2. Membrane Transporter/Ion Channel
  3. P2X Receptor
  4. PSB-12062

PSB-12062  (Synonyms: N-(p-Methylphenylsulfonyl)phenoxazine)

Cat. No.: HY-101910 Purity: 98.70%
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PSB-12062 is a potent and selective P2X4 antagonist with an IC50 of 1.38 μM for human P2X4.

For research use only. We do not sell to patients.

PSB-12062 Chemical Structure

PSB-12062 Chemical Structure

CAS No. : 55476-47-6

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 66 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

PSB-12062 Related Antibodies

Top Publications Citing Use of Products

View All P2X Receptor Isoform Specific Products:

View All Isoforms
P2X1 Receptor P2X2 Receptor P2X3 Receptor P2X4 Receptor P2X7 Receptor

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

PSB-12062 is a potent and selective P2X4 antagonist with an IC50 of 1.38 μM for human P2X4.

IC50 & Target

P2X4 Receptor

 

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.76 μM
Compound: PSB12062
Antagonist activity at human P2X4R transfected in HEK293 cells assessed as inhibition of ATP-mediated calcium influx measured after 10 mins by YOPRO-1 dye uptake assay
Antagonist activity at human P2X4R transfected in HEK293 cells assessed as inhibition of ATP-mediated calcium influx measured after 10 mins by YOPRO-1 dye uptake assay
[PMID: 31532206]
In Vitro

PSB-12062 shows similar potency in human, rat, and mouse species. PSB-12062 shows to be allosteric in nature with a 35-fold selectivity toward P2X4 versus P2X1, P2X2, P2X3, and P2X7. However, PSB-12062 is unable to completely block ATP-induced P2X4-mediated calcium influx even when used at high concentrations (>30 μM)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PSB-12062 Related Antibodies
Molecular Weight

337.39

Formula

C19H15NO3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(N1C2=C(C=CC=C2)OC3=CC=CC=C13)(C4=CC=C(C)C=C4)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (74.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9639 mL 14.8196 mL 29.6393 mL
5 mM 0.5928 mL 2.9639 mL 5.9279 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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  • Dilution Calculator

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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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).
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.
Purity & Documentation
References
Kinase Assay
[1]

The competition binding studies are performed in assay buffer (50 mM Tris-HCl, pH 7.4) containing 1 mM EDTA and 0.2 nM [35S]ATPγS. The incubations are started by the addition of membranes (10-15 μg) and are performed in a 250 μL final assay volume. The reactions are terminated by vacuum filtration over GF/ B glass-fiber filters using a Brandell 48-well harvester. The filters are rinsed three times with ice-cold Tris-HCl buffer (50 mM, pH 7.4). The filters are punched out and transferred to 4 mL scintillation vials. Then 2.5 mL of Ultima Gold scintillation cocktail is added, and samples are counted after 6 h for 1 min each, using a liquid scintillation counter (LSC). Nonspecific binding of [35S]ATPγS is determined using 100 μM ATP[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9639 mL 14.8196 mL 29.6393 mL 74.0982 mL
5 mM 0.5928 mL 2.9639 mL 5.9279 mL 14.8196 mL
10 mM 0.2964 mL 1.4820 mL 2.9639 mL 7.4098 mL
15 mM 0.1976 mL 0.9880 mL 1.9760 mL 4.9399 mL
20 mM 0.1482 mL 0.7410 mL 1.4820 mL 3.7049 mL
25 mM 0.1186 mL 0.5928 mL 1.1856 mL 2.9639 mL
30 mM 0.0988 mL 0.4940 mL 0.9880 mL 2.4699 mL
40 mM 0.0741 mL 0.3705 mL 0.7410 mL 1.8525 mL
50 mM 0.0593 mL 0.2964 mL 0.5928 mL 1.4820 mL
60 mM 0.0494 mL 0.2470 mL 0.4940 mL 1.2350 mL
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PSB-12062 Related Classifications

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.

Keywords:

PSB-1206255476-47-6N-(p-Methylphenylsulfonyl)phenoxazinePSB12062PSB 12062P2X ReceptorP2XRsInhibitorinhibitorinhibit

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