A-740003
Based on 17 publication(s) in Google Scholar
A-740003 is a potent, selective and competitive P2X7 receptor antagonist with IC50 values are 18 and 40 nM for rat and human P2X7 receptors, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.61%
- No. CAS: 861393-28-4
- Fòrmula: C26H30N6O3
- Peso molecular:474.55
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) A-740003
More- Neural Regen Res. 2026 Apr 1;21(4):1628-1640. [Abstract]
- Commun Biol. 2023 Jun 15;6(1):642. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2024 Jan;1870(1):166895. [Abstract]
- Mol Med Rep. 2021 Jul;24(1):521. [Abstract]
- iScience. 2025 Sep 5;28(10):113517. [Abstract]
- Saudi Pharm J. 2024 Jul;32(7):102102. [Abstract]
- Prog Neuropsychopharmacol Biol Psychiatry. 2023 Aug 30:126:110796. [Abstract]
- Vet Res. 2022 Sep 5;53(1):69. [Abstract]
- Cell Biochem Funct. 2025 May;43(5):e70078. [Abstract]
- Vet Microbiol. 2021 Aug:259:109130. [Abstract]
- J Cardiovasc Dev Dis. 2025 Nov 6;12(11):438. [Abstract]
- Purinergic Signal. 2024 Nov 16. [Abstract]
- Purinergic Signal. 2024 Jun;20(3):273-284. [Abstract]
- Purinergic Signal. 2017 Jun;13(2):215-225. [Abstract]
- Dev Comp Immunol. 2022 Jun:131:104377. [Abstract]
- bioRxiv. 2024 September 24.
- Research Square Preprint. 2022 May.
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RT-PCR
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Cell Proliferation/Viability Assay
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Ver todos los productos específicos de isoformas P2X Receptor
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Actividad biológica
Descripciòn
IC50 & Target
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P2X7 Receptor |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.75 μM
Compound: A740003
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Antagonist activity at human P2X7R expressed in HEK293 cells assessed as inhibition of ATP-induced ethidium iodide uptake preincubated for 5 mins followed by ATP induction and measured after 25 mins by fluorescence assay
Antagonist activity at human P2X7R expressed in HEK293 cells assessed as inhibition of ATP-induced ethidium iodide uptake preincubated for 5 mins followed by ATP induction and measured after 25 mins by fluorescence assay
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[PMID: 30528164] |
| Peritoneal macrophage | CC50 |
325.4 μM
Compound: A740003
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Cytotoxicity against Swiss Webster mouse peritoneal macrophages by LDH release assay
Cytotoxicity against Swiss Webster mouse peritoneal macrophages by LDH release assay
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[PMID: 29133043] |
| Peritoneal macrophage | IC50 |
0.723 μM
Compound: A740003
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Antiinflammatory activity in LPS/IFNgamma-differentiated Swiss Webster mouse peritoneal macrophages assessed as inhibition of ATP-induced IL-1beta release preincubated for 15 mins followed by ATP/LPS challenge measured after 30 mins by sandwich ELISA
Antiinflammatory activity in LPS/IFNgamma-differentiated Swiss Webster mouse peritoneal macrophages assessed as inhibition of ATP-induced IL-1beta release preincubated for 15 mins followed by ATP/LPS challenge measured after 30 mins by sandwich ELISA
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[PMID: 29133043] |
| THP-1 | IC50 |
0.689 μM
Compound: A740003
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Antiinflammatory activity in LPS/IFNgamma-differentiated human THP1 cells assessed as inhibition of ATP-induced IL-1beta release after 30 mins by ELISA
Antiinflammatory activity in LPS/IFNgamma-differentiated human THP1 cells assessed as inhibition of ATP-induced IL-1beta release after 30 mins by ELISA
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[PMID: 29133043] |
| THP-1 | IC50 |
156 nM
Compound: 4, A-740003
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Antagonist activity at human recombinant P2X7 receptor expressed in human THP1 cells assessed as inhibition of BzATP-induced IL1-beta release by enzyme-linked immunosorbent assay
