A 438079
Based on 27 publication(s) in Google Scholar
A 438079 is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
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- 純度: 99.88%
- CAS 番号: 899507-36-9
- 分子式: C13H9Cl2N5
- 分子量:306.15
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保管条件: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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溶剤 & 溶解度
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MedChemExpress（MCE）の使用を引用している文献 A 438079
More- J Adv Res. 2025 Jun:72:571-589. [Abstract]
- J Nanobiotechnology. 2025 May 5;23(1):332. [Abstract]
- Basic Res Cardiol. 2025 Sep 16. [Abstract]
- Neural Regen Res. 2021 Aug;16(8):1582-1591. [Abstract]
- Cancer Immunol Res. 2026 Jan 21. [Abstract]
- Cancer Immunol Res. 2020 Nov;8(11):1426-1439. [Abstract]
- Brain Behav Immun. 2020 Aug:88:507-514. [Abstract]
- Chin Med. 2026 Mar 16;21(1):89. [Abstract]
- J Ethnopharmacol. 2025 Jan 30;337(Pt 1):118792. [Abstract]
- J Agric Food Chem. 2025 Aug 27;73(34):21296-21308. [Abstract]
- Eur J Pharmacol. 2025 May 15:995:177421. [Abstract]
- Int Immunopharmacol. 2026 Feb 1:170:116080. [Abstract]
- Int J Mol Sci. 2022 May 17;23(10):5586. [Abstract]
- Inflammation. 2025 Jun 30. [Abstract]
- Inflammation. 2025 Jun;48(3):987-1002. [Abstract]
- Cell Calcium. 2026 Mar:134:103122. [Abstract]
- Med Oncol. 2025 Jul 16;42(8):340. [Abstract]
- Front Mol Neurosci. 2018 Nov 6:11:401. [Abstract]
- J Immunol. 2023 Jun 15;210(12):1962-1973. [Abstract]
- IBRO Neurosci Rep. 2026 Jun 23;21:179-188. [Abstract]
- Purinergic Signal. 2024 Nov 16. [Abstract]
- Purinergic Signal. 2023 Dec;19(4):685-697. [Abstract]
- Med Sci Monit. 2020 Sep 21:26:e925491. [Abstract]
- Gen Physiol Biophys. 2019 Sep;38(5):407-416. [Abstract]
- Patent. US20260034213A1.
- bioRxiv. 2025 Nov 19.
- bioRxiv. 2025 May 8:2025.05.03.652022. [Abstract]
Customer Validation & Images
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
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In Vivo Efficacy Study
P2X Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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P2X7 Receptor |
In 1321N1 cells stably expressing rat P2X7 receptors, A 438079 blocks BzATP-(10 μM) evoked changes in intracellular calcium concentrations with an IC50 of 321 nM. A 438079 is also selective for the P2X7 receptor, at concentrations up to 100 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 899507-36-9
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性状 Solid
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分子量 306.15
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分子式 C13H9Cl2N5
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Color White to off-white
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SMILES
ClC1=C(Cl)C(C2=NN=NN2CC3=CC=CN=C3)=CC=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (27)
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Journal Impact Factor
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Most Recent
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J Adv Res
Hyperibone J exerts antidepressant effects by targeting ADK to inhibit microglial P2X7R/TLR4-mediated neuroinflammation. [Abstract]2025 Jun:72:571-589. PMID: 39019111
A 438079 purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 Jun:72:571-589. [Abstract]
After the treatment with A438079 (20 μM), changes in effects of HJ on the production of cleaved-Caspase-1 and mature IL-1β in LPS-stimulated BV-2 cell.
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J Nanobiotechnology
Improving epilepsy management by targeting P2 × 7 receptor with ROS/electric responsive nanomicelles. [Abstract]2025 May 5;23(1):332. PMID: 40325469
A 438079 purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2025 May 5;23(1):332. [Abstract]
Drug release profile (A438079) of TFP@A in PBS (pH = 7.4) with and without H₂O₂.
A 438079 purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2025 May 5;23(1):332. [Abstract]
Cumulative drug release rate of nanomicelles calculated for A438079. Experiments were performed in triplicate.
A 438079 purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2025 May 5;23(1):332. [Abstract]
Quantification of A438079 (5 mg/kg) distribution in hippocampal tissues across groups at 4 h post-injection.
A 438079 purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2025 May 5;23(1):332. [Abstract]
TFP-mediated delivery of A438079 (5 mg/kg) significantly reduced the frequency and duration of seizures, particularly in GS.
A 438079 purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2025 May 5;23(1):332. [Abstract]
TFP-mediated delivery of A438079 (5 mg/kg) significantly reduced the frequency and duration of seizures, particularly in GS.
