af-353

Modify Date: 2025-08-26 19:08:24

af-353 Structure
af-353 structure
 Common Name af-353
CAS Number 865305-30-2 Molecular Weight 400.21500
Density N/A Boiling Point N/A
Molecular Formula C14H17IN4O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of af-353


AF-353 is a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist, inhibits human and rat P2X3 (pIC50= 8.0).IC50 value: pIC50 = 8.0 (pIC50, for P2X3)Target: P2X3/P2X2/3 receptorin vitro: AF-353 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. AF-353 also blocks human P2X2/3 channel function with marginally reduced potency (pIC50 = 7.3). [1]in vivo: SCI rats has significantly higher frequencies for field potentials and NVC than NL rats. Intravesical ATP increases field potential frequency in control but not SCI rats, while systemic AF-353 significantly reduces this parameter in both groups. AF-353 also reduces the inter-contractile interval in control but not in SCI rats; however, the frequency of NVC in SCI rats was significantly reduced.[2]

 Names

Name 5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidine-2,4-diamine
Synonym More Synonyms

 af-353 Biological Activity

Description AF-353 is a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist, inhibits human and rat P2X3 (pIC50= 8.0).IC50 value: pIC50 = 8.0 (pIC50, for P2X3)Target: P2X3/P2X2/3 receptorin vitro: AF-353 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. AF-353 also blocks human P2X2/3 channel function with marginally reduced potency (pIC50 = 7.3). [1]in vivo: SCI rats has significantly higher frequencies for field potentials and NVC than NL rats. Intravesical ATP increases field potential frequency in control but not SCI rats, while systemic AF-353 significantly reduces this parameter in both groups. AF-353 also reduces the inter-contractile interval in control but not in SCI rats; however, the frequency of NVC in SCI rats was significantly reduced.[2]
Related Catalog
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.

[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.

 Chemical & Physical Properties

Molecular Formula C14H17IN4O2
Molecular Weight 400.21500
Exact Mass 400.04000
PSA 97.74000
LogP 3.03010
InChIKey AATPYXMXFBBKFO-UHFFFAOYSA-N
SMILES COc1cc(C(C)C)c(Oc2cnc(N)nc2N)cc1I

 af-353Bioassay

View more

Name: Inhibition of Staphylococcus aureus DHFR expressed in Escherichia coli BL21 (DE3) usi...
Source: ChEMBL
Target: Dihydrofolate reductase
External Id: CHEMBL5531642
Name: Half life in dog
Source: ChEMBL
Target: Canis lupus familiaris
External Id: CHEMBL960851
Name: Inhibition of human DHFR at 100 nM relative to control
Source: ChEMBL
Target: Dihydrofolate reductase
External Id: CHEMBL5531641
Name: Ratio of permeability from basolateral to apical side over apical to basolateral side...
Source: ChEMBL
Target: Caco-2
External Id: CHEMBL960852
Name: Primary qHTS assay for small molecule inhibitors of Inositol hexaphosphate kinase 1 (...
Source: NCGC
External Id: IP6K1-p1
Name: Cytotoxicity against human NCM460 cells assessed as inhibition rate of cell growth at...
Source: ChEMBL
Target: NCM460
External Id: CHEMBL5531640
Name: Clearance in dog
Source: ChEMBL
Target: Canis lupus familiaris
External Id: CHEMBL960849
Name: Tmax in rat at 2 mg/kg, iv administered as single dose
Source: ChEMBL
Target: Rattus norvegicus
External Id: CHEMBL1017983
Name: Cytotoxicity against HEK293 cells assessed as inhibition rate of cell growth at 100 u...
Source: ChEMBL
Target: HEK293
External Id: CHEMBL5531639
Name: Oral bioavailability in dog
Source: ChEMBL
Target: Canis lupus familiaris
External Id: CHEMBL960850
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 Synonyms

af-353
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Chemsrc provides af-353(CAS#:865305-30-2) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of af-353 are included as well.>> amp version: af-353

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