Antagonist activity at human recombinant P2X7 receptor expressed in human THP1 cells assessed as inhibition of BzATP-induced IL1-beta release by enzyme-linked immunosorbent assay
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[PMID: 19540765] |
In Vitro
A-438079 or A-740003 (10 μM) significantly blocks the sustained phase of the BzATP-induced response[1]. A-740003 infusion reduces SE-induced TNF-α expression in dentate granule cells. A-740003 infusions increases SE-induced neuronal death[2]. A-740003 and A-438079 show significantly greater potency in blocking P2X7 receptor activation across all species compared with other antagonists. A-740003 and A-438079 show greater activity at rat and human, as compared with mouse P2X7 receptors[3]. A-740003 potently blocks agonist-evoked IL-1β release with (IC50=156 nM) and pore formation (IC50=92 nM) in differentiated human THP-1 cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 861393-28-4
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Appearance Solid
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Peso molecular 474.55
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Fòrmula C26H30N6O3
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Color White to off-white
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SMILES
N#C/N=C(NC(NC(CC1=CC(OC)=C(C=C1)OC)=O)C(C)(C)C)\NC2=CC=CC3=NC=CC=C23
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (17)
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Journal Impact Factor
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Most Recent
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Neural Regen Res
Overexpression of the inwardly rectifying potassium channel Kir4.1 or Kir4.1 Tyr 9 Asp in Müller cells exerts neuroprotective effects in an experimental glaucoma model. [Abstract]2026 Apr 1;21(4):1628-1640. PMID: 39589165
A-740003 purchased from MedChemExpress. Usage Cited in: Neural Regen Res. 2026 Apr 1;21(4):1628-1640. [Abstract]
A-740003 (1 μM; 72 h) in microglia co-cultured with Müller cells in which P2X7/P2X4 receptor signaling was inhibited. mRNA levels of the inflammatory factors interleukin-1β (IL-1β) in microglia were assessed by qPCR.
A-740003 purchased from MedChemExpress. Usage Cited in: Neural Regen Res. 2026 Apr 1;21(4):1628-1640. [Abstract]
A-740003 (1 μM; 72 h) in microglia co-cultured with Müller cells in which P2X7/P2X4 receptor signaling was inhibited. IL-1β concentrations in the co-culture medium were measured using enzyme-linked immunosorbent assay.
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Commun Biol
2023 Jun 15;6(1):642. PMID: 37322056
A-740003 purchased from MedChemExpress. Usage Cited in: Commun Biol. 2023 Jun 15;6(1):642. [Abstract]
A549, SK-N-BE(2)C, and T47D cells were treated with 0.1% FBS (starvation conditions), 10% FBS (control conditions) or 20 μM A740003 for 24 h. Subsequently, 200 μM ATP was added, and cells were incubated for 6 h. EVs were isolated from media and detected using a Western blot.
A-740003 purchased from MedChemExpress. Usage Cited in: Commun Biol. 2023 Jun 15;6(1):642. [Abstract]
A549, SK-N-BE(2)C and T47D cells were treated with DMSO (control), 0.1% FBS (starv.) for 18 h, 200 μM ATP (exATP) for 6 h, 2 μM citreoviridin (Citreo) for 24 h, 30 μM mdivi-1 for 24 h, or 20 μM A740003 for 24 h. The levels of Ca2+ in the cell lysates were determined according to the user manual of the calcium ion assay kit.
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Biochim Biophys Acta Mol Basis Dis
Extracellular ATP (eATP) inhibits the progression of endometriosis and enhances the immune function of macrophages. [Abstract]2024 Jan;1870(1):166895. PMID: 37748566
A-740003 purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2024 Jan;1870(1):166895. [Abstract]
A-740003 (10 μM; 4 h) the proliferation inhibition of endometriotic epithelial cells induced by coculture with macrophages accompanied by a high eATP environment was significantly mitigated.
A-740003 purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2024 Jan;1870(1):166895. [Abstract]
A-740003 (10 μM; 4 h) reduced the cell death rate in 0.5 mM and 1 mM eATP environments by 39.3 % and 41.9 %, respectively on macrophages.
