1. Membrane Transporter/Ion Channel
  2. P2X Receptor
  3. P2X3 antagonist 34

P2X3 antagonist 34 

Cat. No.: HY-135976 Purity: 99.42% ee.: 99.86%
Handling Instructions

P2X3 antagonist 34 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC50s of 25 nM, 92 nM and 126 nM for human P2X3, rat P2X3 and guinea pig P2X3 receptors, respectively. P2X3 antagonist 34 is less active against human, rat and guinea pig P2X2/3 heterotrimeric receptors. P2X3 antagonist 34 has strong anti-tussive effect.

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

P2X3 antagonist 34 Chemical Structure

P2X3 antagonist 34 Chemical Structure

CAS No. : 2417288-67-4

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Description

P2X3 antagonist 34 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC50s of 25 nM, 92 nM and 126 nM for human P2X3, rat P2X3 and guinea pig P2X3 receptors, respectively. P2X3 antagonist 34 is less active against human, rat and guinea pig P2X2/3 heterotrimeric receptors. P2X3 antagonist 34 has strong anti-tussive effect[1].

IC50 & Target

IC50: 25 nM (Human P2X3 receptor), 92 nM (Rat P2X3 receptor)and 126 nM (Guinea pig P2X3 receptor), 1820 nM (Rat P2X2/3 heterotrimeric receptor) and 3450 nM (Guinea pig P2X2/3 heterotrimeric receptor)[1]

In Vitro

P2X3 antagonist 34 (BLU-5937; 500 nM) is able to block αβ-meATP-induced sensitization and firing activity of isolated primary nociceptors in rat dorsal root ganglions (DRGs), through P2X3 homotrimeric receptor antagonism. The sensitizing effect of αβ-meATP and the inhibition of P2X3 antagonist 34 are reversible after washout[1].

In Vivo

P2X3 antagonist 34 (BLU-5937; 0.3-0 mg/kg, oral administration; male Dunkin Hartley guinea pigs) treatment significantly reduces the histamine-induced enhancement in the number of citric acid-induced coughs in a dose-dependent fashion in a guinea pig cough model[1].
P2X3 antagonist 34 (BLU-5937; 3 and 30 mg/kg, oral) is also shown to reduce significantly and dose-dependently the ATP-induced enhancement of citric acid-induced coughs in the guinea pig[1].

Animal Model: Male Dunkin Hartley guinea pigs[1]
Dosage: 0.3 mg/kg, 3 mg/kg, 30 mg/kg
Administration: Oral administration
Result: Significantly reduced the histamine-induced enhancement in the number of citric acid-induced coughs in a dose-dependent fashion.
Molecular Weight

456.49

Formula

C₂₄H₂₆F₂N₄O₃

CAS No.

2417288-67-4

SMILES

O=C(OC)N1C[[email protected]@H](CCC1)CC2=C(N=C3C=C(C=CN32)C)C4=C(C=C(C=C4F)C(NC)=O)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (219.06 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1906 mL 10.9531 mL 21.9063 mL
5 mM 0.4381 mL 2.1906 mL 4.3813 mL
10 mM 0.2191 mL 1.0953 mL 2.1906 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: ≥ 5 mg/mL (10.95 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 5 mg/mL (10.95 mM); Clear solution

  • 3.

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

    Solubility: ≥ 5 mg/mL (10.95 mM); Clear solution

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

P2X3 antagonist 34P2X ReceptorP2XRsP2X3anti-tussiveATPion-gatedhomotrimerichypersensitizationnon-competitiveαβ-meATPchroniccoughInhibitorinhibitorinhibit

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P2X3 antagonist 34
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HY-135976
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