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> Phenazopyridine (hydrochloride) [136-40-3]

Phenazopyridine (hydrochloride) [136-40-3]

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Referência HY-B0985-100mg

Tamanho : 100mg

Marca : MedChemExpress

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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.

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Phenazopyridine hydrochloride Chemical Structure

Phenazopyridine hydrochloride Chemical Structure

CAS No. : 136-40-3

This product is a controlled substance and not for sale in your territory.

Based on 2 publication(s) in Google Scholar

Other Forms of Phenazopyridine hydrochloride:

  • Phenazopyridine Obtenir un devis
  • Phenazopyridine hydrochloride (Standard) Obtenir un devis

Voir tous les produits spécifiques à Isoform TRP Channel:

Voir toutes les isoformes
TRPC TRPM TRPV TRPA TRPML
Description

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[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.

Phenazopyridine hydrochloride Related Antibodies

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[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.
Essai clinique
Masse moléculaire

249.70

Formule

C11H12ClN5
CAS No.

136-40-3
Appearance

Solid

Color

Pink to red

SMILES

NC1=NC(N)=CC=C1/N=N/C2=CC=CC=C2.03Cl
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvant et solubilité
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0048 mL 20.0240 mL 40.0481 mL
5 mM 0.8010 mL 4.0048 mL 8.0096 mL
View the 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.

* 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.

  • Calculateur de molarité

  • Calculateur de dilution

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Pureté et documentation

Purity: 99.84%

SDS (419 KB)

COA (248 KB) LCMS (98 KB)

Instruction de manipulation (2659 KB)
Références

  • [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]

  • [1]. Loring H S, et al. Identification of the first noncompetitive SARM1 inhibitors[J]. Bioorganic & Medicinal Chemistry, 2020, 28(18): 115644.

    [2]. Wang C, et al. Phenazopyridine promotes RPS23RG1/Rps23rg1 transcription and ameliorates Alzheimer-associated phenotypes in mice[J]. Neuropsychopharmacology, 2022, 47(12): 2042-2050.

    [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.

    [4]. Luyts N, et al. Inhibition of TRPM8 by the urinary tract analgesic drug phenazopyridine[J]. European Journal of Pharmacology, 2023, 942: 175512.

    [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.

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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Phenazopyridine hydrochloride Related Classifications

  • Membrane Transporter/Ion Channel Neuronal Signaling
  • TRP Channel
Help & FAQs

Keywords:

Phenazopyridine136-40-3TRP ChannelTransient receptor potential channelsSHSY5YN2aCystitisUrethritisUrinary bladderAnalgesiaAlzheimer's diseaseTraumatic brain injuryPeripheral neuropathyNeurodegenerative diseasesHEK293Neuronal differentiationHuman embryonic stem cellsInhibitorinhibitorinhibit

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