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Mol Med Rep
Role of P2X7R in eosinophilic and non‑eosinophilic chronic rhinosinusitis with nasal polyps. [Abstract]2021 Jul;24(1):521. PMID: 34036391 -
iScience
M1-like macrophages regulate T cell infiltration in colorectal cancer through P2X4 receptor. [Abstract]2025 Sep 5;28(10):113517. PMID: 41031375
A-740003 purchased from MedChemExpress. Usage Cited in: iScience. 2025 Sep 5;28(10):113517. [Abstract]
PBMC-derived macrophages were induced into TAMs by SW480-conditioned medium with the addition of 20 μmol/L BAY-1797 (P2X4 blocker), 20 μmol/L A-740003 (P2X7 blocker), and 20 μmol/L NF279 (P2X1 blocker), respectively. An equal final concentration of DMSO (0.05%) was used including vehicle controls. The STAT1 phosphorylation were observed by western blot.
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Saudi Pharm J
Antifibrotic effect of the P2X7 receptor antagonist A740003 against acute myocardial infarction-induced fibrotic remodelling. [Abstract]2024 Jul;32(7):102102. PMID: 39035363 -
Prog Neuropsychopharmacol Biol Psychiatry
Microglial NLRP3 inflammasome activation mediates diabetes-induced depression-like behavior via triggering neuroinflammation. [Abstract]2023 Aug 30:126:110796. PMID: 37209992 -
Vet Res
2022 Sep 5;53(1):69. PMID: 36064470
A-740003 purchased from MedChemExpress. Usage Cited in: Vet Res. 2022 Sep 5;53(1):69. [Abstract]
Cells were primed with LPS for 3 h and then CATH-2 (5 μM) and ATP (1.5 mg/mL) as positive control were added for an additional 21 h. To inhibit K + efflux and the P2X7 receptor, cells were untreated (UT) or treated with KCl (5 mM and 50 mM) and the P2X7R inhibitor (A-740003, 100 μM) after LPS stimulation. Finally, cell supernatants and lysates were collected for different assays. ELISA was used to determine cytokine secretion of IL-1β and TNF-α.
A-740003 purchased from MedChemExpress. Usage Cited in: Vet Res. 2022 Sep 5;53(1):69. [Abstract]
Cells were primed with LPS for 3 h and then CATH-2 (5 μM) and ATP (1.5 mg/mL) as positive control were added for an additional 21 h. To inhibit K + efflux and the P2X7 receptor, cells were untreated (UT) or treated with KCl (5 mM and 50 mM) and the P2X7R inhibitor (A-740003, 100 μM) after LPS stimulation. A representative image (Western blot) is presented to show protein expression including IL-1β, caspase-1, pro-IL-1β, pro-caspase-1 and β-action.
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Cell Biochem Funct
P2X7 Receptor Facilitates Cardiomyocyte Autophagy After Myocardial Infarction via Nox4/PERK/ATF4 Signaling Pathway. [Abstract]2025 May;43(5):e70078. PMID: 40289672 -
Vet Microbiol
ATP-dependent activation of NLRP3 inflammasome in primary murine macrophages infected by pseudorabies virus. [Abstract]2021 Aug:259:109130. PMID: 34052623 -
J Cardiovasc Dev Dis
Role of P2X7 Receptor on Hypoxia-Induced Vascular Endothelial Growth Factor Gene Expression in H9c2 Rat Cardiomyocytes. [Abstract]2025 Nov 6;12(11):438. PMID: 41295364 -
Purinergic Signal
Antagonism of the ATP-gated P2X7 receptor inhibits the proliferation of hepatocellular carcinoma cells. [Abstract]2024 Nov 16. PMID: 39549156 -
Purinergic Signal
Potential role of the P2X7 receptor in the proliferation of human diffused large B-cell lymphoma. [Abstract]2024 Jun;20(3):273-284. PMID: 37222921 -
Purinergic Signal
Effect of electroacupuncture on the cervicospinal P2X7 receptor/fractalkine/CX3CR1 signaling pathway in a rat neck-incision pain model. [Abstract]2017 Jun;13(2):215-225. PMID: 28028627
A-740003 purchased from MedChemExpress. Usage Cited in: Purinergic Signal. 2017 Jun;13(2):215-225. [Abstract]
Effect of A-740003 on thermal pain thresholds and P2X7R expression following the neck incision and EA stimulation.