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Basic Res Cardiol
Renal denervation attenuates cardiac dysfunction in HFpEF by inhibiting the ATP-P2X7-NLRP3 inflammasome axis. [Abstract]2025 Sep 16. PMID: 40958035 -
Neural Regen Res
P2X7 receptor activation aggravates NADPH oxidase 2-induced oxidative stress after intracerebral hemorrhage. [Abstract]2021 Aug;16(8):1582-1591. PMID: 33433488 -
Cancer Immunol Res
Regulatory T-cell sensing of extracellular ATP via P2RX7 promotes their accumulation and suppression and drives lung tumor growth. [Abstract]2026 Jan 21. PMID: 41564348 -
Cancer Immunol Res
Blocking P2X7-Mediated Macrophage Polarization Overcomes Treatment Resistance in Lung Cancer. [Abstract]2020 Nov;8(11):1426-1439. PMID: 32933967 -
Brain Behav Immun
Inhibition of P2X7R in the amygdala ameliorates symptoms of neuropathic pain after spared nerve injury in rats. [Abstract]2020 Aug:88:507-514. PMID: 32311494 -
Chin Med
Qiming granules regulate Müller cell pyroptosis and the P2X7R/NLRP3 immune inflammatory pathway in diabetic retinopathy. [Abstract]2026 Mar 16;21(1):89. PMID: 41840640 -
J Ethnopharmacol
Tangzu granule alleviate neuroinflammation in diabetic peripheral neuropathy by suppressing pyroptosis through P2X7R /NLRP3 signaling pathway. [Abstract]2025 Jan 30;337(Pt 1):118792. PMID: 39251151 -
J Agric Food Chem
β-Hydroxybutyric Acid-Induced Bovine Endometrial Epithelial Cell Pyroptosis via Activating P2X7R. [Abstract]2025 Aug 27;73(34):21296-21308. PMID: 40742321 -
Eur J Pharmacol
Overexpression or knockdown of the P2X7 receptor regulates the progression of non-small cell lung cancer, involving GSK-3β and JNK signaling pathways. [Abstract]2025 May 15:995:177421. PMID: 39993700 -
Int Immunopharmacol
CGRP alleviates epilepsy via JAK1-STAT1-P2RX7 signaling: a novel neuroprotective axis targeting neuronal damage. [Abstract]2026 Feb 1:170:116080. PMID: 41429063 -
Int J Mol Sci
2022 May 17;23(10):5586. PMID: 35628400 -
Inflammation
Vitexin Alleviates Kainic Acid-Induced Seizure Through Inhibiting P2X7R/NLRP3 Signaling Pathway. [Abstract]2025 Jun 30. PMID: 40586851 -
Inflammation
Arctiin Mitigates Neuronal Injury by Modulating the P2X7R/NLPR3 Inflammasome Signaling Pathway. [Abstract]2025 Jun;48(3):987-1002. PMID: 39154088 -
Cell Calcium
A NOX2-independent mechanism of Hv1 channel activation promotes inflammatory cytokine release from BV-2 microglia via intracellular Ca2+ mobilisation. [Abstract]2026 Mar:134:103122. PMID: 41581267 -
Med Oncol
Blocking or knockdown of P2X7 receptor inhibits invasion and migration of mouse breast cancer cells via PI3K/Akt/GSK-3β pathways and EMT. [Abstract]2025 Jul 16;42(8):340. PMID: 40670670 -
Front Mol Neurosci
Inhibition of Heat Shock Protein 90 by 17-AAG Reduces Inflammation via P2X7 Receptor/NLRP3 Inflammasome Pathway and Increases Neurogenesis After Subarachnoid Hemorrhage in Mice. [Abstract]2018 Nov 6:11:401. PMID: 30459553
A 438079 purchased from MedChemExpress. Usage Cited in: Front Mol Neurosci. 2018 Nov 6:11:401. [Abstract]
Western analysis of protein expression levels in the treatment of compounds such as A 438079.
A 438079 purchased from MedChemExpress. Usage Cited in: Front Mol Neurosci. 2018 Nov 6:11:401. [Abstract]
Immunohistochemistry staining analysis of effects of rHSP90 and A438079 on neurobehavior and neurogenesis 48 h after SAH.
