2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. DA-0218

DA-0218 是一种 Nav1.7 抑制剂。DA-0218 可产生状态依赖性抑制作用。DA-0218 可减轻小鼠的福尔马林诱导炎性痛行为及 Paclitaxel 诱导机械性痛觉过敏。DA-0218 抑制小鼠的 Histamine 诱导急性瘙痒及淋巴瘤诱导慢性瘙痒。DA-0218 可用于炎性疼痛、神经病理性疼痛、急性瘙痒及慢性瘙痒的相关研究。

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DA-0218

DA-0218 Chemical Structure

CAS No. : 1081317-31-8

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DA-0218 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DA-0218 is a Nav1.7 inhibitor. DA-0218 exerts state-dependent inhibitory effects. DA-0218 alleviates formalin-induced inflammatory pain behavior and Paclitaxel-induced mechanical hyperalgesia in mice. DA-0218 inhibits Histamine-induced acute pruritus and lymphoma-induced chronic pruritus in mice. DA-0218 can be used in research related to inflammatory pain, neuropathic pain, acute pruritus and chronic pruritus[1][2].

IC50 & Target[1]

Nav1.7

 

体外研究
(In Vitro)

DA-0218 (Compound 9) (0.01-10 μM; 14 min) 可强效抑制表达 Nav1.7 的 HEK293 细胞中 Nav1.7 介导的钠电流，其 IC50 为 0.74 μM，且对表达 Nav1.5 的 HEK293 细胞无活性[1]。
DA-0218 (10 μM) 对人 DRG 神经元的瞬时钠电流产生中等程度的抑制作用，在 10 μM 时可使峰值电流降低 22%[1]。
DA-0218 (10 μM; up to 14 min incubation and recording) 可使经 Paclitaxel (HY-B0015) 预处理的小鼠小直径背根神经节神经元的瞬时钠电流峰值抑制 44%[2]。
DA-0218 (10 μM; up to 14 min incubation and recording) 可将小直径人背根神经节神经元的瞬时钠电流峰值抑制 22%[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

DA-0218 相关抗体:
体内研究
(In Vivo)

DA-0218 (鞘内注射 3-30 nM；腹腔注射 30 mg/kg；足底注射 60 nM；一次) 可强效抑制小鼠中福尔马林诱导的炎性疼痛，在最高鞘内剂量下可使 II 期疼痛缓解达 80%[2]。
DA-0218 (10-30 nM；鞘内注射；10-30 mg/kg；腹腔注射；一次) 可短暂逆转小鼠体内 Paclitaxel 诱导的机械性痛觉过敏，但重复给药会产生急性耐受，且腹腔给药无效果[2]。
DA-0218 (鞘内注射，3-30 nM) 可抑制 Histamine (HY-B1204) 诱导的小鼠急性瘙痒[2]。
DA-0218 (鞘内注射，30 nM) 可强效抑制小鼠淋巴瘤诱导的慢性瘙痒，作用持续时间至少达 5 h[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (male and female; formalin-induced inflammatory pain model)[2]
Dosage: 3; 10; 30 nM (i.t.); 30 mg/kg (i.p.); 60 nM (i.pl.)
Administration: i.t.; i.p.; i.pl.; single administration
Result: Produced dose-dependent inhibition of formalin-induced phase II pain by up to 80%.
Reduced phase I pain at the 30 nmol i.t. dose.
Inhibited phase II pain by 76% at 30 mg/kg i.p..
Significantly reduced phase II pain at 60 nmol i.pl..
Animal Model: C57BL/6 (male and female; paclitaxel-induced neuropathic pain model)[2]
Dosage: 10; 20 ; 30 nM (i.t.); 10; 30 mg/kg (i.p.)
Administration: i.t.; i.p.; single administration
Result: Transiently but completely reversed paclitaxel-induced mechanical allodynia at 1 h and 3 h post-injection in a dose-dependent manner.
Showed no effect on mechanical allodynia at 5 h post-injection.
Resulted in acute tolerance after repeated intrathecal injections of 20 nmol, with no analgesic effect after the second and third injections.
Had no effect on mechanical allodynia at 10 mg/kg and 30 mg/kg i.p..
Animal Model: C57BL/6 (male and female; histamine-induced acute itch model)[2]
Dosage: 3; 10 ; 30 nM
Administration: i.t.; single administration
Result: Produced a dose-dependent reduction in histamine-induced scratch bouts.
Resulted in a statistically significant reduction in total scratches over 30 min at the 30 nmol dose compared to vehicle.
Animal Model: NOD.CB-17-Prkdcscid (male; 8 to 10 weeks old; lymphoma-induced chronic itch model)[2]
Dosage: 30 nM (i.t.)
Administration: i.t.; single administration
Result: Produced a profound reduction in lymphoma-induced chronic scratch bouts at 1 h, 3 h, and 5 h post-injection.
Maintained statistically significant effects through 5 h post-injection.
分子量

543.70

Formula

C36H37N3O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

DA-0218 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DA-02181081317-31-8DA0218DA 0218Sodium ChannelNa channelsNa+ channelschronic itchneuropathic painhuman DRG neuronsinflammatory painNav1.5paclitaxel-pretreated neuronsHEK293 cellsacute itchdorsal root ganglion neuronsNav1.7Inhibitorinhibitorinhibit

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