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

Phenazopyridine 是競爭性的 SARM1 抑制劑， IC50 為 145 μM。Phenazopyridine 是 TRPM8 拮抗劑。Phenazopyridine 具有局部麻醉/止痛作用。Phenazopyridine 用于緩解膀胱炎和尿道炎等疾病的疼痛癥狀。Phenazopyridine 能促進神經(jīng)元分化，還可以用于創(chuàng)傷性腦損傷、周圍神經(jīng)病變和神經(jīng)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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5 mg ￥630
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10 mg ￥1035
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Other Forms of Phenazopyridine:

查看 TRP Channel 亞型特異性產品:

  • 生物活性

  • 純度 & 產品資料

  • 參考文獻

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].
細胞效力
(Cellular Effect)
Cell Line Type Value Description References
BHK-21 CC50
> 20 μM
Compound: 64
cytotoxicity against golden hamster BHK-21 cells incubated for 72 hrs by MTT assay
cytotoxicity against golden hamster BHK-21 cells incubated for 72 hrs by MTT assay
[PMID: 32845145]
LLC-MK2 CC50
> 20 μM
Compound: 64
Cytotoxicity against Rhesus macaque LLC-MK2 cells incubated for 72 hrs by MTT assay
Cytotoxicity against Rhesus macaque LLC-MK2 cells incubated for 72 hrs by MTT assay
[PMID: 32845145]
Vero CC50
> 50 μM
Compound: Phenazopyridine
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
10.1101/2020.03.20.999730
Vero IC50
28 μM
Compound: Phenazopyridine
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
10.1101/2020.03.20.999730
體外研究
(In Vitro)

Phenazopyridine (10-30 μM; 12 h) 在人 SHSY5Y 和小鼠 N2a 細胞中均增加了 RPS23RG1 的 mRNA 的表達[2]。
Phenazopyridine (5-50 μM; 2 分鐘) 在 HEK293 細胞中以濃度依賴和可逆的方式抑制薄荷醇 ( 50 μM) 誘導的 TRPM8 反應，IC50 值為9.6 μM[4]。
Phenazopyridine hydrochloride(3 μM; 6 周) 在人胚胎干細胞中能促進神經(jīng)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.
體內研究
(In Vivo)

Phenazopyridine (15 m/kg; 側腦室注射; 一天一次連續(xù) 2 周) 通過促進 Rps23rg1 的表達來改善阿爾茲海默癥 (AD) APP/PS1小鼠的一些 AD 相關認知障礙和病理[2]。
Phenazopyridine (0.1-3 mg/kg; 靜脈注射；單劑量) 能抑制 Sprague–Dawley 大鼠中機械敏感的 Aδ-纖維，而對 C-纖維無抑制作用[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 號
性狀

固體

顏色

Orange to red

運輸條件

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

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

純度 & 產品資料

純度: 99.93%

參考文獻

  • 摩爾計算器

  • 稀釋計算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   體積   分子量 *
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start) × 體積 (start) = 濃度 (final) × 體積 (final)
× = ×
C1   V1   C2   V2
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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目錄號：
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