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Dev Comp Immunol
Chicken cathelicidin-2 promotes IL-1β secretion via the NLRP3 inflammasome pathway and serine proteases activity in LPS-primed murine neutrophils. [Abstract]2022 Jun:131:104377. PMID: 35189160 -
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Solvente y solubilidad
In Vitro:
DMSO : 50 mg/mL (105.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 (5.27 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.
In Vivo Dissolution Calculator
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.
Protocolo
Animal Administration[4]
The response to acute thermal stimulation is determined using a commercially available paw thermal stimulator. Rats are placed individually in Plexiglas cubicles mounted on a glass surface maintained at 30°C and allowed a 30-min habituation period. A thermal stimulus, in the form of radiant heat emitted from a focused projection bulb, is then applied to the plantar surface of each hind paw. In each test session, each rat is tested in three sequential trials at approximately 5-min intervals. Paw-withdrawal latencies (PWLs) are calculated as the median of the two shortest latencies. An assay cut off is set at 20.5 s. A-740003 is injected i.p. 30 min before testing for acute thermal pain.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Grol MW, et al. P2X?-mediated calcium influx triggers a sustained, PI3K-dependent increase in metabolic acid production by osteoblast-like cells. Am J Physiol Endocrinol Metab. 2012 Mar 1;302(5):E561-75. [Content Brief]
[2]. Kim JE, et al. P2X7 receptor activation ameliorates CA3 neuronal damage via a tumor necrosis factor-α-mediated pathway in the rat hippocampus following status epilepticus. J Neuroinflammation. 2011 Jun 2;8:62. [Content Brief]
[3]. Donnelly-Roberts DL, et al. Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors.Br J Pharmacol. 2009 Aug;157(7):1203-14. Epub 2009 Jun 22. [Content Brief]
[4]. Honore P, et al. A-740003 [N-(1-{[(cyanoimino)(5-quinolinylamino) methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide], a novel and selective P2X7 receptor antagonist, dose-dependently reduces neuropathic pain in the rat. J Pharmacol Exp Ther. 2006 Dec;319(3):1376-85. Epub 2006 Sep 18. [Content Brief]
[5]. Y. H. Gao, et al. Effect of electroacupuncture on the cervicospinal P2X7 receptor/fractalkine/CX3CR1 signaling pathway in a rat neck-incision pain model. Purinergic Signal. 2017 Jun;13(2):215-225. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1073 mL | 10.5363 mL | 21.0726 mL | 52.6815 mL |
| 5 mM | 0.4215 mL | 2.1073 mL | 4.2145 mL | 10.5363 mL | |
| 10 mM | 0.2107 mL | 1.0536 mL | 2.1073 mL | 5.2681 mL | |
| 15 mM | 0.1405 mL | 0.7024 mL | 1.4048 mL | 3.5121 mL | |
| 20 mM | 0.1054 mL | 0.5268 mL | 1.0536 mL | 2.6341 mL | |
| 25 mM | 0.0843 mL | 0.4215 mL | 0.8429 mL | 2.1073 mL | |
| 30 mM | 0.0702 mL | 0.3512 mL | 0.7024 mL | 1.7560 mL | |
| 40 mM | 0.0527 mL | 0.2634 mL | 0.5268 mL | 1.3170 mL | |
| 50 mM | 0.0421 mL | 0.2107 mL | 0.4215 mL | 1.0536 mL | |
| 60 mM | 0.0351 mL | 0.1756 mL | 0.3512 mL | 0.8780 mL | |
| 80 mM | 0.0263 mL | 0.1317 mL | 0.2634 mL | 0.6585 mL | |
| 100 mM | 0.0211 mL | 0.1054 mL | 0.2107 mL | 0.5268 mL |
A-740003 Related Classifications
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