=C2C=CC=NC2=CC=C1)/NC#N)C3=CC=CC=C3
Chemical Name
N-Cyano-N′′-[(1S)-1-phenylethyl]-N′-5-quinolinyl-guanidine
Synonyms
A-804598; A 804598; A804598
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)
Solubility Data
Solubility (In Vitro)
DMSO: > 10mg/mL
Water: N/A
Ethanol:N/A
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.1708 mL 15.8539 mL 31.7078 mL
5 mM 0.6342 mL 3.1708 mL 6.3416 mL
10 mM 0.3171 mL 1.5854 mL 3.1708 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.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Biological Data
  • A-804598

    P2X7 activation modulates microtubule-associated protein 1 light chain 3 (LC3)-II in superoxide dismutase 1 (SOD1)-G93A microglia.2017 Aug 21;11:249.

  • A-804598

    P2X7 induces autophagic flux in SOD1-G93A microglia.2017 Aug 21;11:249.

  • A-804598

    In vivochronic treatment with P2X7 antagonist A-804598 decreases SQSTM1/p62 expression in lumbar spinal cord of SOD1-G93A mice.2017 Aug 21;11:249.

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