| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| A409222-1ml |
1ml |
现货  |
|
| 英文别名 | 5-(4-chlorophenyl)-N-(3,5-dimethoxyphenyl)furan-2-carboxamide |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | A-803467 |
| 生化机理 | A-803467 是一种选择性NaV1.8 通道阻断剂，IC50 为 8 nM，可阻断河豚毒素抗性电流，对人类NaV1.2、NaV1.3、NaV1.5 和NaV1.7 的选择性大于 100 倍。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 通道阻滞剂 |
| 作用机制 | Na 通道阻断器 v1.8 |
| 产品介绍 |
A-803467能够抑制感觉神经元的自发和诱发动作电位。它具有镇痛作用。A-803467能够在体内减少脊髓背角神经元的放电。 小分子A-803467是一种有效的选择性Nav1.8钠离子通道阻滞剂。Nav1.8是一种抗河豚毒素（TTX-R）钠离子通道，通过在周围感觉神经元中传递疼痛刺激而产生痛觉；A-803467通过阻滞该通道，能够对多种模型产生不同程度的疼痛减轻作用。A-803467已被用于进一步探究Nav1.8在传递疼痛刺激中的作用. Information A-803467 A-803467 is a selective Na V 1.8 channel blocker with IC50 of 8 nM, blocks tetrodotoxin-resistant currents, exhibits >100-fold selectivity against human Na V 1.2, Na V 1.3, Na V 1.5, and Na V 1.7. A-803467 potently blocks recombinant human or rat NaV1.8 channels with IC50 of 8 nM and 45 nM, respectively, at a holding potential of -40 mV. At a resting state, A-803467 also potently blocks human NaV1.8 channels with IC50 of 79 nM. A-803467 blocks tetrodotoxin-resistant (TTX-R) currents in rat dorsal root ganglion neurons in a concentration-dependent manner with IC50 of 140 nM, more potently compared with both mexiletine and lamotrigine with IC50 of >30 μM. A-803467 displays 300- to 1,000-fold higher selectivity for hNaV1.8 over hNaV1.2, hNaV1.3, hNaV1.5, and hNaV1.7 channels with IC50 of 7.38 μM, 2.45 μM, 7.34 μM, and 6.74 μM, respectively. A-803467 shows no significant activity against other channels and receptors expressed in peripheral sensory neurons including TRPV1, P2X2/3, CaV2.2 and KCNQ2/3 channels with IC50 >10 μM. A-803467 also shows no or weak activity against a broad screening panel of cell-surface receptors, ion channels, and enzymes with IC50 of >2 μM. A-803467 at 0.3 μM but not 0.1 μM significantly inhibits the generation of spontaneous and electrically evoked action potentials. In vivo Consistent with its effects on neuronal action potential electrogenesis in vitro, systemic administration of A-803467 (20 mg/kg, i.v.) to spinal nerve ligated rats, significantly reduces both spontaneous and von Frey hairevoked firing of spinal dorsal horn wide dynamic range neurons by 66% and 53%, respectively, compared with baseline levels. Administration of A-803467 also dose-dependently reduces mechanical allodynia in a variety of rat pain models including spinal nerve ligation (ED50 = 47 mg/kg, i.p.), sciatic nerve injury (ED50 = 85 mg/kg, i.p.), capsaicin-induced secondary mechanical allodynia (ED50 ≈ 100 mg/kg, i.p.), and thermal hyperalgesia after intraplantar complete Freund\'s adjuvant injection (ED50 = 41 mg/kg, i.p.). A-803467 is inactive against formalin-induced nociception and acute thermal and postoperative pain, as well as in a chemotherapy-induced pain model (vincristine). cell lines： Concentrations： Incubation Time： Powder Purity:≥99% |
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | COC1=CC(=CC(=C1)NC(=O)C2=CC=C(O2)C3=CC=C(C=C3)Cl)OC |
| 分子量 | 357.79 |
| Reaxy-Rn | 15782387 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=15782387&ln= |
| 象形图 | GHS07 |
|---|---|
| 信号词 | Warning |
| 危险声明 |
H302: 吞食有害 |
| 预防措施声明 |
P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P330: 漱口 P301+P317: 如果被吞咽：请寻求医疗帮助。 |
| WGK Germany | 3 |
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