A dual P2X3 and P2X2/3 receptor antagonist
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AF-353 (hydrochloride)

Item No. 23034

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[5-iodo-4-methoxy-2-(1-methylethyl)phenoxy]-2,4-pyrimidinediamine, monohydrochloride
CAS Number
927887-18-1
Molecular Formula
C14H17IN4O2 • HCl
Formula Weight
436.7
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 20 mg/ml
λmax
231 nm
SMILES
COC1=CC(C(C)C)=C(OC2=C(N)N=C(N)N=C2)C=C1I.Cl
InChi Code
InChI=1S/C14H17IN4O2.ClH/c1-7(2)8-4-11(20-3)9(15)5-10(8)21-12-6-18-14(17)19-13(12)16;/h4-7H,1-3H3,(H4,16,17,18,19);1H
InChi Key
QRBBKDZPXABQPE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $128

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    10 mg

    $235

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    Product Description

    AF-353 is a noncompetitive dual antagonist of the purinoreceptors P2X3 and P2X2/3 (IC50s = 10 and 79.4 nM, respectively).1,2 It is selective for P2X3 and P2X2/3 over P2X1, P2X2, P2X4, P2X5, and P2X7 (IC50 = >10 µM for all).2 It inhibits calcium flux in CHO-K1 cells expressing the rat P2X3 receptor and in 1321N1 cells expressing the human P2X3 and P2X2/3 receptors (IC50s = 8.91, 8.71, and 38.9 nM, respectively). AF-353 decreases the electrical signals in the detrusor, but not striated, muscle of the bladder in female rats.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Carter, D.S., Alam, M., Cai, H., et al. Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X3/P2X2/3 antagonist for the treatment of pain. Bioorg. Med. Chem. Lett. 19(6), 1628-1631 (2009).

    2. Gever, J.R., Soto, R., Henningsen, R.A., et al. AF-353, a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist. Br. J. Pharmacol. 160(6), 1387-1398 (2010).

    3. Salazar, B.H., Hoffman, K.A., Zhang, C., et al. Electrical activity of the bladder Is attenuated by intravesical inhibition of P2X2/3 receptors during micturition in female rats. Int. Neurourol. J. 21(4), 259-269 (2017).