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

A-887826 

Cat. No.: HY-100080 Purity: 99.76%
COA Handling Instructions

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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Solution
10 mM * 1 mL in DMSO USD 132 In-stock
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10 mM * 1 mL
ready for reconstitution
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Solid
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10 mg USD 220 In-stock
25 mg USD 470 In-stock
50 mg USD 800 In-stock
100 mg USD 1350 In-stock
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Based on 1 publication(s) in Google Scholar

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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].

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

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].

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

Appearance

Solid

Formula

C26H29ClN4O3

CAS No.
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)

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
10 mM 0.2079 mL 1.0395 mL 2.0790 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.76%

References
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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.

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Product Name:
A-887826
Cat. No.:
HY-100080
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