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

AF-353 (Synonyms: Ro-4)

Cat. No.: HY-14483 Purity: 98.95%
Handling Instructions

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
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 192 In-stock
Estimated Time of Arrival: December 31
50 mg USD 780 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

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].

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.

865305-30-2

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (249.87 mM; Need ultrasonic)

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
10 mM 0.2499 mL 1.2493 mL 2.4987 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.25 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 98.95%

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AF-353
Cat. No.:
HY-14483
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