A-803467
Based on 3 publication(s) in Google Scholar
A-803467 is a potent and selective tetrodotoxin-resistant Nav1.8 sodium channel blocker (IC50=8 nM). A-803467 has shown significant anti-nociception in neuropathic and inflammatory pain models. A-803467 enhances the chemosensitivity of conventional anticancer agents through interaction with the ATP-binding cassette subfamily G member 2 (ABCG2) transporter.
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- Pureté: 99.69%
- CAS No.: 944261-79-4
- Formule: C19H16ClNO4
- Masse moléculaire:357.79
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) A-803467
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
Activité biologique
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Nav1.8 8 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
>30 μM
Compound: 27
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Inhibition of hERG potassium channel expressed in CHO cells by isotope efflux assay
Inhibition of hERG potassium channel expressed in CHO cells by isotope efflux assay
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[PMID: 18176998] |
| HEK293 | IC50 |
0.008 μM
Compound: A-803467
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Inhibition of human Nav1.8 channel expressed in HEK293 cells at -40 mV by patch clamp method
Inhibition of human Nav1.8 channel expressed in HEK293 cells at -40 mV by patch clamp method
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[PMID: 17483457] |
| HEK293 | IC50 |
0.008 μM
Compound: A-803467
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Inhibition of human recombinant NaV1.8 expressed in HEK293 cells by conventional voltage clamp electrophysiology assay
Inhibition of human recombinant NaV1.8 expressed in HEK293 cells by conventional voltage clamp electrophysiology assay
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[PMID: 20965738] |
| HEK293 | IC50 |
0.008 μM
Compound: 27
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Inhibition of human recombinant Nav 1.8 channel expressed in HEK293 cells
Inhibition of human recombinant Nav 1.8 channel expressed in HEK293 cells
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[PMID: 18176998] |
| HEK293 | IC50 |
0.079 μM
Compound: A-803467
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Inhibition of human Nav1.8 channel expressed in HEK293 cells at -100 mV by patch clamp method
Inhibition of human Nav1.8 channel expressed in HEK293 cells at -100 mV by patch clamp method
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[PMID: 17483457] |
| HEK293 | IC50 |
0.85 μM
Compound: 27
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Inhibition of mouse recombinant Nav 1.8 channel expressed in HEK293 cells by isotopic efflux assay
Inhibition of mouse recombinant Nav 1.8 channel expressed in HEK293 cells by isotopic efflux assay
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[PMID: 18176998] |
| HEK293 | IC50 |
0.85 μM
Compound: A-803467
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Inhibition of mouse NaV1.8 expressed in HEK293 cells by isotopic efflux assay
Inhibition of mouse NaV1.8 expressed in HEK293 cells by isotopic efflux assay
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[PMID: 20965738] |
| HEK293 | IC50 |
11.76 μM
Compound: A-803467
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Inhibition of human Nav1.3 channel expressed in HEK293 cells at -120 mV by patch clamp method
Inhibition of human Nav1.3 channel expressed in HEK293 cells at -120 mV by patch clamp method
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[PMID: 17483457] |
| HEK293 | IC50 |
2.45 μM
Compound: A-803467
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Inhibition of human Nav1.3 channel expressed in HEK293 cells at -60 mV by patch clamp method
Inhibition of human Nav1.3 channel expressed in HEK293 cells at -60 mV by patch clamp method
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[PMID: 17483457] |
| HEK293 | IC50 |
32.82 μM
Compound: A-803467
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Inhibition of human Nav1.5 channel expressed in HEK293 cells at -150 mV by patch clamp method
Inhibition of human Nav1.5 channel expressed in HEK293 cells at -150 mV by patch clamp method
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[PMID: 17483457] |
| HEK293 | IC50 |
35.34 μM
Compound: A-803467
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Inhibition of human Nav1.7 channel expressed in HEK293 cells at -120 mV by patch clamp method
Inhibition of human Nav1.7 channel expressed in HEK293 cells at -120 mV by patch clamp method
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[PMID: 17483457] |
| HEK293 | IC50 |
6.74 μM
Compound: A-803467
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Inhibition of human Nav1.7 channel expressed in HEK293 cells at -60 mV by patch clamp method
Inhibition of human Nav1.7 channel expressed in HEK293 cells at -60 mV by patch clamp method
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[PMID: 17483457] |
| HEK293 | IC50 |
7.34 μM
Compound: A-803467
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Inhibition of human Nav1.5 channel expressed in HEK293 cells at -90 mV by patch clamp method
Inhibition of human Nav1.5 channel expressed in HEK293 cells at -90 mV by patch clamp method
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[PMID: 17483457] |
| HEK293 | IC50 |
7.38 μM
Compound: A-803467
