A 887826 |
| رقم الكتالوجGC14481 |
887826 عبارة عن مانع قناة صوديوم قوي ، انتقائي ، متاح حيويًا عن طريق الفم ويعتمد على الجهد الكهربائي Na (v) 1.8 مع IC50 يبلغ 11 نانومتر.
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Cas No.: 1266212-81-0
Sample solution is provided at 25 µL, 10mM.
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A 887826 is a potent and voltage-dependent Nav1.8 sodium channel blocker. It blocked recombinant human Nav1.8 channels with an IC50 value of 11nM [1].
Voltage-gated sodium channels are important in the generation and propagation of action potential. At least 9 genes encode functional sodium channels, namely Nav1.1-Nav1.9. Nav1.8 is a TTX-resistant (TTX-R) sodium channel. Nav1.8 is highly localized on primary sensory afferent neurons. Nav1.8 is involved in the processing of nociceptive information.
-100 mV without prepulse did make a resting state for rat DRG neurons. Prepulse to -40 mV did make an inactivated state for channels. In rat DRG neurons in these two states, treatment with A 887826 at 1 µM significantly blocked TTXR Na+ currents. A 887826 blocked TTX-R Na+ currents with an IC50 value of 7.9 ± 0.2 nM (n= 5~9) when channels were in an inactivated state (-40 mV). A 887826 showed an IC50 value of 63.6 ± 0.2 nM (n=5~9) to less depolarized (at -60, -80 or -100 mV) TTX-R Na+ currents. That meant A 887826 state-dependently blocked TTX-R Na+ currents [1].
Knockdown of Nav1.8 caused a significant reduction in mechanical hyperalgesia and allodynia in rat models of inflammatory and neuropathic pain. Suppression of Nav1.8 expression also reduced visceral pain in several experimental models. Activation of Nav1.8 sodium channels primarily drove nociceptor excitability under cold conditions. A rat spinal nerve ligation model of neuropathic pain was used. Oral administration with A 887826 dose-dependently attenuated tactile allodynia in this pain model. The range of free plasma concentrations of A 887826 to produce analgesic efficacy in a spinal nerve ligation model was 3-10 nM. This was consistent with the IC50 value for blocking rat DRG TTX-R sodium currents [1].
Reference:
[1]. Zhang XF, Shieh CC, Chapman ML, et al. A-887826 is a structurally novel, potent and voltage-dependent NaV1.8 sodium channel blocker that attenuates neuropathic tactile allodynia in rats. Neuropharmacology, 2010, 59(3): 201-207.
| Cas No. | 1266212-81-0 | SDF | |
| Chemical Name | 5-(4-butoxy-3-chlorophenyl)-N-((2-morpholinopyridin-3-yl)methyl)nicotinamide | ||
| Canonical SMILES | ClC1=CC(C2=CN=CC(C(NCC3=CC=CN=C3N4CCOCC4)=O)=C2)=CC=C1OCCCC | ||
| Formula | C26H29ClN4O3 | M.Wt | 480.99 |
| الذوبان | <24.05mg/ml in DMSO | Storage | Store at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.079 mL | 10.3952 mL | 20.7905 mL |
| 5 mM | 0.4158 mL | 2.079 mL | 4.1581 mL |
| 10 mM | 0.2079 mL | 1.0395 mL | 2.079 mL |
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- Purity: >98.00%
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