Art. -Nr.: HY-11079

A-803467

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

A-803467 is a potent and selective tetrodotoxin-resistant Na_v1.8 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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Reinheit: 99.69%
CAS. Nr.: 944261-79-4
Formel: C₁₉H₁₆ClNO₄
Molecular Weight:357.79

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

A-803467 Chemical Structure

CAS. Nr.: 944261-79-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]^[2]

Na_v1.8

8 nM (IC₅₀)

Alle Sodium Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	>30 μM Compound: 27	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	[PMID: 18176998]
HEK293	IC₅₀	0.008 μM Compound: A-803467	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	[PMID: 17483457]
HEK293	IC₅₀	0.008 μM Compound: A-803467	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	[PMID: 20965738]
HEK293	IC₅₀	0.008 μM Compound: 27	Inhibition of human recombinant Nav 1.8 channel expressed in HEK293 cells Inhibition of human recombinant Nav 1.8 channel expressed in HEK293 cells	[PMID: 18176998]
HEK293	IC₅₀	0.079 μM Compound: A-803467	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	[PMID: 17483457]
HEK293	IC₅₀	0.85 μM Compound: 27	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	[PMID: 18176998]
HEK293	IC₅₀	0.85 μM Compound: A-803467	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	[PMID: 20965738]
HEK293	IC₅₀	11.76 μM Compound: A-803467	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	[PMID: 17483457]
HEK293	IC₅₀	2.45 μM Compound: A-803467	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	[PMID: 17483457]
HEK293	IC₅₀	32.82 μM Compound: A-803467	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	[PMID: 17483457]
HEK293	IC₅₀	35.34 μM Compound: A-803467	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	[PMID: 17483457]
HEK293	IC₅₀	6.74 μM Compound: A-803467	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	[PMID: 17483457]
HEK293	IC₅₀	7.34 μM Compound: A-803467	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	[PMID: 17483457]
HEK293	IC₅₀	7.38 μM Compound: A-803467	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	[PMID: 17483457]
HEK293	IC₅₀	8 nM Compound: A-803467	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	[PMID: 17483457]
HEK293	IC₅₀	9.49 μM Compound: A-803467	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	[PMID: 17483457]

In Vitro

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.

In Vivo

A-803467 (35 mg/kg; p.o.) shows no noticeable toxicity in the male NCR nude mice^[1].
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.

Animal Model:

Nude mice^[1]
Dosage:

35 mg/kg
Administration:

P.o.
Result:

Showed no noticeable toxicity in the male NCR nude mice.

Chemical Information

CAS. Nr. 944261-79-4
Appearance Solid
Molecular Weight 357.79
Formel C₁₉H₁₆ClNO₄
Color White to light yellow
SMILES

O=C(C1=CC=C(C2=CC=C(Cl)C=C2)O1)NC3=CC(OC)=CC(OC)=C3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (3)

All Bio/Physico-chemical AssayIn Vivo Efficacy Study

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Journal Impact Factor

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.
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.
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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7949 mL

13.9747 mL

27.9494 mL

5 mM

0.5590 mL

2.7949 mL

5.5899 mL

10 mM

0.2795 mL

1.3975 mL

2.7949 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.99 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

A-803467

3 Cited Publications

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A-803467

Immunology/Inflammation Compound Library

Membrane Transporter/Ion Channel Compound Library

Anti-Cancer Compound Library

Neuroprotective Compound Library

Lipid Metabolism Compound Library

Targeted Diversity Library

Sodium Channel Blocker Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Anti-Drug-Resistant Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) A-803467

Alle Sodium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

A-803467

Immunology/Inflammation Compound Library

Membrane Transporter/Ion Channel Compound Library

Anti-Cancer Compound Library

Neuroprotective Compound Library

Lipid Metabolism Compound Library

Targeted Diversity Library

Sodium Channel Blocker Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Anti-Drug-Resistant Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) A-803467

Alle Sodium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

A-803467 Related Classifications

HY-11079 Related Classifications