AZ194是一种 CRMP2-Ubc9 抑制剂和 NaV1.7 抑制剂 (IC50=1.2 μM),具有口服活性。AZ194抑制 CRMP2 的 Sumoylation,减少NaV1.7的表达,具有一定抗伤害作用。
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产品名称 | Sodium Channel ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Tolperisone HCl | ✔ | 99% | |||||||||||||||||
Lamotrigine | ✔ | 98% | |||||||||||||||||
Vinpocetine | ✔ | 98% | |||||||||||||||||
Zonisamide | ✔ | 99% | |||||||||||||||||
Dronedarone Hydrochloride | ✔ | 95% | |||||||||||||||||
Procainamide hydrochloride | ✔ | 99% | |||||||||||||||||
Bupivacaine HCl | ✔ | 99+% | |||||||||||||||||
Benzocaine | ✔ | 98% | |||||||||||||||||
Carbamazepine |
++
Sodium channel, IC50: 131 μM |
98% | |||||||||||||||||
Quinidine sulfate dihydrate | ✔ | 98% | |||||||||||||||||
Ibutilide fumarate | ✔ | 99%+ | |||||||||||||||||
Dibucaine HCl | ✔ | 99+% | |||||||||||||||||
Mexiletine HCl | ✔ | 99% | |||||||||||||||||
Phenytoin | ✔ | 99+% | |||||||||||||||||
Camostat Mesylate |
+++
epithelial sodium channel (ENaC), IC50: 50 nM |
99%+ | |||||||||||||||||
Levobupivacaine | ✔ | 97+% | |||||||||||||||||
Oxcarbazepine |
+
sodium channel, IC50: 160 μM |
98% | |||||||||||||||||
Ambroxol | 98+% | ||||||||||||||||||
Primidone | ✔ | 99% | |||||||||||||||||
Propafenone | ✔ | 99% | |||||||||||||||||
A-803467 |
++++
Na(V1.8) channel, IC50: 8 nM |
99%+ | |||||||||||||||||
Rufinamide | ✔ | 99% | |||||||||||||||||
Phenytoin sodium | ✔ | 98% | |||||||||||||||||
Proparacaine Hydrochloride |
+
Voltage-gated sodium channel, ED50: 3.4 mM |
98+% | |||||||||||||||||
Riluzole | ✔ | 97% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | AZ194 is a pioneering, orally administered inhibitor that disrupts the CRMP2-Ubc9 interaction and inhibits NaV1.7 with an IC50 of 1.2 µM. It prevents the SUMOylation of CRMP2, effectively decreasing the amount of NaV1.7 expressed on the cell surface and provides antinociceptive effects[1]. |
体内研究 | AZ194 offers pain relief in rat models of chemotherapy-induced and nerve injury-induced neuropathic pain. Administered orally at doses of 2 and 10 mg/kg, AZ194 restores mechanical sensitivity in animals experiencing neuropathic nociception from these conditions[1]. AZ194, given at 10 mg/kg intraperitoneally to CD1 male mice, does not impact motor performance in an open field test. It enhances the efficacy of commonly used painkillers and activates NaV1.7-dependent endogenous opioid signaling[1]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.76mL 0.35mL 0.18mL |
8.81mL 1.76mL 0.88mL |
17.62mL 3.52mL 1.76mL |
CAS号 | 2241651-99-8 |
分子式 | C34H31F2N3O3 |
分子量 | 567.625 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,2-8°C |
溶解方案 |
DMSO: 35 mg/mL(61.66 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |