Cas No.: | 865305-30-2 |
Chemical 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]-;5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidine-2,4-diamine;AF 353;Ro-4 |
SMILES: | CC(C)C1=C(OC2=CN=C(N)N=C2N)C=C(I)C(OC)=C1 |
Formula: | C14H17N4O2I |
M.Wt: | 400.21438 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | AF-353 is a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist, inhibits human and rat P2X3 (pIC50= 8.0). |
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] |
In 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] |