2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. A-887826

A-887826 is a potent, selective, oral bioavailable and voltage-dependent Na(v)1.8 sodium channel blocker with an IC50 of 11 nM . A-887826 attenuates neuropathic tactile allodynia in vivo.

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

A-887826 Chemical Structure

A-887826 Chemical Structure

CAS No. : 1266212-81-0

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 132 In-stock
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10 mg USD 220 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

A-887826 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

A-887826 is a potent, selective, oral bioavailable and voltage-dependent Na(v)1.8 sodium channel blocker with an IC50 of 11 nM . A-887826 attenuates neuropathic tactile allodynia in vivo[1].

IC50 & Target[1]

Nav1.8

1.1 nM (IC50)

In Vitro

A-887826 is approximately 3 fold less potent to block Na(v)1.2, approximately 10 fold less potent to block tetrodotoxin-sensitive sodium (TTX-S Na(+)) currents and is >30 fold less potent to block Na(v)1.5 channels[1].
A-887826 potently blocks tetrodotoxin-resistant sodium (TTX-R Na(+)) currents (IC50=8 nM) from small diameter rat dorsal root ganglion (DRG) neurons in a voltage-dependent fashion[1].
A-887826 effectively suppresses evoked action potential firing when DRG neurons are held at depolarized potentials and reversibly suppresses spontaneous firing in small diameter DRG neurons from complete Freund's adjuvant inflamed rats[1].
A-887826 (100 nM) shifts the mid-point of voltage-dependent inactivation of TTX-R currents by approximately 4mV without affecting voltage-dependent activation and do not exhibit frequency-dependent inhibition[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

A-887826 Related Antibodies
In Vivo

A-887826 (3-30 mg/kg; p.o.; 1 hour pre-treatment) significantly attenuates tactile allodynia in a rat neuropathic pain model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Spraguee Dawley rats (200-300 g)[1]
Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration: Oral administration; 1 hour before testing; fourteen days after L5-L6 spinal nerve ligation
Result: Produced a dose-dependent attenuation of tactile allodynia in this experimental pain model.
Molecular Weight

480.99

Formula

C26H29ClN4O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC(C2=CC=C(OCCCC)C(Cl)=C2)=CN=C1)NCC3=CC=CN=C3N4CCOCC4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (519.76 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 2.0790 mL 10.3952 mL 20.7905 mL
5 mM 0.4158 mL 2.0790 mL 4.1581 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, 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.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.08 mg/mL (4.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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:

Dosage

mg/kg

Animal weight
(per animal)

g

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: 99.76%

SDS (479 KB)

COA (246 KB) LCMS (254 KB)

Handling Instructions (2659 KB)
References

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 2.0790 mL 10.3952 mL 20.7905 mL 51.9761 mL
5 mM 0.4158 mL 2.0790 mL 4.1581 mL 10.3952 mL
10 mM 0.2079 mL 1.0395 mL 2.0790 mL 5.1976 mL
15 mM 0.1386 mL 0.6930 mL 1.3860 mL 3.4651 mL
20 mM 0.1040 mL 0.5198 mL 1.0395 mL 2.5988 mL
25 mM 0.0832 mL 0.4158 mL 0.8316 mL 2.0790 mL
30 mM 0.0693 mL 0.3465 mL 0.6930 mL 1.7325 mL
40 mM 0.0520 mL 0.2599 mL 0.5198 mL 1.2994 mL
50 mM 0.0416 mL 0.2079 mL 0.4158 mL 1.0395 mL
60 mM 0.0347 mL 0.1733 mL 0.3465 mL 0.8663 mL
80 mM 0.0260 mL 0.1299 mL 0.2599 mL 0.6497 mL
100 mM 0.0208 mL 0.1040 mL 0.2079 mL 0.5198 mL
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A-887826 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-8878261266212-81-0A887826A 887826Sodium ChannelNa channelsNa+ channelsNa(v)1.8neuropathictactileallodyniaInhibitorinhibitorinhibit

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