A-803467

Name: A-803467
Brand: MedChemExpress
SKU: HY-11079
Rating: 5.0 (2 reviews)

Cat. No.: HY-11079 Purity: 99.09%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

A-803467 Chemical Structure

CAS No. : 944261-79-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 38	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 230	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 370	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE A-803467

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View All Sodium Channel Isoform Specific Products:

View All Isoforms

Na_v1.1 Na_v1.2 Na_v1.3 Na_v1.4 Na_v1.5 Na_v1.6 Na_v1.7 Na_v1.8

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]^[2]

Na_v1.8

8 nM (IC₅₀)

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 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: 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	0.079 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: 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	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	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.

Molecular Weight

357.79

Formula

C₁₉H₁₆ClNO₄

CAS No.

944261-79-4

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.09%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (247 KB) LCMS (277 KB)

Handling Instructions (2659 KB)

References

[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

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

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

A-803467944261-79-4A803467A 803467Sodium ChannelNa channelsNa+ channelspotentselectivetetrodotoxin-resistantNav1.8sodiumchannelanti-nociceptionneuropathicinflammatoryInhibitorinhibitorinhibit

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A-803467

Customer Review

A-803467 Related Antibodies

2 Publications Citing Use of MCE A-803467

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•Related Screening Libraries:

•Related Small Molecules:

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View All Sodium Channel Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

A-803467 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

A-803467 Related Classifications

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