Phenazopyridine
Based on 2 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity : 99.93%
- CAS No.: 94-78-0
- Formula: C11H11N5
- Molecular Weight:213.24
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Storage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Phenazopyridine
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Biological Activity
Description
IC50 & Target
EC50: 145 μM (SARM1)[1].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BHK-21 | CC50 |
>20 μM
Compound: 64
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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
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[PMID: 32845145] |
| LLC-MK2 | CC50 |
>20 μM
Compound: 64
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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
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[PMID: 32845145] |
| Vero | CC50 |
>50 μM
Compound: Phenazopyridine
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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
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10.1101/2020.03.20.999730 |
| Vero | IC50 |
28 μM
Compound: Phenazopyridine
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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
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10.1101/2020.03.20.999730 |
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.
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Cell Line:Human ES cells
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Concentration:3 μM
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Incubation Time:6 weeks
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Result:After 10 weeks formed a neural network in the cells.
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Cell Line:Human ES cells
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Concentration:3 μM
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Incubation Time:6 weeks
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Result:Accelerated emergence of early neuronal markers and decreased markers of undifferentiated and non-neural cells.
In Vivo
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.
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Animal Model:C57BL/6 mice model of Alzheimer's disease< sup>[2]
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Dosage:15 mg/kg
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Administration:Intraperitoneal injection (i.p.); Once daily for 2 weeks
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Result:Increased the RPS23RG1 levels in lungs, liver and kidneys of mice.
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Animal Model:APP/PS1 mice model of Alzheimer's disease[2]
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Dosage:15 mg/kg
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Administration:Intracerebroventricularly injection; Once daily for 2 weeks
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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.
Chemical Information
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CAS No. 94-78-0
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Appearance Solid
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Molecular Weight 213.24
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Formula C11H11N5
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Color Yellow to orange
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SMILES
NC1=NC(N)=CC=C1/N=N/C2=CC=CC=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (2)
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Journal Impact Factor
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Most Recent
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Neuropsychopharmacology
Phenazopyridine promotes RPS23RG1/Rps23rg1 transcription and ameliorates Alzheimer-associated phenotypes in mice. [Abstract]2022 Nov;47(12):2042-2050. PMID: 35821069 -
EMBO Rep
2022 Jun 7;23(6):e53932. PMID: 35403787
Solvent & Solubility
In Vitro:
DMSO : 5 mg/mL (23.45 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 0.5 mg/mL (2.34 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 0.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 0.5 mg/mL (2.34 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 0.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Loring H S, et al. Identification of the first noncompetitive SARM1 inhibitors[J]. Bioorganic & Medicinal Chemistry, 2020, 28(18): 115644. [Content Brief]
[2]. Wang C, et al. Phenazopyridine promotes RPS23RG1/Rps23rg1 transcription and ameliorates Alzheimer-associated phenotypes in mice[J]. Neuropsychopharmacology, 2022, 47(12): 2042-2050. [Content Brief]
[3]. Aizawa N, et al. Effects of phenazopyridine on rat bladder primary afferent activity, and comparison with lidocaine and acetaminophen[J]. Neurourology and Urodynamics, 2010, 29(8): 1445-1450. [Content Brief]
[4]. Luyts N, et al. Inhibition of TRPM8 by the urinary tract analgesic drug phenazopyridine[J]. European Journal of Pharmacology, 2023, 942: 175512. [Content Brief]
[5]. Suter, David M et al. Phenazopyridine hydrochlorideinduces and synchronizes neuronal differentiation of embryonic stem cells. Journal of cellular and molecular medicine vol. 13,9B (2009): 3517-27. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.6896 mL | 23.4478 mL | 46.8955 mL | 117.2388 mL |
| 5 mM | 0.9379 mL | 4.6896 mL | 9.3791 mL | 23.4478 mL | |
| 10 mM | 0.4690 mL | 2.3448 mL | 4.6896 mL | 11.7239 mL | |
| 15 mM | 0.3126 mL | 1.5632 mL | 3.1264 mL | 7.8159 mL | |
| 20 mM | 0.2345 mL | 1.1724 mL | 2.3448 mL | 5.8619 mL |
Phenazopyridine Related Classifications
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