Phenazopyridine hydrochloride
Based on 2 publication(s) in Google Scholar
Phenazopyridine hydrochlorideis a competitive SARM1 inhibitor, with IC50 145 μM. Phenazopyridine hydrochlorideis a TRPM8 antagonist. Phenazopyridine hydrochloride has a local anesthetic/analgesic effect. Phenazopyridine hydrochlorideis used to relieve painful symptoms of conditions such as cystitis and urethritis. Phenazopyridine hydrochloridecan 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: 99.55%
- CAS No.: 136-40-3
- Formula: C11H12ClN5
- Molecular Weight:249.70
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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
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Publications Citing Use of MedChemExpress (MCE) Phenazopyridine hydrochloride
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Biological Activity
EC50: 145 μM (SARM1)[1].
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.
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[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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 136-40-3
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Appearance Solid
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Molecular Weight 249.70
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Formula C11H12ClN5
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Color Pink to red
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SMILES
NC1=NC(N)=CC=C1/N=N/C2=CC=CC=C2.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
DMSO : 25 mg/mL (100.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 1 mg/mL (4.00 mM; ultrasonic and warming and heat to 60°C)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.5 mg/mL (10.01 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (10.01 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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 (sealed storage, away from moisture)
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 (280 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 4.0048 mL | 20.0240 mL | 40.0481 mL | 100.1201 mL |
| DMSO | 5 mM | 0.8010 mL | 4.0048 mL | 8.0096 mL | 20.0240 mL |
| 10 mM | 0.4005 mL | 2.0024 mL | 4.0048 mL | 10.0120 mL | |
| 15 mM | 0.2670 mL | 1.3349 mL | 2.6699 mL | 6.6747 mL | |
| 20 mM | 0.2002 mL | 1.0012 mL | 2.0024 mL | 5.0060 mL | |
| 25 mM | 0.1602 mL | 0.8010 mL | 1.6019 mL | 4.0048 mL | |
| 30 mM | 0.1335 mL | 0.6675 mL | 1.3349 mL | 3.3373 mL | |
| 40 mM | 0.1001 mL | 0.5006 mL | 1.0012 mL | 2.5030 mL | |
| 50 mM | 0.0801 mL | 0.4005 mL | 0.8010 mL | 2.0024 mL | |
| 60 mM | 0.0667 mL | 0.3337 mL | 0.6675 mL | 1.6687 mL | |
| 80 mM | 0.0501 mL | 0.2503 mL | 0.5006 mL | 1.2515 mL | |
| 100 mM | 0.0400 mL | 0.2002 mL | 0.4005 mL | 1.0012 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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