2. Membrane Transporter/Ion Channel
  3. P2X Receptor
  4. PSFL2915

PSFL2915 is a selective, orally active P2X receptor inhibitor with oral effectiveness, with an IC50 of 0.319 μM for human P2X3, 0.261 μM for rat P2X2/3, and 13.3 μM for human P2X2. PSFL2915 exhibits ~42-fold selectivity over human P2X2. PSFL2915 can be used for the research of chronic cough.

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PSFL2915

PSFL2915 Chemical Structure

CAS No. : 88134-39-8

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PSFL2915 Related Antibodies

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Description

PSFL2915 is a selective, orally active P2X receptor inhibitor with oral effectiveness, with an IC50 of 0.319 μM for human P2X3, 0.261 μM for rat P2X2/3, and 13.3 μM for human P2X2. PSFL2915 exhibits ~42-fold selectivity over human P2X2. PSFL2915 can be used for the research of chronic cough[1].

In Vitro

PSFL2915 (0.01-3 μM; 0.6 μM; 1 μM) is a noncompetitive, Mg2+-dependent allosteric inhibitor of hP2X3, with ~42-fold selectivity for hP2X3 over hP2X2, potent inhibition of rP2X2/3 heterotrimers, and low activity at other P2X subtypes[1].
PSFL2915 (1 μM) exerts inhibitory effects by targeting the inner pocket of the head domain of hP2X3, as evidenced by potent inhibition of the hP2X4 chimera containing this hP2X3 domain[1].
PSFL2915 (500 nM) prevents the ATP-induced conformational change of the inner pocket of the head domain in hP2X3, which is required for channel activation[1].

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

PSFL2915 Related Antibodies
In Vivo

PSFL2915 (15 mg/kg; i.g.; twice daily; 7 days) produces significant cough-suppressant activity in male C57BL/6 mice with ammonia-induced chronic cough, with potency equivalent to Gefapixant (HY-101588) at the same dose[1].
PSFL2915 (10 mg/kg; i.g.; twice daily; 7 days) produces significant cough-suppressant activity in male Hartley guinea pigs with citric acid/ATP-induced chronic cough, with potency equivalent to Gefapixant (HY-101588) at the same dose[1].
PSFL2915 (15 mg/kg; i.g.; twice daily; 7-10 days) does not impair taste perception in mice, as measured by two-bottle preference tests for bitter and sweet tastants[1].
PSFL2915 (10-20 mg/kg; i.p.) does not impair bitter taste perception in rats, as measured by two-bottle preference testing with quinine[1].

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

Animal Model: C57BL/6 mice (male, 6-7 weeks old)[1]
Dosage: 15 mg/kg
Administration: i.g.; twice daily; 7 days
Result: Significantly reduced cough frequency, with efficacy comparable to Gefapixant (HY-101588) at an equivalent dose.
Animal Model: C57BL/6 mice (male, 6-7 weeks old)[1]
Dosage: 15 mg/kg
Administration: i.g.; twice daily; 7-10 days
Result: Did not alter quinine consumption rate 46.1%.
Did not alter acesulfame-K consumption rate 86.7%.
Molecular Weight

462.36

Formula

C15H10O13S2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1C(O)=C(C2=CC(S(=O)(O)=O)=C(O)C(O)=C2)OC3=C(S(=O)(O)=O)C(O)=CC(O)=C31
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (21.63 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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1628 mL 10.8141 mL 21.6282 mL
5 mM 0.4326 mL 2.1628 mL 4.3256 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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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

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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: ≥ 1 mg/mL (2.16 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: ≥ 1 mg/mL (2.16 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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).
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

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. 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 2.1628 mL 10.8141 mL 21.6282 mL 54.0704 mL
5 mM 0.4326 mL 2.1628 mL 4.3256 mL 10.8141 mL
10 mM 0.2163 mL 1.0814 mL 2.1628 mL 5.4070 mL
15 mM 0.1442 mL 0.7209 mL 1.4419 mL 3.6047 mL
20 mM 0.1081 mL 0.5407 mL 1.0814 mL 2.7035 mL
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PSFL2915 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:

PSFL291588134-39-8PSFL 2915PSFL-2915P2X ReceptorP2XRshuman P2X7P2X receptorhuman P2X2head domain inner pocketC57BL/6 micechronic coughhuman P2X1human P2X4rat P2X2/3human P2X3Inhibitorinhibitorinhibit

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