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2,4-PyriMidinediaMine, 5-[5-iodo-4-Methoxy-2-(1-Methylethyl)phenoxy]-

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CAS:865305-30-2
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  • CAS:865305-30-2
  • Purity: 99.35%
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  • af-353
  • af-353 pictures
  • $100.00
  • 2022-02-25
  • CAS:865305-30-2
  • Min. Order: 1KG
  • Purity: 99%
  • Supply Ability: 10kg
2,4-PyriMidinediaMine, 5-[5-iodo-4-Methoxy-2-(1-Methylethyl)phenoxy]- Basic information
Product Name:2,4-PyriMidinediaMine, 5-[5-iodo-4-Methoxy-2-(1-Methylethyl)phenoxy]-
Synonyms:2,4-PyriMidinediaMine, 5-[5-iodo-4-Methoxy-2-(1-Methylethyl)phenoxy]-;AF 353;Ro 4;5-{[5-iodo-2-(1-Methylethyl)-4-(Methyloxy)phenyl]oxy}-2,4-pyriMidinediaMine;CHEMBL526307;CHEMBL526307;AF 353;AF353;CS-2469;5-[5-iodo-4-methoxy-2-(1-methylethyl)phenoxy]-2,4-pyrimidinediamine hydrochloride Ro 4 hydrochloride
CAS:865305-30-2
MF:C14H17IN4O2
MW:400.21
EINECS:
Product Categories:Inhibitors
Mol File:865305-30-2.mol
2,4-PyriMidinediaMine, 5-[5-iodo-4-Methoxy-2-(1-Methylethyl)phenoxy]- Structure
2,4-PyriMidinediaMine, 5-[5-iodo-4-Methoxy-2-(1-Methylethyl)phenoxy]- Chemical Properties
Boiling point 510.2±60.0 °C(Predicted)
density 1.619±0.06 g/cm3(Predicted)
storage temp. Store at -20°C
solubility DMSO : ≥ 32 mg/mL (79.96 mM)
pka6.89±0.10(Predicted)
form Solid
color Light brown to brown
InChIInChI=1S/C14H17IN4O2/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)
InChIKeyAATPYXMXFBBKFO-UHFFFAOYSA-N
SMILESC1(N)=NC=C(OC2=CC(I)=C(OC)C=C2C(C)C)C(N)=N1
Safety Information
MSDS Information
2,4-PyriMidinediaMine, 5-[5-iodo-4-Methoxy-2-(1-Methylethyl)phenoxy]- Usage And Synthesis
DescriptionAF-353 is a noncompetitive dual antagonist of the purinoreceptors P2X3 and P2X2/3 (IC50s = 10 and 79.4 nM, respectively). It is selective for P2X3 and P2X2/3 over P2X1, P2X2, P2X4, P2X5, and P2X7 (IC50 = >10 μM for all). 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.
UsesAF-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].
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.
IC 50P2X3 Receptor
References[1] Gever JR, et al. AF-353, a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist. Br J Pharmacol. 2010 Jul;160(6):1387-1398. DOI:10.1111/j.1476-5381.2010.00796.x
[2] Munoz A, et al. Modulation of bladder afferent signals in normal and spinal cord-injured rats by purinergic P2X3 and P2X2/3receptors. BJU Int. 2012 Oct;110(8 Pt B):E409-414. DOI:10.1111/j.1464-410X.2012.11189.x
2,4-PyriMidinediaMine, 5-[5-iodo-4-Methoxy-2-(1-Methylethyl)phenoxy]- Preparation Products And Raw materials
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