1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. TRP Channel
  3. Phenazopyridine

Phenazopyridine 是竞争性的 SARM1 抑制剂, IC50 为 145 μM。Phenazopyridine 是 TRPM8 拮抗剂。Phenazopyridine 具有局部麻醉/止痛作用。Phenazopyridine 用于缓解膀胱炎和尿道炎等疾病的疼痛症状。Phenazopyridine 能促进神经元分化,还可以用于创伤性脑损伤、周围神经病变和神经退行性疾病的研究。

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Phenazopyridine Chemical Structure

Phenazopyridine Chemical Structure

CAS No. : 94-78-0

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生物活性

Phenazopyridine is a competitive SARM1 inhibitor, with IC50 145 μM. Phenazopyridine is a TRPM8 antagonist. Phenazopyridine has a local anesthetic/analgesic effect. Phenazopyridine is used to relieve painful symptoms of conditions such as cystitis and urethritis. Phenazopyridine can promote neuronal differentiation and can also be used in the study of traumatic brain injury, peripheral neuropathy and neurodegenerative diseases[1][2][3][4][5].

IC50 & Target

EC50: 145 μM (SARM1)[1].

体外研究
(In Vitro)

Phenazopyridine (10-30 μM; 12 h) 在人 SHSY5Y 和小鼠 N2a 细胞中均增加了 RPS23RG1 的 mRNA 的表达[2]
Phenazopyridine (5-50 μM; 2 分钟) 在 HEK293 细胞中以浓度依赖和可逆的方式抑制薄荷醇 ( 50 μM) 诱导的 TRPM8 反应,IC50 值为9.6 μM[4]
Phenazopyridine hydrochloride(3 μM; 6 周) 在人胚胎干细胞中能促进神经元分化[5]

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

Cell Differentiation Assay[5].

Cell Line: Human ES cells
Concentration: 3 μM
Incubation Time: 6 weeks
Result: After 10 weeks formed a neural network in the cells.

RT-PCR[5].

Cell Line: Human ES cells
Concentration: 3 μM
Incubation Time: 6 weeks
Result: Accelerated emergence of early neuronal markers and decreased markers of undifferentiated and non-neural cells.
体内研究
(In Vivo)

Phenazopyridine (15 m/kg; 侧脑室注射; 一天一次连续 2 周) 通过促进 Rps23rg1 的表达来改善阿尔兹海默症 (AD) APP/PS1小鼠的一些 AD 相关认知障碍和病理[2]
Phenazopyridine (0.1-3 mg/kg; 静脉注射;单剂量) 能抑制 Sprague–Dawley 大鼠中机械敏感的 Aδ-纤维,而对 C-纤维无抑制作用[3]

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

Animal Model: C57BL/6 mice model of Alzheimer's disease< sup>[2]
Dosage: 15 mg/kg
Administration: Intraperitoneal injection (i.p.); Once daily for 2 weeks
Result: Increased the RPS23RG1 levels in lungs, liver and kidneys of mice.
Animal Model: APP/PS1 mice model of Alzheimer's disease[2]
Dosage: 15 mg/kg
Administration: Intracerebroventricularly injection; Once daily for 2 weeks
Result: Significantly reduced amyloid plaques.
Increased protein levels of RPS23RG1, PSD-95, and phosphorylated/inactivated GSK-3β, though without affecting levels of tau, phosphorylated tau, and p35.
Clinical Trial
分子量

213.24

Formula

C11H11N5

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
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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.

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