2. Membrane Transporter/Ion Channel
  3. P2X Receptor
  4. AF-353

AF-353 (Ro-4) is a potent, selective and orally bioavailable P2X3/P2X2/3 receptor antagonist, with a pIC50 of 8.0 for both human and rat P2X3, and with a pIC50 of 7.3 for human P2X2/3.

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

AF-353 Chemical Structure

AF-353 Chemical Structure

CAS No. : 865305-30-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 96 In-stock
Solution
10 mM * 1 mL in DMSO USD 96 In-stock
Solid
1 mg USD 41 In-stock
5 mg USD 88 In-stock
10 mg USD 155 In-stock
25 mg USD 310 In-stock
50 mg USD 435 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

AF-353 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE AF-353

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  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

AF-353 (Ro-4) is a potent, selective and orally bioavailable P2X3/P2X2/3 receptor antagonist, with a pIC50 of 8.0 for both human and rat P2X3, and with a pIC50 of 7.3 for human P2X2/3[1][2].

IC50 & Target

pIC50: 8.0 (human P2X3), 8.0 (rat P2X3), 7.3 (human P2X2/3)[1]
In Vitro

AF-353 (Ro-4) is a highly potent inhibitor of α,β-meATP-evoked intracellular calcium flux in cell lines expressing recombinant rat and human P2X3 and human P2X2/3 channels[1].
AF-353 (Ro-4) also blocks human P2X2/3 channel function with marginally reduced potency with a p50 of 7.3[1].

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

AF-353 Related Antibodies
In Vivo

AF-353 (Ro-4) does not compromise oxygen levels or cardiac function[2].
AF-353 (Ro-4) (10 mg/kg, 20 mg/kg; i.v.; for 4-6 hours) inhibits the purinergic response in both normal and spinal cord-injured (SCI) rats[2].
AF-353 (Ro-4) (10 mg/kg, 20 mg/kg; i.v.; for 4-6 hours) also reduces the inter-contractile interval in normal but not in SCI rats; however, the frequency of non-voiding (NVC) in SCI rats is significantly reduced[2].

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

Animal Model: Female Sprague-Dawley rats (250–300 g) bearing SCI[2]
Dosage: 10 mg/kg, 20 mg/kg
Administration: Intravenous injection; interval of 90 minutes, for 4 hours to 6 hours
Result: Significantly reduced purinergic response in both normal and SCI rats.
Molecular Weight

400.21

Formula

C14H17IN4O2
CAS No.
Appearance

Solid

Color

Light brown to brown

SMILES

CC(C)C1=C(OC2=CN=C(N)N=C2N)C=C(I)C(OC)=C1
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 : 83.33 mg/mL (208.22 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 2.4987 mL 12.4934 mL 24.9869 mL
5 mM 0.4997 mL 2.4987 mL 4.9974 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.

  • 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

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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: ≥ 2.5 mg/mL (6.25 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 (6.25 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).
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

Purity: 99.53%

COA (247 KB) HNMR (241 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
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 2.4987 mL 12.4934 mL 24.9869 mL 62.4672 mL
5 mM 0.4997 mL 2.4987 mL 4.9974 mL 12.4934 mL
10 mM 0.2499 mL 1.2493 mL 2.4987 mL 6.2467 mL
15 mM 0.1666 mL 0.8329 mL 1.6658 mL 4.1645 mL
20 mM 0.1249 mL 0.6247 mL 1.2493 mL 3.1234 mL
25 mM 0.0999 mL 0.4997 mL 0.9995 mL 2.4987 mL
30 mM 0.0833 mL 0.4164 mL 0.8329 mL 2.0822 mL
40 mM 0.0625 mL 0.3123 mL 0.6247 mL 1.5617 mL
50 mM 0.0500 mL 0.2499 mL 0.4997 mL 1.2493 mL
60 mM 0.0416 mL 0.2082 mL 0.4164 mL 1.0411 mL
80 mM 0.0312 mL 0.1562 mL 0.3123 mL 0.7808 mL
100 mM 0.0250 mL 0.1249 mL 0.2499 mL 0.6247 mL
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AF-353 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:

AF-353865305-30-2Ro-4AF353AF 353Ro4Ro 4P2X ReceptorP2XRsInhibitorinhibitorinhibit

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