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J Immunol
Upregulation of P2X7 Exacerbates Myocardial Ischemia-Reperfusion Injury through Enhancing Inflammation and Apoptosis in Diabetic Mice. [Abstract]2023 Jun 15;210(12):1962-1973. PMID: 37144844 -
IBRO Neurosci Rep
Vitamin D alleviates intracerebral hemorrhage symptoms by modulating pro-inflammatory/anti-inflammatory phenotypic transformation of microglia through P2X7R activation of NLRP3. [Abstract]2026 Jun 23;21:179-188. PMID: 42381883 -
Purinergic Signal
Antagonism of the ATP-gated P2X7 receptor inhibits the proliferation of hepatocellular carcinoma cells. [Abstract]2024 Nov 16. PMID: 39549156 -
Purinergic Signal
P2X7 receptor promotes migration and invasion of non-small cell lung cancer A549 cells through the PI3K/Akt pathways. [Abstract]2023 Dec;19(4):685-697. PMID: 36854856 -
Med Sci Monit
P2X7 Receptor (P2X7R) of Microglia Mediates Neuroinflammation by Regulating (NOD)-Like Receptor Protein 3 (NLRP3) Inflammasome-Dependent Inflammation After Spinal Cord Injury. [Abstract]2020 Sep 21:26:e925491. PMID: 32952148 -
Gen Physiol Biophys
Involvement of P2X7 receptors in satellite glial cells of dorsal root ganglia in the BmK I -induced pain model of rats. [Abstract]2019 Sep;38(5):407-416. PMID: 31595882 -
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bioRxiv
Sensing of extracellular ATP via P2RX7 drives lung tumor growth through regulatory T cell suppressive function. [Abstract]2025 May 8:2025.05.03.652022. PMID: 40654622
溶剤 & 溶解度
DMSO : 100 mg/mL (326.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 0.2 mg/mL (0.65 mM; Need ultrasonic)
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.17 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 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.
プロトコル
Human astrocytoma cells, 1321N1, are grown to stably express rat P2X7, human P2X4, P2X2a, P2X2/3, P2X1, P2Y1 and P2Y2 recombinant receptors. Agonist, BzATP, 2,3-O-(4-ben-zoylbenzoyl)-ATP or ATP-induced changes in intracellular Ca2+ concentrations are assessed in all of the cell lines using the Ca2+ chelating dye, Fluo-4, in conjunction with a Fluorometric Imaging Plate Reader. The cells are plated out the day before the experiment onto poly-D-lysine-coated black 96 well plates. After the agonist addition, changes in intracellular Ca2+ concentrations are recorded, per second, for 3 min. Ligands are tested at 11 half-log concentrations from 10-10 to 10-4 M. BzATP or ATP concentrations corresponds to the EC70 values for each receptor to enable comparison of antagonist potencies across the multiple P2 receptor subtypes. A 438079 is added to the cell plate and fluorescence data are collected for 3 min before the addition of agonist, subsequently, data are then collected for another 2 min. The pEC50 or pIC50 values are derived from a single curve fit.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
To confirm A 438079 reach the brain after systemic administration, P10 rat pups are injected with 5 mg/kg A 438079 and killed either 10 min, 30 min, or 2 h later (n=4 per group). Blood samples are centrifuged at 1000×g for 10 min to isolate the plasma. Samples are analyzed using liquid chromatography-mass spectrometry (LC-MS/MS) by a service provider. Briefly, protein is precipitated from 50 μL aliquots of the individual plasma or brain tissue homogenate, and A 438079 is quantified by LC-MS/MS from a five-point standard curve.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (282 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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取扱説明書 (2659 KB)
参考文献
[1]. McGaraughty S, et al. P2X7-related modulation of pathological nociception in rats. Neuroscience. 2007 Jun 8;146(4):1817-28. [Content Brief]
[2]. Mesuret G, et al. CNS Neurosci Ther. 2014 Jun;20(6):556-64. [Content Brief]
[3]. Marcellino D, et al. On the role of P2X(7) receptors in dopamine nerve cell degeneration in a rat model of Parkinson's disease: studies with the P2X(7) receptor antagonist A-438079. J Neural Transm (Vienna). 2010 Jun;117(6):681-7. [Content Brief]
[4]. Martins JP, et al. The role of P2X7 purinergic receptors in inflammatory and nociceptive changes accompanying cyclophosphamide-induced haemorrhagic cystitis in mice. Br J Pharmacol. 2012 Jan;165(1):183-96. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2664 mL | 16.3319 mL | 32.6637 mL | 81.6593 mL |
| 5 mM | 0.6533 mL | 3.2664 mL | 6.5327 mL | 16.3319 mL | |
| 10 mM | 0.3266 mL | 1.6332 mL | 3.2664 mL | 8.1659 mL | |
| 15 mM | 0.2178 mL | 1.0888 mL | 2.1776 mL | 5.4440 mL | |
| 20 mM | 0.1633 mL | 0.8166 mL | 1.6332 mL | 4.0830 mL | |
| 25 mM | 0.1307 mL | 0.6533 mL | 1.3065 mL | 3.2664 mL | |
| 30 mM | 0.1089 mL | 0.5444 mL | 1.0888 mL | 2.7220 mL | |
| 40 mM | 0.0817 mL | 0.4083 mL | 0.8166 mL | 2.0415 mL | |
| 50 mM | 0.0653 mL | 0.3266 mL | 0.6533 mL | 1.6332 mL | |
| 60 mM | 0.0544 mL | 0.2722 mL | 0.5444 mL | 1.3610 mL | |
| 80 mM | 0.0408 mL | 0.2041 mL | 0.4083 mL | 1.0207 mL | |
| 100 mM | 0.0327 mL | 0.1633 mL | 0.3266 mL | 0.8166 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
A 438079 関連分類
HY-15488 関連分類
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