A-804598
Based on 3 publication(s) in Google Scholar
A-804598 is a BBB penetrant, competitive and selective P2X7 receptor antagonist with IC50s of 9 nM, 10 nM and 11 nM for mouse, rat and human P2X7 receptors, respectively.
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- Purity: 98.68%
- CAS No.: 1125758-85-1
- 화학식: C19H17N5
- 분자량:315.37
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) A-804598
MoreAll P2X Receptor Isoforms
More
Biological Activity
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P2X7 Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| THP-1 | IC50 |
15 nM
Compound: 6; A-804598
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Antiinflammatory activity against human THP-1 cells assessed as reduction in LPS and BzATP-induced IL-1beta release measured after 50 mins by microplate reader
Antiinflammatory activity against human THP-1 cells assessed as reduction in LPS and BzATP-induced IL-1beta release measured after 50 mins by microplate reader
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[PMID: 33822617] |
Pre-incubation with A-804598 (0.1-10 μM; 1 hour) significantly attenuates BzATP-induced cell loss in a concentration-dependent manner. 3 μM A-804598 exhibits the greatest protective effect against BzATP-induced cytotoxicity[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:microglial cell
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Concentration:0.1, 0.3, 1, 3, 10 μM
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Incubation Time:1 hour
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Result:Protected against BzATP-induced cytotoxicity in both inactivated and activated microglia.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult B6.Cg-Tg (SOD1-G93A) 1Gur/J female mice [3]
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Dosage:30 mg/kg
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Administration:Intraperitoneal injection; five times a week
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Result:Decreased SQSTM1/p62 expression.
Chemical Information
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CAS No. 1125758-85-1
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Appearance Solid
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분자량 315.37
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화학식 C19H17N5
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Color White to off-white
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SMILES
C[C@H](/N=C(NC1=C2C=CC=NC2=CC=C1)/NC#N)C3=CC=CC=C3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Int Immunopharmacol
Extracellular ATP contributes to the reactive oxygen species burst and exaggerated mitochondrial damage in D-galactosamine and lipopolysaccharide-induced fulminant hepatitis. [Abstract]2024 Mar 30:130:111680. PMID: 38368772 -
Front Pharmacol
The NLRP3 inflammasome is involved in resident intruder paradigm-induced aggressive behaviors in mice. [Abstract]2023 Jan 25:14:974905. PMID: 36778007 -
Cell Cycle
LncRNA MIAT downregulates IL-1β, TNF-ɑ to suppress macrophage inflammation but is suppressed by ATP-induced NLRP3 inflammasome activation. [Abstract]2021 Jan;20(2):194-203. PMID: 33459112
용액&용해도
DMSO : ≥ 32 mg/mL (101.47 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.93 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (7.93 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (279 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[2]. Yingbo He et al. The role of microglial P2X7: modulation of cell death and cytokine release. Neuroinflammation, 2017 Jul, 14(1):135. [Content Brief]
[3]. Paola Fabbrizio et al. P2X7 Receptor Activation Modulates Autophagy in SOD1-G93A Mouse Microglia.Cell Neurosci, 2017 Aug, 11:249. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.1709 mL | 15.8544 mL | 31.7088 mL | 79.2720 mL |
| 5 mM | 0.6342 mL | 3.1709 mL | 6.3418 mL | 15.8544 mL | |
| 10 mM | 0.3171 mL | 1.5854 mL | 3.1709 mL | 7.9272 mL | |
| 15 mM | 0.2114 mL | 1.0570 mL | 2.1139 mL | 5.2848 mL | |
| 20 mM | 0.1585 mL | 0.7927 mL | 1.5854 mL | 3.9636 mL | |
| 25 mM | 0.1268 mL | 0.6342 mL | 1.2684 mL | 3.1709 mL | |
| 30 mM | 0.1057 mL | 0.5285 mL | 1.0570 mL | 2.6424 mL | |
| 40 mM | 0.0793 mL | 0.3964 mL | 0.7927 mL | 1.9818 mL | |
| 50 mM | 0.0634 mL | 0.3171 mL | 0.6342 mL | 1.5854 mL | |
| 60 mM | 0.0528 mL | 0.2642 mL | 0.5285 mL | 1.3212 mL | |
| 80 mM | 0.0396 mL | 0.1982 mL | 0.3964 mL | 0.9909 mL | |
| 100 mM | 0.0317 mL | 0.1585 mL | 0.3171 mL | 0.7927 mL |
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