| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| Other Sizes |
|
| ln Vitro |
Blocking Na(v)1.2 is about three times less effective with A-887826, blocking tetrodotoxin-sensitive sodium (TTX-S Na(+)) currents is around ten times less effective, and blocking Na(v)> 30 times)1.5 channels is about ten times less effective[1]. In a voltage-dependent manner (IC50=8 nM), A-887826 potently inhibits tetrodotoxin-resistant sodium (TTX-R Na(+)) currents from small-diameter rat dorsal root ganglion (DRG) neurons[1]. In rats given Freund's adjuvant-induced inflammation, A-887826 reversibly inhibits the spontaneous firing of small-diameter DRG neurons and effectively blocks evoked action potential discharges when DRG neurons maintain depolarizing potentials [1]. Without altering voltage-dependent activation, A-887826 (100 nM) shifts the midpoint of voltage-dependent inactivation of TTX-R currents by around 4 mV and does not show frequency-dependent inhibition [1].
|
|---|---|
| ln Vivo |
In a rat neuropathic pain model, A-887826 (3–30 mg/kg; oral; 1 hour before treatment) effectively improves tactile allodynia [1].
|
| Animal Protocol |
Animal/Disease Models: Male Spraguee Dawley rat (200-300 g) [1]
Doses: 3 mg/kg, 10 mg/kg, 30 mg/kg Route of Administration: oral; Route of Administration: oral. 1 hour before testing; Fourteen days after L5-L6 spinal nerve ligation Experimental Results: A dose-dependent attenuation of tactile allodynia was produced in this experimental pain model. |
| References |
| Molecular Formula |
C₂₆H₂₉CLN₄O₃
|
|---|---|
| Molecular Weight |
480.99
|
| Exact Mass |
480.193
|
| CAS # |
1266212-81-0
|
| PubChem CID |
46919335
|
| Appearance |
White to off-white solid powder
|
| LogP |
5.382
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
34
|
| Complexity |
621
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
JPJGFWKHSMUKFO-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C26H29ClN4O3/c1-2-3-11-34-24-7-6-19(15-23(24)27)21-14-22(17-28-16-21)26(32)30-18-20-5-4-8-29-25(20)31-9-12-33-13-10-31/h4-8,14-17H,2-3,9-13,18H2,1H3,(H,30,32)
|
| Chemical Name |
5-(4-butoxy-3-chlorophenyl)-N-[(2-morpholin-4-ylpyridin-3-yl)methyl]pyridine-3-carboxamide
|
| Synonyms |
A887826; A 887826
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~519.76 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.32 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
