1. Phenazopyridine

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.

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Phenazopyridine Chemical Structure

Phenazopyridine Chemical Structure

CAS No. : 94-78-0

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Based on 2 publication(s) in Google Scholar

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Description

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].

In Vitro

Phenazopyridine (10-30 μM; 12 h) increases mRNA expression of RPS23RG1 in both human SHSY5Y and mouse N2a cells[2].
Phenazopyridine (5-50 μM; 2 min) inhibits menthol induced (50 μM) TRPM8 response in a dose-dependent and reversible manner in HEK293 cells with an IC50 of 9.6 μM[4].
Phenazopyridine hydrochloride(3 μM; 6 weeks) can promote neuronal differentiation in human embryonic stem cells[5].

MedChemExpress (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.
In Vivo

Phenazopyridine (15 m/kg; Intracerebroventricularly injection; Once daily for 2 weeks) improves some AD-related cognitive impairment and pathology in Alzheimer's disease (AD) APP/PS1 mice by promoting the expression of Rps23rg1[2].
Phenazopyridine (0.1-3 mg/kg; i.v.; Single dose) can inhibit mechanosensitive Aδ- fibers, but has no inhibitory effect on C-fibers in Sprague - Dawley rats[3].

MedChemExpress (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
Molecular Weight

213.24

Formula

C11H11N5

CAS No.
SMILES

NC1=NC(N)=CC=C1/N=N/C2=CC=CC=C2

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • 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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