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Inhibition of human Nav1.2 channel expressed in HEK293 cells at -60 mV by patch clamp method
Inhibition of human Nav1.2 channel expressed in HEK293 cells at -60 mV by patch clamp method
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[PMID: 17483457] |
| HEK293 | IC50 |
8 nM
Compound: A-803467
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Inhibition of human Nav1.8 channel expressed in human HEK293 cells by patch clamp method
Inhibition of human Nav1.8 channel expressed in human HEK293 cells by patch clamp method
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[PMID: 17483457] |
| HEK293 | IC50 |
9.49 μM
Compound: A-803467
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Inhibition of human Nav1.2 channel expressed in HEK293 cells at -120 mV by patch clamp method
Inhibition of human Nav1.2 channel expressed in HEK293 cells at -120 mV by patch clamp method
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[PMID: 17483457] |
A-803467 selectively and significantly reverses the ABCG2-mediated multidrug resistance. A-803467 (7.5 μM) significantly increases the cytotoxicity of mitoxantrone and topotecan in ABCG2-transfected cell lines. A-803467 (7.5 μM) significantly enhanced theintracellular [3H]-MX accumulation in ABCG2-transfected cells. A-803467 (7.5 μM; 0~120 minutes) significantly blocks the intracellular [3H]-MX efflux at different time periods from ABCG2-transfected cells. A-803467 stimulates the ATPase activity of ABCG2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
A-803467 in combination with topotecan, significantly decreases the tumor growth in mice implanted with ABCG2 overexpressing H460/MX20 cells. A-803467 effectively restores the sensitivity of tumors overexpressing ABCG2 transporter to topotecan without having any significant effect on tumors lacking ABCG2 expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice[1]
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Dosage:35 mg/kg
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Administration:P.o.
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Result:Showed no noticeable toxicity in the male NCR nude mice.
Chemical Information
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CAS No. 944261-79-4
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Appearance Solid
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Masse moléculaire 357.79
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Formule C19H16ClNO4
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Color White to light yellow
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SMILES
O=C(C1=CC=C(C2=CC=C(Cl)C=C2)O1)NC3=CC(OC)=CC(OC)=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
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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Cell Rep Med
Intra-channel bi-epitopic crosslinking unleashes ultrapotent antibodies targeting NaV1.7 for pain alleviation. [Abstract]2024 Oct 22:101800. PMID: 39461335
A-803467 purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2024 Oct 22:101800. [Abstract]
A-803467 (100 nM) blocked NaV1.8 currents in mouse dorsal root ganglia cells.
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Front Pharmacol
The Role of Voltage-Gated Sodium Channel 1.8 in the Effect of Atropine on Heart Rate: Evidence From a Retrospective Clinical Study and Mouse Model. [Abstract]2020 Jul 31;11:1163. PMID: 32848771
A-803467 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 Jul 31;11:1163. [Abstract]
A-803467 (25 mg/kg; IP) significantly decreased the heart rate compared to the vehicle+NS (normal saline) group.
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Cell Transplant
Bone marrow mesenchymal stem cells attenuate pain and modulate peripheral sodium channel activity in a rat model of complex regional pain syndrome type I. [Abstract]2025 Jan-Dec:34:9636897251383588. PMID: 41288153
Solvant et solubilité
DMSO : 50 mg/mL (139.75 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, 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 (6.99 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.
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.
Pureté et documentation
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Fiche technique (274 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Anreddy N, et al. A-803467, a tetrodotoxin-resistant sodium channel blocker, modulates ABCG2-mediated MDR in vitro and in vivo. Oncotarget. 2015;6(36):39276-39291. [Content Brief]
[2]. Jarvis MF, et al. A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. Proc Natl Acad Sci U S A. 2007;104(20):8520-8525. [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 | 2.7949 mL | 13.9747 mL | 27.9494 mL | 69.8734 mL |
| 5 mM | 0.5590 mL | 2.7949 mL | 5.5899 mL | 13.9747 mL | |
| 10 mM | 0.2795 mL | 1.3975 mL | 2.7949 mL | 6.9873 mL | |
| 15 mM | 0.1863 mL | 0.9316 mL | 1.8633 mL | 4.6582 mL | |
| 20 mM | 0.1397 mL | 0.6987 mL | 1.3975 mL | 3.4937 mL | |
| 25 mM | 0.1118 mL | 0.5590 mL | 1.1180 mL | 2.7949 mL | |
| 30 mM | 0.0932 mL | 0.4658 mL | 0.9316 mL | 2.3291 mL | |
| 40 mM | 0.0699 mL | 0.3494 mL | 0.6987 mL | 1.7468 mL | |
| 50 mM | 0.0559 mL | 0.2795 mL | 0.5590 mL | 1.3975 mL | |
| 60 mM | 0.0466 mL | 0.2329 mL | 0.4658 mL | 1.1646 mL | |
| 80 mM | 0.0349 mL | 0.1747 mL | 0.3494 mL | 0.8734 mL | |
| 100 mM | 0.0279 mL | 0.1397 mL | 0.2795 mL | 0.6987 mL |
A-803467 Related Classifications
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