{{cart_num}}
My CartCAS：944261-79-4
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
Qty：
Size：
| CAS | 944261-79-4 |
| Name | A-803467 |
| Molecular Formula | C19H16ClNO4 |
| Molecular Weight | 357.79 |
| Solubility | Soluble in DMSO ≥5mg/mL(Need ultrasonic) |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD01860946 |
| SMILES | O=C(C1=CC=C(C2=CC=C(Cl)C=C2)O1)NC3=CC(OC)=CC(OC)=C3 |
| Target Point | Sodium Channel |
| Passage | Membrane Transporter&Ion Channel |
| Background | A-803467 is a selective NaV1.8 channel inhibitor. |
| Biological Activity | A-803467是一种选择性NaV1.8 channel抑制剂，IC50为8 nM，抑制抗河豚毒的电流，比作用于人类NaV1.2， NaV1.3， NaV1.5和NaV1.7选择性高100倍以上。[1-2] |
| In Vitro | A-803467有效阻挡重组人类或大鼠Nav1.8 通道，IC50分别为8 nM 和45 nM，保持-40 mV电位。处于静息电位时，A-803467也有效阻断人类Nav1.8 通路，IC50为79 nM。A-803467作用于大鼠背根神经节神经元阻断抗Tetrodotoxin(TTX-R)的电流，这种作用存在浓度依赖性，IC50为140 nM，比Mexiletine和 Lamotrigine(IC50>30 μM)更有效。A-803467作用于hNav1.8 比作用于hNav1.2，hNav1.3，hNav1.5，和hNav1.7通道选择性高300到1000倍，IC50分别为7.38 μM，2.45 μM，7.34 μM，和6.74 μM。A-803467作用于周围感觉神经元通道和受体，包括TRPV1，P2X2/3，Cav2.2 和KCNQ2/3 通道，没有显著活性，IC50>10 μM。A-803467为0.3 μM而不是0.1 μM 时，显著抑制自发和电刺激诱发的动作电位产生。[1] |
| In Vivo | 与体外作用于神经元动作电位的产电一致，A-803467 按20 mg/kg剂量静脉注射给药脊神经结扎大鼠，显著降低自发的和von Frey hair 诱发的脊髓背角宽动态范围神经元，分别降低66%和53%。A-803467作用于多种大鼠疼痛模型，包括脊神经结扎(ED50 = 47 mg/kg，腹腔注射)，坐骨神经损伤(ED50 = 85 mg/kg，腹腔注射)，辣椒素引起的继发性机械性异常疼痛(ED50 ≈100 mg/kg，腹腔注射)，和足底完全注射Freund 佐剂后引起热痛觉过敏(ED50 = 41 mg/kg，腹腔注射)，也降低机械痛，这种作用存在剂量依赖性。A-803467对福尔马林诱导的伤害和急性热和术后疼痛，以及化疗引起的疼痛模型(Vincristine)没有作用活性。[1] |
| Cell Experiment | Animal Models: 脊髓神经结扎，坐骨神经损伤，辣椒素引起的继发性机械性异常疼痛，或足底完全注射Freund佐剂后引起热痛觉过敏的雄性Sprague-Dawley大鼠，及雄性CD1小鼠; Dosages: ~100 mg/kg; Administration: 行为测验前30分钟腹腔注射[1] |
| Data Literature Source | [1] Jarvis MF，et al. Proc Natl Acad Sci U S A，2007，104(20)，8520-8525. [2] Joshi SK，et al. J Pain，2009，10(3)，306-315. |
| Unit | Bottle |
| Specification | 5mg 10mg |
是一种选择性NaV1.8 channel抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
Sorry, there is no more information.
Manual Download
